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Context, anatomy, and key evidence

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GnRH agonist

Triptorelin

Published evidence · coverage incomplete
Anatomical contextAnatomy connections are not mapped yet.

No body region is highlighted until this profile has a supported anatomical connection. This does not mean the peptide has no biological effects.

Read published mechanism findings ↓

At a glance

What is it—and why does it matter?

Triptorelin binds and activates GnRH receptors (i.e., it is a gonadotropin-releasing hormone agonist). As a GnRH agonist, triptorelin can produce an initial transient testosterone surge before suppression occurs. Contraindication for triptorelin pamoate (TRELSTAR) includes hypersensitivity to triptorelin, product components, or other GnRH agonists/GnRH. Post-reconstitution handling for triptorelin pamoate (TRELSTAR) specifies administration within 2 minutes.

Sources for this introduction: [1] [2] [3] [4]

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.

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

How does it work?

Target, response, and disposition.

Mechanism

Triptorelin binds and activates GnRH receptors (i.e., it is a gonadotropin-releasing hormone agonist).

Source records
1
Regulatory records
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    Triptorelin is a GnRH agonist.

    These highlights do not include all the information needed to use TRIPTODUR®safely and effectively. See full prescribing information for TRIPTODUR.TRIPTODUR (triptorelin) for extended-release injectable suspension, for intramuscular useInitial U.S. Approval: 2000 · 12.1 Mechanism of Action

    dailymed:f41380e7-b830-432d-a5f5-a872932f107e:f8ce63dc8a39:f8ce63dc8a39

Pharmacokinetics

Following single-dose IM administration of TRELSTAR in prostate cancer patients, triptorelin shows dose-related mean Cmax values with Tmax of 1 to 3 hours.

Reported result
Cmax 28.4 ng/mL, 38.5 ng/mL, 44.1 ng/mL (Tmax 1 to 3 hours)
Source records
1
Regulatory records
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    Following a single intramuscular injection of TRELSTAR to patients with prostate cancer, mean peak serum concentrations of 28.4 ng/mL, 38.5 ng/mL, and 44.1 ng/mL occurred in 1 to 3 hours after the 3.75 mg, 11.25 mg, and 22.5 mg formulations, respectively.

    These highlights do not include all the information needed to use TRELSTAR safely and effectively. See full prescribing information for TRELSTAR.TRELSTAR®(triptorelin pamoate for injectable suspension), for intramuscular useInitial U.S. Approval: 2000 · 12.3 Pharmacokinetics

    dailymed:b1b84d62-a369-a4b7-5c41-dd1f553a18f3:026d61f74712:026d61f74712

Pharmacokinetics

With repeat dosing (second 22.5 mg IM injection), triptorelin showed no apparent accumulation in the described pediatric CPP regimen.

Source records
1
Regulatory records
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    No apparent accumulation of triptorelin occurred after the second injection.

    These highlights do not include all the information needed to use TRIPTODUR®safely and effectively. See full prescribing information for TRIPTODUR.TRIPTODUR (triptorelin) for extended-release injectable suspension, for intramuscular useInitial U.S. Approval: 2000 · 12.3 Pharmacokinetics

    dailymed:f41380e7-b830-432d-a5f5-a872932f107e:f8ce63dc8a39:f8ce63dc8a39

What has been studied?

What the evidence says.

Study findings

As a GnRH agonist, triptorelin can produce an initial transient testosterone surge before suppression occurs.

Source records
1
Regulatory records
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    Initially, triptorelin (TRELSTAR), like other GnRH agonists, causes a transient increase in serum testosterone levels [seeClinical Pharmacology (12.2)].

    These highlights do not include all the information needed to use TRELSTAR safely and effectively. See full prescribing information for TRELSTAR.TRELSTAR®(triptorelin pamoate for injectable suspension), for intramuscular useInitial U.S. Approval: 2000 · 5.2 Tumor Flare

    dailymed:b1b84d62-a369-a4b7-5c41-dd1f553a18f3:026d61f74712:026d61f74712

Risks and interactions

Risks, organized for scanning.

Contraindications

Because of expected hormonal changes with triptorelin therapy, TRIPTODUR is associated with potential fetal harm.

Source records
1
Regulatory records
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    Pregnancy: TRIPTODUR may cause fetal harm[seeUse in Specific Populations (8.1)].

    These highlights do not include all the information needed to use TRIPTODUR®safely and effectively. See full prescribing information for TRIPTODUR.TRIPTODUR (triptorelin) for extended-release injectable suspension, for intramuscular useInitial U.S. Approval: 2000 · 4 CONTRAINDICATIONS

    dailymed:f41380e7-b830-432d-a5f5-a872932f107e:f8ce63dc8a39:f8ce63dc8a39

Contraindications

Contraindication for triptorelin pamoate (TRELSTAR) includes hypersensitivity to triptorelin, product components, or other GnRH agonists/GnRH.

Source records
1
Regulatory records
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    TRELSTAR is contraindicated in individuals with a known hypersensitivity to triptorelin or any other component of the product, or other GnRH agonists or GnRH [seeWarnings and Precautions (5.1)].

    These highlights do not include all the information needed to use TRELSTAR safely and effectively. See full prescribing information for TRELSTAR.TRELSTAR®(triptorelin pamoate for injectable suspension), for intramuscular useInitial U.S. Approval: 2000 · 4.1 Hypersensitivity

    dailymed:b1b84d62-a369-a4b7-5c41-dd1f553a18f3:026d61f74712:026d61f74712

Interactions

The labeling states that dedicated drug–drug interaction studies have not been performed for triptorelin pamoate (TRELSTAR).

Source records
1
Regulatory records
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    No drug-drug interaction studies involving TRELSTAR have been conducted.

    These highlights do not include all the information needed to use TRELSTAR safely and effectively. See full prescribing information for TRELSTAR.TRELSTAR®(triptorelin pamoate for injectable suspension), for intramuscular useInitial U.S. Approval: 2000 · 7DRUG INTERACTIONS

    dailymed:b1b84d62-a369-a4b7-5c41-dd1f553a18f3:026d61f74712:026d61f74712

Safety findings

GnRH agonist therapy with triptorelin (TRELSTAR) is associated with potential metabolic changes including hyperglycemia, diabetes mellitus, and hyperlipidemia.

Source records
1
Regulatory records
1

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 use of GnRH agonists (including TRELSTAR) may lead to metabolic changes such as hyperglycemia, diabetes mellitus, and hyperlipidemia.

    These highlights do not include all the information needed to use TRELSTAR safely and effectively. See full prescribing information for TRELSTAR.TRELSTAR®(triptorelin pamoate for injectable suspension), for intramuscular useInitial U.S. Approval: 2000 · 5.3 Metabolic Syndrome

    dailymed:b1b84d62-a369-a4b7-5c41-dd1f553a18f3:026d61f74712:026d61f74712

Safety findings

Triptorelin can produce a transient stimulatory effect causing temporary increases in gonadotropins and sex steroids early in therapy or after subsequent doses.

Source records
1
Regulatory records
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    During the early phase of initial therapy or after subsequent doses, gonadotropins and sex steroids may rise above baseline because of a transient stimulatory effect of the drug[seeClinical Pharmacology (12.2)].

    These highlights do not include all the information needed to use TRIPTODUR®safely and effectively. See full prescribing information for TRIPTODUR.TRIPTODUR (triptorelin) for extended-release injectable suspension, for intramuscular useInitial U.S. Approval: 2000 · 5.1 Initial Rise of Gonadotropins and Sex Steroid Levels

    dailymed:f41380e7-b830-432d-a5f5-a872932f107e:f8ce63dc8a39:f8ce63dc8a39

Safety findings

QT/QTc prolongation is a potential cardiac electrophysiology risk during androgen deprivation therapy with triptorelin (TRELSTAR).

Source records
1
Regulatory records
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    Androgen deprivation therapy with TRELSTAR may prolong the QT/QTc interval.

    These highlights do not include all the information needed to use TRELSTAR safely and effectively. See full prescribing information for TRELSTAR.TRELSTAR®(triptorelin pamoate for injectable suspension), for intramuscular useInitial U.S. Approval: 2000 · 5.7 Effect on QT/QTc Interval

    dailymed:b1b84d62-a369-a4b7-5c41-dd1f553a18f3:026d61f74712:026d61f74712

Safety findings

Because of early hormonal stimulation, patients may show transient clinical pubertal signs (including vaginal bleeding) in the first weeks after starting therapy or after subsequent dosing.

Source records
1
Regulatory records
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    Therefore, a transient increase in clinical signs and symptoms of puberty, including vaginal bleeding, may be observed during the first weeks of therapy or after subsequent doses.

    These highlights do not include all the information needed to use TRIPTODUR®safely and effectively. See full prescribing information for TRIPTODUR.TRIPTODUR (triptorelin) for extended-release injectable suspension, for intramuscular useInitial U.S. Approval: 2000 · 5.1 Initial Rise of Gonadotropins and Sex Steroid Levels

    dailymed:f41380e7-b830-432d-a5f5-a872932f107e:f8ce63dc8a39:f8ce63dc8a39

Products and regulatory status

Same ingredient. Different records.

Regulatory status

The approved indication for triptorelin (TRIPTODUR) is central precocious puberty in pediatric patients starting at age 2 years.

Source records
1
Regulatory records
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    TRIPTODUR is indicated for the treatment of pediatric patients 2 years of age and older with central precocious puberty (CPP).

    These highlights do not include all the information needed to use TRIPTODUR®safely and effectively. See full prescribing information for TRIPTODUR.TRIPTODUR (triptorelin) for extended-release injectable suspension, for intramuscular useInitial U.S. Approval: 2000 · 1 INDICATIONS AND USAGE

    dailymed:f41380e7-b830-432d-a5f5-a872932f107e:f8ce63dc8a39:f8ce63dc8a39

Regulatory status

The labeled indication for triptorelin pamoate (TRELSTAR) is treatment of advanced prostate cancer.

Source records
1
Regulatory records
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    TRELSTAR is indicated for the treatment of advanced prostate cancer [seeClinical Studies (14)].

    These highlights do not include all the information needed to use TRELSTAR safely and effectively. See full prescribing information for TRELSTAR.TRELSTAR®(triptorelin pamoate for injectable suspension), for intramuscular useInitial U.S. Approval: 2000 · 1INDICATIONS AND USAGE

    dailymed:b1b84d62-a369-a4b7-5c41-dd1f553a18f3:026d61f74712:026d61f74712

Administration context

The practical clinical context.

Administration

Administration of triptorelin (TRIPTODUR) is restricted to healthcare-provider administration.

Source records
1
Regulatory records
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    TRIPTODUR must only be administered by a healthcare provider.

    These highlights do not include all the information needed to use TRIPTODUR®safely and effectively. See full prescribing information for TRIPTODUR.TRIPTODUR (triptorelin) for extended-release injectable suspension, for intramuscular useInitial U.S. Approval: 2000 · 2.1 Dosing Information

    dailymed:f41380e7-b830-432d-a5f5-a872932f107e:f8ce63dc8a39:f8ce63dc8a39

Administration

Administration route and site for triptorelin pamoate (TRELSTAR) are intramuscular injection into either buttock.

Source records
1
Regulatory records
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    TRELSTAR is administered by a single intramuscular injection in either buttock.

    These highlights do not include all the information needed to use TRELSTAR safely and effectively. See full prescribing information for TRELSTAR.TRELSTAR®(triptorelin pamoate for injectable suspension), for intramuscular useInitial U.S. Approval: 2000 · 2.1 Dosing Information

    dailymed:b1b84d62-a369-a4b7-5c41-dd1f553a18f3:026d61f74712:026d61f74712

Administration

Post-reconstitution handling for triptorelin pamoate (TRELSTAR) specifies administration within 2 minutes.

Source records
1
Regulatory records
1

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 suspension should be administered within 2 minutes after reconstitution.

    These highlights do not include all the information needed to use TRELSTAR safely and effectively. See full prescribing information for TRELSTAR.TRELSTAR®(triptorelin pamoate for injectable suspension), for intramuscular useInitial U.S. Approval: 2000 · 2.1 Dosing Information

    dailymed:b1b84d62-a369-a4b7-5c41-dd1f553a18f3:026d61f74712:026d61f74712

Dose records

TRELSTAR has three strength-specific dosing schedules: 3.75 mg (q4 weeks), 11.25 mg (q12 weeks), and 22.5 mg (q24 weeks).

Source records
1
Regulatory records
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    Table 1. TRELSTAR Recommended DosingDosage3.75 mg11.25 mg22.5 mgRecommended dose1 injection every4 weeks1 injection every12 weeks1 injection every24 weeks

    These highlights do not include all the information needed to use TRELSTAR safely and effectively. See full prescribing information for TRELSTAR.TRELSTAR®(triptorelin pamoate for injectable suspension), for intramuscular useInitial U.S. Approval: 2000 · 2.1 Dosing Information

    dailymed:b1b84d62-a369-a4b7-5c41-dd1f553a18f3:026d61f74712:026d61f74712

Dose records

Because the formulations have different release characteristics, triptorelin pamoate (TRELSTAR) strengths are not interchangeable by addition; selection is schedule-driven.

Source records
1
Regulatory records
1

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

Exact passages, locators, and provenance
  1. supports · Source-backed record
    Due to different release characteristics, the dosage strengths are not additive and must be selected based upon the desired dosing schedule.

    These highlights do not include all the information needed to use TRELSTAR safely and effectively. See full prescribing information for TRELSTAR.TRELSTAR®(triptorelin pamoate for injectable suspension), for intramuscular useInitial U.S. Approval: 2000 · 2.1 Dosing Information

    dailymed:b1b84d62-a369-a4b7-5c41-dd1f553a18f3:026d61f74712:026d61f74712

Dose records

TRIPTODUR dosing is a fixed 22.5 mg dose, reconstituted with 2 mL sterile water diluent, administered intramuscularly at 24-week intervals.

Source records
1
Regulatory records
1

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 dosage of TRIPTODUR is 22.5 mg reconstituted with accompanying diluent (Sterile Water) 2 mL, and administered as a single intramuscular injection once every 24 weeks.

    These highlights do not include all the information needed to use TRIPTODUR®safely and effectively. See full prescribing information for TRIPTODUR.TRIPTODUR (triptorelin) for extended-release injectable suspension, for intramuscular useInitial U.S. Approval: 2000 · 2.1 Dosing Information

    dailymed:f41380e7-b830-432d-a5f5-a872932f107e:f8ce63dc8a39:f8ce63dc8a39

Research status + gaps

What still needs better answers?

  • No publishable claim yet for: identity
  • 26 compiled claim(s) withheld by automated assurance: assurance_score_below_0.58 (18), assurance_score_below_0.72 (7), current_regulatory_source_required (4), extraction_ambiguity (25), high_risk_requires_regulatory_or_two_independent_sources (8), no_direct_support (25)

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

References + discovery

Open the records yourself.

  1. These highlights do not include all the information needed to use TRELSTAR safely and effectively. See full prescribing information for TRELSTAR.TRELSTAR®(triptorelin pamoate for injectable suspension), for intramuscular useInitial U.S. Approval: 2000

    dailymed · published 2026-06-30 · retrieved 2026-09-04T22:25:19Z

  2. These highlights do not include all the information needed to use TRIPTODUR®safely and effectively. See full prescribing information for TRIPTODUR.TRIPTODUR (triptorelin) for extended-release injectable suspension, for intramuscular useInitial U.S. Approval: 2000

    dailymed · published 2025-09-14 · retrieved 2026-09-04T22:25:19Z

Publication history and provenance

Version 3 · Automated assessment · 2026-09-04T22:25:19Z

fff6fb7ce83c21a6dcb34a747e804bc76170e7ce80ad219aef2514fdb2c0f47e