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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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.
- 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
- 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