Triptorelin
approvedAlso known as: Trelstar, Decapeptyl
**Mechanism of Action** Triptorelin is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH) with enhanced receptor affinity and prolonged half-life. Upon initial administration, it stimulates pituitary GnRH receptors, causing a transient surge in luteinizing hormone (LH) and follicle-stimulating hormone (FSH) — the "flare effect." Chronic exposure leads to receptor desensitization and downregulation, resulting in profound suppression of pituitary gonadotropin secretion. This reduces testicular testosterone production to castrate levels in males and ovarian estradiol production in females, achieving a reversible chemical castration state. **Key Research Findings** Clinical trials have established triptorelin’s efficacy in advanced prostate cancer, where monthly or 3-month depot formulations achieve sustained testosterone suppression (<50 ng/dL) comparable to surgical castration. In endometriosis, 3–6 months of treatment reduces lesion size and pain scores, with efficacy similar to leuprolide. Studies also support its use in central precocious puberty, where it halts progression of secondary sexual characteristics and bone age advancement. Pharmacokinetic data show dose-dependent suppression lasting 28–90 days depending on formulation, with recovery of gonadal function typically occurring within 3–6 months after discontinuation. **Clinical Relevance** Triptorelin is FDA-approved for palliative treatment of advanced prostate cancer, management of endometriosis (including pain relief and lesion reduction), and central precocious puberty. Its long-acting depot formulations improve patient compliance compared to daily GnRH agonist injections. Adverse effects are primarily related to hypoestrogenism/hypoandrogenism (hot flashes, bone density loss, mood changes) and the initial flare (transient tumor exacerbation in prostate cancer, mitigated by concurrent antiandrogen therapy). It is contraindicated in pregnancy and hypersensitivity to GnRH analogs. For research purposes only — not medical advice.
Key data
C64H82N18O13Research & studies
Triptorelin elicited significantly higher FSH peaks than gonadorelin, while LH peaks were comparable.; Optimal diagnostic LH peak cut-off for triptorelin was 7.14 IU/L (sensitivity 94%, specificity 96%; AUC 0.985).; Peak LH occurred predominantly at 180 minutes after triptorelin in both CPP and NPT groups.; Triptorelin demonstrated diagnostic accuracy comparable to gonadorelin, supporting its use as an alternative.
102 statistically significant preferred terms were identified for triptorelin-associated adverse events.; Unexpected safety signals included defiant behavior and Alzheimer's dementia, meeting EMA 2024 criteria for further investigation.; Median time-to-onset of adverse events was 132 days, with peaks in the first month (22.59%) and after one year (25.07%).; Distinct statistical signal profiles were observed between genders.
At month 6, 100% of patients had LH suppression (stimulated peak LH ≤5 IU/L), maintained in 98.5% at month 12.; Sex hormone levels were suppressed to prepubertal levels in all patients from months 3 to 12.; Mean growth velocity decreased from 9.82 cm/year at baseline to 5.88 cm/year at month 6 and 5.17 cm/year at month 12.; Drug-related TEAEs occurred in 19.7% of patients, with no grade 3 events reported.
Triptorelin-loaded nanoparticles were prepared in silk fibroin solution to control release and prevent enzymatic degradation.; Nanoparticle-encapsulated microneedles showed good mechanical properties due to increased β-sheet content.; Transdermal release of triptorelin reached 65% with prolonged half-life and increased bioavailability in rats.; Plasma luteinizing hormone and estradiol levels surged and then were prolonged downregulated, suggesting therapeutic efficacy.
Triptorelin therapy led to a clinically significant reduction in IPSS scores over 48 weeks in men with moderate to severe LUTS.; The meta-analysis showed a statistically significant pooled effect size of 1.05 (95% CI: 0.65-1.45) for LUTS improvement.; Quality of life improved in patients receiving triptorelin, though heterogeneity and bias were noted.; Further well-designed studies are needed to confirm findings and determine optimal use.
Triptorelin causes a transient gonadotropin surge followed by receptor desensitization and HPG axis downregulation.; In healthy women, triptorelin's HPG modulation supports assisted reproduction techniques.; For PCOS, triptorelin shows promise in restoring ovulatory function and reducing hyperandrogenism.; In hypothalamic amenorrhea, triptorelin may help restore proper GnRH pulsatility as a therapeutic avenue.
Over 98% of patients in both groups achieved chemical castration (estradiol ≤184 pmol/L) at week 12.; Both formulations were equally efficacious in reducing endometriosis-associated pelvic pain.; Triptorelin pamoate PR 3-month requires fewer injections, potentially lowering the burden of care.; No new safety concerns were identified with either formulation.
Frequently asked questions
What is Triptorelin?
**Mechanism of Action** Triptorelin is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH) with enhanced receptor affinity and prolonged half-life. Upon initial administration, it stimulates pituitary GnRH receptors, causing a transient surge in luteinizing hormone (LH) and follicle-stimulating horm
How does Triptorelin work?
Long-acting GnRH agonist that after initial flare downregulates pituitary receptors, suppressing sex hormones for prostate cancer and endometriosis.
What is the research status of Triptorelin?
Triptorelin is currently classified as approved, with 998 research references on record. This is for research purposes only and is not medical advice.
What is the molecular weight of Triptorelin?
Triptorelin has a molecular weight of approximately 1311.4 g/mol (formula C64H82N18O13).
Related peptides
Nonapeptide posterior pituitary hormone driving uterine contraction and milk letdown; studied intranasally for social cognition.
Selective V2-receptor vasopressin analog that concentrates urine; used for diabetes insipidus, nocturnal enuresis, and bleeding disorders.
GnRH agonist that suppresses gonadotropin and sex-steroid production after initial stimulation; used in prostate cancer, endometriosis, and precocious puberty.
Synthetic GnRH decapeptide that stimulates pituitary LH and FSH release; used diagnostically and to support gonadal function.
Build on Triptorelin data programmatically
Structured peptide data, semantic search, and AI summaries via one API.
Get a free API key