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GnRH agonist

Nafarelin

Published evidence · coverage incomplete

Anatomy in the research

Anatomy evidence is still being assembled.

These are anatomical mentions in cited research—not established treatment targets or proof of benefit in people.

This publication has no anatomy passages that meet our source-linking checks yet. Read the available findings ↓

General anatomy view only. No peptide-specific structures are highlighted.

At a glance

What is it—and why does it matter?

Nafarelin acts as an agonist at the gonadotropin releasing hormone (GnRH) receptor. Nafarelin is described as a gonadotropin-releasing hormone (GnRH) agonist; in this source it is stated to reversibly suppress ovarian function and induce a low-estrogen (hypoestrogenemic) state. Quantitative CT measurements showed decreases in vertebral trabecular bone density and total vertebral bone mass after six months of SYNAREL, with partial post-treatment recovery that remained below pretreatment on average.

Sources for this introduction: [1] [2] [3]

This published profile is a reference in progress. Findings retain their source context; missing topics are marked below.

What is it?

A molecule, not a product name.

Identity

Nafarelin acts as an agonist at gonadotropin-releasing hormone (GnRH) pathways.

Sources[4]doiAbsorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone.Nafarelin, a potent gonadotropin-releasing hormone (GnRH) agonist,[11]pubmedAbsorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone.Nafarelin, a potent gonadotropin-releasing hormone (GnRH) agonist,
Molecular / pharmacology evidence

2 cited sources · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

2 cited passages across 2 source records. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Nafarelin, a potent gonadotropin-releasing hormone (GnRH) agonist,”

    Absorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone. · Abstract

    doi:10.1038/clpt.1988.150:09613316ad4b:09613316ad4b
  2. supports · Source-backed record
    “Nafarelin, a potent gonadotropin-releasing hormone (GnRH) agonist,”

    Absorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone. · Abstract

    pubmed:2970910:f5314fec7d78:f5314fec7d78

Identity

Nafarelin is classified as a peptide ligand (Ligand ID: 3902).

Sources[6]iuphar-ligandnafarelinName: nafarelin Ligand ID: 3902 Type: Peptide
Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Name: nafarelin Ligand ID: 3902 Type: Peptide”

    nafarelin · Identity and approval

    iuphar-ligand:3902:3505c7ebf6ec:3505c7ebf6ec

Identity

In ChEMBL, nafafrelin (CHEMBL1201309) is classified with molecule type “Protein,” with preferred name “NAFARELIN.”

Sources[2]chembl-moleculeNAFARELINChEMBL ID: CHEMBL1201309 Preferred name: NAFARELIN Molecule type: Protein
Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “ChEMBL ID: CHEMBL1201309 Preferred name: NAFARELIN Molecule type: Protein”

    NAFARELIN · Molecule identity

    chembl-molecule:chembl1201309:a04eee51f26c:a04eee51f26c

Identity

Nafarelin acetate is a synthetically produced analog of endogenous gonadotropin-releasing hormone (GnRH).

Sources[3]dailymedSynarel®(nafarelin acetate)nasal solutionNafarelin acetate is a synthetic analog of the naturally occurring gonadotropin-releasing hormone (GnRH).
Regulatory record

1 cited source · 1 regulatory record

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Nafarelin acetate is a synthetic analog of the naturally occurring gonadotropin-releasing hormone (GnRH).”

    Synarel®(nafarelin acetate)nasal solution · DESCRIPTION

    dailymed:d0aa57cb-d2f4-46d7-af43-7c8b06aa81a6:e94a8d18814b:e94a8d18814b

Identity

Nafarelin is a synthetic agonist of gonadotrophin-releasing hormone (GnRH), also referred to as luteinising hormone-releasing hormone (LH-RH) or gonadorelin.

Sources[9]pubmedNafarelin. A review of its pharmacodynamic and pharmacokinetic properties, and clinical potential in sex hormone-related conditions.Nafarelin, a synthetic agonist of gonadotrophin-releasing hormone (GnRH) [luteinising hormone-releasing hormone (LH-RH); gonadorelin]
Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Nafarelin, a synthetic agonist of gonadotrophin-releasing hormone (GnRH) [luteinising hormone-releasing hormone (LH-RH); gonadorelin]”

    Nafarelin. A review of its pharmacodynamic and pharmacokinetic properties, and clinical potential in sex hormone-related conditions. · Abstract

    pubmed:2140979:7b7ec0510792:7b7ec0510792

Identity

Nafarelin acetate is a 10–amino-acid peptide (decapeptide) used as the active drug in SYNAREL nasal solution.

Sources[3]dailymedSynarel®(nafarelin acetate)nasal solutionNafarelin acetate, the active component of SYNAREL Nasal Solution, is a decapeptide
Regulatory record

1 cited source · 1 regulatory record

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Nafarelin acetate, the active component of SYNAREL Nasal Solution, is a decapeptide”

    Synarel®(nafarelin acetate)nasal solution · DESCRIPTION

    dailymed:d0aa57cb-d2f4-46d7-af43-7c8b06aa81a6:e94a8d18814b:e94a8d18814b

Identity

Nafarelin acts as an agonist at the gonadotropin releasing hormone (GnRH) receptor.

Sources[5]iuphar-commentsIUPHAR ligand commentaryNafarelin is a gonadotropin releasing hormone receptor agonist.
Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Nafarelin is a gonadotropin releasing hormone receptor agonist.”

    IUPHAR ligand commentary · General comments

    iuphar-comments:3902:77a29e62c52d:77a29e62c52d

Identity

The molecular formula reported for nafafrelin is C66H83N17O13, indicating its elemental composition.

Sources[2]chembl-moleculeNAFARELINMolecular formula: C66H83N17O13
Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecular formula: C66H83N17O13”

    NAFARELIN · Molecular properties

    chembl-molecule:chembl1201309:a04eee51f26c:a04eee51f26c

How does it work?

Target, response, and disposition.

Mechanism

As a potent GnRH agonist analog, nafarelin produces an initial pituitary gonadotropin (LH/FSH) surge; with repeated dosing, the pituitary becomes nonresponsive to continued stimulation.

Sources[3]dailymedSynarel®(nafarelin acetate)nasal solutionNafarelin acetate is a potent agonistic analog of gonadotropin-releasing hormone (GnRH). At the onset of administration, nafarelin stimulates the release of the pituitary gonadotropins, LH and FSH, resulting in a temporary increase of gonadal steroidogenesis. Repeated dosing abolishes the stimulatory effect on the pituitary gland.
Regulatory record

1 cited source · 1 regulatory record

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Nafarelin acetate is a potent agonistic analog of gonadotropin-releasing hormone (GnRH). At the onset of administration, nafarelin stimulates the release of the pituitary gonadotropins, LH and FSH, resulting in a temporary increase of gonadal steroidogenesis. Repeated dosing abolishes the stimulatory effect on the pituitary gland.”

    Synarel®(nafarelin acetate)nasal solution · CLINICAL PHARMACOLOGY

    dailymed:d0aa57cb-d2f4-46d7-af43-7c8b06aa81a6:e94a8d18814b:e94a8d18814b

Mechanism

Repeated administration of the GnRH agonist nafarelin leads to pituitary desensitisation, which suppresses gonadotrophin release and thereby inhibits downstream sex hormone synthesis.

Sources[9]pubmedNafarelin. A review of its pharmacodynamic and pharmacokinetic properties, and clinical potential in sex hormone-related conditions.With repeated administration, the pituitary becomes desensitised, and gonadotrophin release, and therefore sex hormone synthesis, are inhibited.
Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “With repeated administration, the pituitary becomes desensitised, and gonadotrophin release, and therefore sex hormone synthesis, are inhibited.”

    Nafarelin. A review of its pharmacodynamic and pharmacokinetic properties, and clinical potential in sex hormone-related conditions. · Abstract

    pubmed:2140979:7b7ec0510792:7b7ec0510792

Mechanism

Nafarelin is described as a gonadotropin-releasing hormone (GnRH) agonist; in this source it is stated to reversibly suppress ovarian function and induce a low-estrogen (hypoestrogenemic) state.

Sources[10]pubmedAdministration of nasal nafarelin as compared with oral danazol for endometriosis. A multicenter double-blind comparative clinical trial.Treatment with nafarelin, a gonadotropin-releasing hormone agonist, reversibly inhibits ovarian function and induces hypoestrogenemia.
Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Treatment with nafarelin, a gonadotropin-releasing hormone agonist, reversibly inhibits ovarian function and induces hypoestrogenemia.”

    Administration of nasal nafarelin as compared with oral danazol for endometriosis. A multicenter double-blind comparative clinical trial. · Abstract

    pubmed:2963213:926fdcf39aa7:926fdcf39aa7

Mechanism

Binding kinetics for CHEMBL1201309 at the gonadotropin-releasing hormone receptor (CHEMBL1855) included an association rate constant (kon) of 0.139 nM^-1 min^-1 measured in a TR-FRET competitive binding format.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL1201309Molecule: CHEMBL1201309 Target: Gonadotropin-releasing hormone receptor (CHEMBL1855) Assay: The basic principle of this assay is explained in (Schiele et al., 2014). Prior to eachexperiment, 6 uL of fluorescent probe (final concentration 15 nM) was dispensed to the assayready plates containing 100 nl of compound dilutions using a Multidrop Combi and the injection system of the PHERAstar FS plate reader was washed with NaOH/H20 and primed with Tag-liteâ„¢ cells. Finally, the assay plates were introduced into the instrument, 4 ul of cells (1000 cells/ul) were rapidly dispensed with the syringe to each well and the TR-FRET signals corresponding to the competitive binding of probe and test compounds were recorded with kinetic intervals of 78 seconds. (excitation: 5 laser flashes at a wavelength of 337 nm; emission at wavelengths of 520 nm and 490 nm ) Assay format: assay format Standard result: kon 0.139 nM^-1 min^-1 Document: CHEMBL3885741
Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL1201309 Target: Gonadotropin-releasing hormone receptor (CHEMBL1855) Assay: The basic principle of this assay is explained in (Schiele et al., 2014). Prior to eachexperiment, 6 uL of fluorescent probe (final concentration 15 nM) was dispensed to the assayready plates containing 100 nl of compound dilutions using a Multidrop Combi and the injection system of the PHERAstar FS plate reader was washed with NaOH/H20 and primed with Tag-liteâ„¢ cells. Finally, the assay plates were introduced into the instrument, 4 ul of cells (1000 cells/ul) were rapidly dispensed with the syringe to each well and the TR-FRET signals corresponding to the competitive binding of probe and test compounds were recorded with kinetic intervals of 78 seconds. (excitation: 5 laser flashes at a wavelength of 337 nm; emission at wavelengths of 520 nm and 490 nm ) Assay format: assay format Standard result: kon 0.139 nM^-1 min^-1 Document: CHEMBL3885741”

    ChEMBL activities for CHEMBL1201309 · Activity 16915332

    chembl-activities:chembl1201309:c690379eb996:c690379eb996

Mechanism

Binding kinetics were reported for CHEMBL1201309 at the gonadotropin-releasing hormone receptor (CHEMBL1855), including an off-rate (koff) of 0.025 min^-1 measured using a TR-FRET competitive binding setup.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL1201309Molecule: CHEMBL1201309 Target: Gonadotropin-releasing hormone receptor (CHEMBL1855) Assay: The basic principle of this assay is explained in (Schiele et al., 2014). Prior to eachexperiment, 6 uL of fluorescent probe (final concentration 15 nM) was dispensed to the assayready plates containing 100 nl of compound dilutions using a Multidrop Combi and the injection system of the PHERAstar FS plate reader was washed with NaOH/H20 and primed with Tag-liteâ„¢ cells. Finally, the assay plates were introduced into the instrument, 4 ul of cells (1000 cells/ul) were rapidly dispensed with the syringe to each well and the TR-FRET signals corresponding to the competitive binding of probe and test compounds were recorded with kinetic intervals of 78 seconds. (excitation: 5 laser flashes at a wavelength of 337 nm; emission at wavelengths of 520 nm and 490 nm ) Assay format: assay format Standard result: koff 0.025 min^-1 Document: CHEMBL3885741
Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL1201309 Target: Gonadotropin-releasing hormone receptor (CHEMBL1855) Assay: The basic principle of this assay is explained in (Schiele et al., 2014). Prior to eachexperiment, 6 uL of fluorescent probe (final concentration 15 nM) was dispensed to the assayready plates containing 100 nl of compound dilutions using a Multidrop Combi and the injection system of the PHERAstar FS plate reader was washed with NaOH/H20 and primed with Tag-liteâ„¢ cells. Finally, the assay plates were introduced into the instrument, 4 ul of cells (1000 cells/ul) were rapidly dispensed with the syringe to each well and the TR-FRET signals corresponding to the competitive binding of probe and test compounds were recorded with kinetic intervals of 78 seconds. (excitation: 5 laser flashes at a wavelength of 337 nm; emission at wavelengths of 520 nm and 490 nm ) Assay format: assay format Standard result: koff 0.025 min^-1 Document: CHEMBL3885741”

    ChEMBL activities for CHEMBL1201309 · Activity 16915329

    chembl-activities:chembl1201309:c690379eb996:c690379eb996

Pharmacokinetics

Urinary radioactivity after subcutaneous radiolabeled nafarelin was largely attributable to six metabolites.

Sources[11]pubmedAbsorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone.Six metabolites accounted for most of the radioactivity in urine.
Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Six metabolites accounted for most of the radioactivity in urine.”

    Absorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone. · Abstract

    pubmed:2970910:f5314fec7d78:f5314fec7d78

Pharmacokinetics

Pediatric intranasal nafarelin shows rapid absorption with Tmax 10–45 minutes, and observed Cmax values of 2.2 ng/mL (400 µg base) and 6.6 ng/mL (600 µg base) by RIA.

Sources[3]dailymedSynarel®(nafarelin acetate)nasal solutionInchildren,nafarelin acetate was rapidly absorbed into the systemic circulation after intranasal administration. Maximum serum concentrations (measured by RIA) were achieved between 10 and 45 minutes. Following a single dose of 400 µg base, the observed peak concentration was 2.2 ng/mL, whereas following a single dose of 600 µg base, the observed peak concentration was 6.6 ng/mL.
Regulatory record

1 cited source · 1 regulatory record

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Inchildren,nafarelin acetate was rapidly absorbed into the systemic circulation after intranasal administration. Maximum serum concentrations (measured by RIA) were achieved between 10 and 45 minutes. Following a single dose of 400 µg base, the observed peak concentration was 2.2 ng/mL, whereas following a single dose of 600 µg base, the observed peak concentration was 6.6 ng/mL.”

    Synarel®(nafarelin acetate)nasal solution · CLINICAL PHARMACOLOGY

    dailymed:d0aa57cb-d2f4-46d7-af43-7c8b06aa81a6:e94a8d18814b:e94a8d18814b

Pharmacokinetics

Nafarelin is eliminated from serum with an approximate half-life of 2 hours.

Sources[4]doiAbsorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone.Serum elimination half-life was about 2 hours.[11]pubmedAbsorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone.Serum elimination half-life was about 2 hours.
Molecular / pharmacology evidence

2 cited sources · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

2 cited passages across 2 source records. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Serum elimination half-life was about 2 hours.”

    Absorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone. · Abstract

    doi:10.1038/clpt.1988.150:09613316ad4b:09613316ad4b
  2. supports · Source-backed record
    “Serum elimination half-life was about 2 hours.”

    Absorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone. · Abstract

    pubmed:2970910:f5314fec7d78:f5314fec7d78

Pharmacokinetics

An ex vivo intestinal stability assay using a rat jejunum sac reported a half-life (T1/2) of 0.4667 hr for CHEMBL1201309.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL1201309Molecule: CHEMBL1201309 Target: Rattus norvegicus (CHEMBL376) Assay: Intestinal stability against rat jejunum sac, activity is expressed as T1/2 Assay format: organism-based format Standard result: T1/2 = 0.4667 hr Document: CHEMBL1126585
Animal / laboratory evidence

1 cited source · Study independence not established

Animal or laboratory findings do not establish benefit or safety in people.

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL1201309 Target: Rattus norvegicus (CHEMBL376) Assay: Intestinal stability against rat jejunum sac, activity is expressed as T1/2 Assay format: organism-based format Standard result: T1/2 = 0.4667 hr Document: CHEMBL1126585”

    ChEMBL activities for CHEMBL1201309 · Activity 865743

    chembl-activities:chembl1201309:c690379eb996:c690379eb996

Pharmacokinetics

A rat in vivo pharmacokinetic measurement reported systemic clearance (CL) for CHEMBL1201309 as 5.5 mL.min-1.kg-1 following an iv dose of 100 ug/kg.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL1201309Molecule: CHEMBL1201309 Target: Rattus norvegicus (CHEMBL376) Assay: Clearance in rat after iv dose (100 ug/kg) Assay format: organism-based format Standard result: CL = 5.5 mL.min-1.kg-1 Document: CHEMBL1126585
Animal / laboratory evidence

1 cited source · Study independence not established

Animal or laboratory findings do not establish benefit or safety in people.

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL1201309 Target: Rattus norvegicus (CHEMBL376) Assay: Clearance in rat after iv dose (100 ug/kg) Assay format: organism-based format Standard result: CL = 5.5 mL.min-1.kg-1 Document: CHEMBL1126585”

    ChEMBL activities for CHEMBL1201309 · Activity 865744

    chembl-activities:chembl1201309:c690379eb996:c690379eb996

Pharmacokinetics

Mass-balance data in men given subcutaneous radiolabeled nafarelin show urinary recovery of 44–55% and fecal recovery of 18.5–44.2%, with ~3% excreted unchanged in urine.

Sources[3]dailymedSynarel®(nafarelin acetate)nasal solutionAfter subcutaneous administration of14C-nafarelin acetate to men, 44–55% of the dose was recovered in urine and 18.5–44.2% was recovered in feces. Approximately 3% of the administered dose appeared as unchanged nafarelin in urine.
Regulatory record

1 cited source · 1 regulatory record

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “After subcutaneous administration of14C-nafarelin acetate to men, 44–55% of the dose was recovered in urine and 18.5–44.2% was recovered in feces. Approximately 3% of the administered dose appeared as unchanged nafarelin in urine.”

    Synarel®(nafarelin acetate)nasal solution · CLINICAL PHARMACOLOGY

    dailymed:d0aa57cb-d2f4-46d7-af43-7c8b06aa81a6:e94a8d18814b:e94a8d18814b

Pharmacokinetics

The abstract identifies urinary metabolite identities: four short peptide fragments derived from nafarelin and two non-peptide metabolites (naphthylalanine and 2-naphthylacetic acid).

Sources[11]pubmedAbsorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone.Four metabolites were short peptide fragments of nafarelin and the other metabolites were naphthylalanine and 2-naphthylacetic acid.
Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Four metabolites were short peptide fragments of nafarelin and the other metabolites were naphthylalanine and 2-naphthylacetic acid.”

    Absorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone. · Abstract

    pubmed:2970910:f5314fec7d78:f5314fec7d78

Pharmacokinetics

Protein binding of nafarelin acetate is reported as about 80% at 4°C.

Sources[3]dailymedSynarel®(nafarelin acetate)nasal solutionAbout 80% of nafarelin acetate was bound to plasma proteins at 4°C.
Regulatory record

1 cited source · 1 regulatory record

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “About 80% of nafarelin acetate was bound to plasma proteins at 4°C.”

    Synarel®(nafarelin acetate)nasal solution · CLINICAL PHARMACOLOGY

    dailymed:d0aa57cb-d2f4-46d7-af43-7c8b06aa81a6:e94a8d18814b:e94a8d18814b

Pharmacokinetics

Following subcutaneous dosing with radiolabeled nafarelin, excreted radioactivity was distributed approximately equally between urinary and fecal routes.

Sources[11]pubmedAbsorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone.Radioactivity was excreted in approximately equal amounts in urine and stool.
Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Radioactivity was excreted in approximately equal amounts in urine and stool.”

    Absorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone. · Abstract

    pubmed:2970910:f5314fec7d78:f5314fec7d78

Pharmacokinetics

Intranasal nafarelin shows rapid systemic absorption, achieving peak concentration within 20 to 40 minutes.

Sources[4]doiAbsorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone.Nafarelin, a potent gonadotropin-releasing hormone (GnRH) agonist, was absorbed rapidly into systemic circulation (time to reach peak concentration, 20 to 40 minutes) after intranasal[11]pubmedAbsorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone.was absorbed rapidly into systemic circulation (time to reach peak concentration, 20 to 40 minutes) after intranasal
Molecular / pharmacology evidence

2 cited sources · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

2 cited passages across 2 source records. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Nafarelin, a potent gonadotropin-releasing hormone (GnRH) agonist, was absorbed rapidly into systemic circulation (time to reach peak concentration, 20 to 40 minutes) after intranasal”

    Absorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone. · Abstract

    doi:10.1038/clpt.1988.150:09613316ad4b:09613316ad4b
  2. supports · Source-backed record
    “was absorbed rapidly into systemic circulation (time to reach peak concentration, 20 to 40 minutes) after intranasal”

    Absorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone. · Abstract

    pubmed:2970910:f5314fec7d78:f5314fec7d78

Pharmacokinetics

Relative bioavailability compares exposure from the nasal formulation to exposure after a single subcutaneous dose; the average reported value was 21%.

Sources[11]pubmedAbsorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone.Bioavailability of this nasal formulation relative to a single subcutaneous dose averaged 21%.
Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Bioavailability of this nasal formulation relative to a single subcutaneous dose averaged 21%.”

    Absorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone. · Abstract

    pubmed:2970910:f5314fec7d78:f5314fec7d78

What has been studied?

What the evidence says.

Study findings

Both study arms showed statistically significant reductions in patient-reported pelvic pain scores after 6 months, indicating improvement over time in each group.

Sources[12]pubmedUse of nafarelin versus placebo after reductive laparoscopic surgery for endometriosis.The patients' pelvic pain scores dropped significantly in the nafarelin and placebo groups after 6 months of treatment.
Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “The patients' pelvic pain scores dropped significantly in the nafarelin and placebo groups after 6 months of treatment.”

    Use of nafarelin versus placebo after reductive laparoscopic surgery for endometriosis. · RESULT(S)

    pubmed:9389816:70134bba7266:70134bba7266

Study findings

Primary endpoints included a time-to-event measure (initiation of alternative treatment) and pelvic pain assessments reported by patients and evaluated by physicians.

Sources[12]pubmedUse of nafarelin versus placebo after reductive laparoscopic surgery for endometriosis.Time to initiation of alternative treatment (the length of time from beginning study medication to receiving alternative therapy or to deeming that the study drug was ineffective) and patient-reported and physician-assessed pelvic pain scores.
Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Time to initiation of alternative treatment (the length of time from beginning study medication to receiving alternative therapy or to deeming that the study drug was ineffective) and patient-reported and physician-assessed pelvic pain scores.”

    Use of nafarelin versus placebo after reductive laparoscopic surgery for endometriosis. · MAIN OUTCOME MEASURE(S)

    pubmed:9389816:70134bba7266:70134bba7266

Study findings

Across reviewed clinical trials, nafarelin was reported to reduce uterine size, suggesting shrinkage of the enlarged uterus associated with leiomyomas.

Sources[7]pubmedClinical use of nafarelin in the treatment of leiomyomas. A review of the literature.Nafarelin consistently suppressed estrogen production, reduced leiomyoma and uterine size, and controlled menorrhagia.
Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Nafarelin consistently suppressed estrogen production, reduced leiomyoma and uterine size, and controlled menorrhagia.”

    Clinical use of nafarelin in the treatment of leiomyomas. A review of the literature. · RESULTS

    pubmed:10900582:13b5094018c2:13b5094018c2

Study findings

In this randomized, placebo-controlled multicenter trial, nafarelin was associated with a longer median time until alternative treatment was initiated than placebo.

Sources[12]pubmedUse of nafarelin versus placebo after reductive laparoscopic surgery for endometriosis.The median time to initiation of alternative treatment was > 24 months in the nafarelin group versus 11.7 months in the placebo group.
Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “The median time to initiation of alternative treatment was > 24 months in the nafarelin group versus 11.7 months in the placebo group.”

    Use of nafarelin versus placebo after reductive laparoscopic surgery for endometriosis. · RESULT(S)

    pubmed:9389816:70134bba7266:70134bba7266

Study findings

Across the reviewed clinical trials, nafarelin was reported to suppress estrogen production, consistent with a systemic endocrine effect in leiomyoma patients.

Sources[7]pubmedClinical use of nafarelin in the treatment of leiomyomas. A review of the literature.Nafarelin consistently suppressed estrogen production, reduced leiomyoma and uterine size, and controlled menorrhagia.
Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Nafarelin consistently suppressed estrogen production, reduced leiomyoma and uterine size, and controlled menorrhagia.”

    Clinical use of nafarelin in the treatment of leiomyomas. A review of the literature. · RESULTS

    pubmed:10900582:13b5094018c2:13b5094018c2

Study findings

The reviewed trials reported improvements in hematologic parameters with nafarelin, both among women with anemia and those without anemia.

Sources[7]pubmedClinical use of nafarelin in the treatment of leiomyomas. A review of the literature.In addition, nafarelin improved hematologic parameters in women with and without anemia.
Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “In addition, nafarelin improved hematologic parameters in women with and without anemia.”

    Clinical use of nafarelin in the treatment of leiomyomas. A review of the literature. · RESULTS

    pubmed:10900582:13b5094018c2:13b5094018c2

Study findings

The review’s conclusion states that nafarelin effectively decreases uterine bleeding in women with symptomatic leiomyomas, indicating clinically meaningful reduction in bleeding in that population.

Sources[7]pubmedClinical use of nafarelin in the treatment of leiomyomas. A review of the literature.Nafarelin treatment of women with symptomatic leiomyomas effectively decreases uterine bleeding; improves hematologic parameters; manages symptoms of menometrorrhagia, dysmenorrhea and pelvic discomfort; reduces uterine and myoma size; and is well tolerated.
Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Nafarelin treatment of women with symptomatic leiomyomas effectively decreases uterine bleeding; improves hematologic parameters; manages symptoms of menometrorrhagia, dysmenorrhea and pelvic discomfort; reduces uterine and myoma size; and is well tolerated.”

    Clinical use of nafarelin in the treatment of leiomyomas. A review of the literature. · CONCLUSION

    pubmed:10900582:13b5094018c2:13b5094018c2

Study findings

The reviewed trials reported control of menorrhagia with nafarelin, indicating improvement in heavy menstrual bleeding in leiomyoma patients.

Sources[7]pubmedClinical use of nafarelin in the treatment of leiomyomas. A review of the literature.Nafarelin consistently suppressed estrogen production, reduced leiomyoma and uterine size, and controlled menorrhagia.
Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Nafarelin consistently suppressed estrogen production, reduced leiomyoma and uterine size, and controlled menorrhagia.”

    Clinical use of nafarelin in the treatment of leiomyomas. A review of the literature. · RESULTS

    pubmed:10900582:13b5094018c2:13b5094018c2

Study findings

The reviewed clinical trial literature reported that nafarelin reduced leiomyoma size, indicating a decrease in fibroid burden during treatment.

Sources[7]pubmedClinical use of nafarelin in the treatment of leiomyomas. A review of the literature.Nafarelin consistently suppressed estrogen production, reduced leiomyoma and uterine size, and controlled menorrhagia.
Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Nafarelin consistently suppressed estrogen production, reduced leiomyoma and uterine size, and controlled menorrhagia.”

    Clinical use of nafarelin in the treatment of leiomyomas. A review of the literature. · RESULTS

    pubmed:10900582:13b5094018c2:13b5094018c2

Study findings

An in vitro functional assay measured LH release from cultured rat pituitary cells in response to CHEMBL1201309, reporting potency as pD2 = 11.05.

Sources[1]chembl-activitiesChEMBL activities for CHEMBL1201309Molecule: CHEMBL1201309 Target: Rattus norvegicus (CHEMBL376) Assay: Tested in vitro for LH release from cultured rat pituitary cells, activity is expressed as pD2 value Assay format: organism-based format Standard result: pD2 = 11.05 Document: CHEMBL1126585
Animal / laboratory evidence

1 cited source · Study independence not established

Animal or laboratory findings do not establish benefit or safety in people.

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecule: CHEMBL1201309 Target: Rattus norvegicus (CHEMBL376) Assay: Tested in vitro for LH release from cultured rat pituitary cells, activity is expressed as pD2 value Assay format: organism-based format Standard result: pD2 = 11.05 Document: CHEMBL1126585”

    ChEMBL activities for CHEMBL1201309 · Activity 865741

    chembl-activities:chembl1201309:c690379eb996:c690379eb996

Risks and interactions

Risks, organized for scanning.

Contraindications

The contraindications state avoidance in pregnancy (or potential pregnancy) and note rat findings of major fetal abnormalities after administration during organogenesis.

Sources[3]dailymedSynarel®(nafarelin acetate)nasal solutionUse in pregnancy or in women who may become pregnant while receiving the drug. SYNAREL may cause fetal harm when administered to a pregnant woman. Major fetal abnormalities were observed in rats, but not in mice or rabbits after administration of SYNAREL during the period of organogenesis.
Animal / laboratory evidence

1 cited source · 1 regulatory record

Animal or laboratory findings do not establish benefit or safety in people.

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Use in pregnancy or in women who may become pregnant while receiving the drug. SYNAREL may cause fetal harm when administered to a pregnant woman. Major fetal abnormalities were observed in rats, but not in mice or rabbits after administration of SYNAREL during the period of organogenesis.”

    Synarel®(nafarelin acetate)nasal solution · CONTRAINDICATIONS

    dailymed:d0aa57cb-d2f4-46d7-af43-7c8b06aa81a6:e94a8d18814b:e94a8d18814b

Safety findings

Across pediatric clinical trials (n=155), the reported rate of symptoms suggestive of hypersensitivity/drug sensitivity was 2.6%, including respiratory, chest, and cutaneous manifestations.

Sources[3]dailymedSynarel®(nafarelin acetate)nasal solutionIn clinical trials of 155 pediatric patients, 2.6% reported symptoms suggestive of drug sensitivity, such as shortness of breath, chest pain, urticaria, rash, and pruritus.
Regulatory record

1 cited source · 1 regulatory record

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “In clinical trials of 155 pediatric patients, 2.6% reported symptoms suggestive of drug sensitivity, such as shortness of breath, chest pain, urticaria, rash, and pruritus.”

    Synarel®(nafarelin acetate)nasal solution · ADVERSE REACTIONS

    dailymed:d0aa57cb-d2f4-46d7-af43-7c8b06aa81a6:e94a8d18814b:e94a8d18814b

Safety findings

Quantitative CT measurements showed decreases in vertebral trabecular bone density and total vertebral bone mass after six months of SYNAREL, with partial post-treatment recovery that remained below pretreatment on average.

Sources[3]dailymedSynarel®(nafarelin acetate)nasal solutionAfter six months of treatment with SYNAREL, vertebral trabecular bone density and total vertebral bone mass, measured by quantitative computed tomography (QCT), decreased by an average of 8.7% and 4.3%, respectively, compared to pretreatment levels. There was partial recovery of bone density in the post-treatment period; the average trabecular bone density and total bone mass were 4.9% and 3.3% less than the pretreatment levels, respectively.
Regulatory record

1 cited source · 1 regulatory record

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “After six months of treatment with SYNAREL, vertebral trabecular bone density and total vertebral bone mass, measured by quantitative computed tomography (QCT), decreased by an average of 8.7% and 4.3%, respectively, compared to pretreatment levels. There was partial recovery of bone density in the post-treatment period; the average trabecular bone density and total bone mass were 4.9% and 3.3% less than the pretreatment levels, respectively.”

    Synarel®(nafarelin acetate)nasal solution · Changes in Bone Density

    dailymed:d0aa57cb-d2f4-46d7-af43-7c8b06aa81a6:e94a8d18814b:e94a8d18814b

Products and regulatory status

Same ingredient. Different records.

Regulatory status

The labeled indication includes treatment of gonadotropin-dependent central precocious puberty in pediatric patients of both sexes.

Sources[3]dailymedSynarel®(nafarelin acetate)nasal solutionSYNAREL is indicated for treatment ofcentral precocious puberty (CPP)(gonadotropin-dependent precocious puberty) in children of both sexes.
Regulatory record

1 cited source · 1 regulatory record

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “SYNAREL is indicated for treatment ofcentral precocious puberty (CPP)(gonadotropin-dependent precocious puberty) in children of both sexes.”

    Synarel®(nafarelin acetate)nasal solution · INDICATIONS AND USAGE FOR CENTRAL PRECOCIOUS PUBERTY

    dailymed:d0aa57cb-d2f4-46d7-af43-7c8b06aa81a6:e94a8d18814b:e94a8d18814b

Regulatory status

The labeled indication includes management of endometriosis (pain relief and reduction of endometriotic lesions), with stated experience limited to adult women (18 years and older) treated for 6 months.

Sources[3]dailymedSynarel®(nafarelin acetate)nasal solutionSYNAREL is indicated for management of endometriosis, including pain relief and reduction of endometriotic lesions. Experience with SYNAREL for the management of endometriosis has been limited to women 18 years of age and older treated for 6 months.
Regulatory record

1 cited source · 1 regulatory record

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “SYNAREL is indicated for management of endometriosis, including pain relief and reduction of endometriotic lesions. Experience with SYNAREL for the management of endometriosis has been limited to women 18 years of age and older treated for 6 months.”

    Synarel®(nafarelin acetate)nasal solution · INDICATIONS AND USAGE FOR ENDOMETRIOSIS

    dailymed:d0aa57cb-d2f4-46d7-af43-7c8b06aa81a6:e94a8d18814b:e94a8d18814b

Administration context

The practical clinical context.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Additional research & classification gaps

6 archived statements are kept separate from drug-effect findings. Media studies, economic models, methods, and records with unresolved scope are not used as medical-effect evidence.

Inspect contextual research (6)
Research context · scope unclassified

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Systemic absorption was observed for intranasal nafarelin, whereas sublingual and vaginal administration did not produce this absorption.

Research context only—not evidence of a treatment effect.

Research context · scope unclassified

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

This source explicitly states that danazol and nafarelin differ considerably in pharmacologic profile, indicating meaningful differences in their pharmacologic characteristics.

Research context only—not evidence of a treatment effect.

Research context · scope unclassified

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

2 cited passages across 1 source record. 1 publication group(s) lack a resolved study identity.

Increasing nafarelin concentration in the nasal dose solution increased nasal absorption.

Research context only—not evidence of a treatment effect.

Research context · scope unclassified

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

The review reports that nafarelin-associated decreases in uterine bleeding (including amenorrhea) were linked with increased mean hemoglobin, consistent with improved blood-loss anemia indices.

Research context only—not evidence of a treatment effect.

Research context · scope unclassified

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

In this study’s conclusion, post-surgical nafarelin was associated with a statistically significant delay in recurrence of symptoms that led to additional treatment, versus placebo.

Research context only—not evidence of a treatment effect.

Research context · scope unclassified

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Physician-assessed summary ratings indicated statistically significant improvement with nafarelin, while placebo showed no statistically significant change at 6 months.

Research context only—not evidence of a treatment effect.

Research status + gaps

What still needs better answers?

  • No publishable claim yet for: administration, interaction
  • 132 compiled claim(s) withheld by automated assurance: assurance_score_below_0.58 (58), assurance_score_below_0.72 (61), current_regulatory_source_required (40), extraction_ambiguity (72), high_risk_requires_regulatory_or_two_independent_sources (69), no_direct_support (112)

These are the limits of this profile, not an exhaustive list of scientific uncertainties.

References + discovery

Open the records yourself.

  1. ChEMBL activities for CHEMBL1201309 ↗

    chembl-activities · published 2026-08-28 · retrieved 2026-08-28T12:35:21Z

  2. NAFARELIN ↗

    chembl-molecule · published 2026-08-28 · retrieved 2026-08-28T12:35:21Z

  3. Synarel®(nafarelin acetate)nasal solution ↗

    dailymed · published 2026-03-05 · retrieved 2026-09-08T21:51:50Z

  4. Absorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone. ↗

    doi · published 1988-09-01 · retrieved 2026-09-08T21:51:51Z

  5. IUPHAR ligand commentary ↗

    iuphar-comments · published 2026-08-28 · retrieved 2026-08-28T12:35:21Z

  6. nafarelin ↗

    iuphar-ligand · published 2026-08-28 · retrieved 2026-08-28T12:35:21Z

  7. Clinical use of nafarelin in the treatment of leiomyomas. A review of the literature. ↗

    pubmed · published 2000-06-01 · retrieved 2026-09-09T22:27:22Z

  8. Comparison of the pharmacology of nafarelin and danazol. ↗

    pubmed · published 1990-02-01 · retrieved 2026-09-09T22:27:23Z

  9. Nafarelin. A review of its pharmacodynamic and pharmacokinetic properties, and clinical potential in sex hormone-related conditions. ↗

    pubmed · published 1990-04-01 · retrieved 2026-09-09T18:02:58Z

  10. Administration of nasal nafarelin as compared with oral danazol for endometriosis. A multicenter double-blind comparative clinical trial. ↗

    pubmed · published 1988-02-25 · retrieved 2026-09-08T21:51:55Z

  11. Absorption and metabolism of nafarelin, a potent agonist of gonadotropin-releasing hormone. ↗

    pubmed · published 1988-09-01 · retrieved 2026-09-08T21:51:48Z

  12. Use of nafarelin versus placebo after reductive laparoscopic surgery for endometriosis. ↗

    pubmed · published 1997-11-01 · retrieved 2026-09-08T21:51:53Z

Publication history and provenance

Version 2 · Automated assessment · 2026-09-09T22:27:23Z

4706f57a430b0aad1de5f8920222b1889ffea06af6f19b7fc73f32414a1fab86