Triptorelin

Summary

Triptorelin (CHEMBL1201334) is an approved protein gonadotropin releasing hormone agonist (ATC L02AE04) targeting GNRHR; indicated across 15 conditions including neoplasm and infertility disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• ATC class: L02AE04
• Targets: 1 (GNRHR)
• Indications: 15 conditions
• Clinical trials: 118
• Chemistry: 1311.4 Da · C64H82N18O13

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1201334
Name	Triptorelin
Type	Protein
Max phase	4
FDA approved	yes
PubChem CID	25074470
ChEBI	CHEBI:63633
ATC	L02AE04
Molecular formula	C64H82N18O13
Molecular weight	1311.4
InChIKey	VXKHXGOKWPXYNA-PGBVPBMZSA-N

SMILES: CC(C)C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N)NC(=O)[C@@H](CC2=CNC3=CC=CC=C32)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CNC6=CC=CC=C65)NC(=O)[C@H](CC7=CN=CN7)NC(=O)[C@@H]8CCC(=O)N8

IUPAC name: (2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[(2-amino-2-oxoethyl)carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide

ChEBI definition: An oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, D-tryptophyl, leucyl, arginyl, prolyl and glycinamide residues joined in sequence. It is an agonist analogue of gonadotropin-releasing hormone.

Pharmacological roles (ChEBI): gonadotropin releasing hormone agonist, antineoplastic agent, contraceptive drug.

Also known as: Arvekap, AY-25650, CL 118,532, CL-118532, Decapeptyl, Decapeptyl sr, Gonapeptyl depot, Triptodur, Triptorelin, Triptorelina, Triptoreline, Tryptorelin

Parent form; salt/anhydrous children: CHEMBL1200554

Patent coverage: 237 distinct patent families (449 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 298 (66%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
GNRHR	GnRH1 receptor	Full agonist	9.49	0.1%	P30968

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Prostaglandin G/H synthase 1.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): GNRHR.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
Hormone ligand-binding receptors	1	GNRHR
G alpha (q) signalling events	1	GNRHR

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	1
gonadotropin secretion	1
cellular response to hormone stimulus	1
signal transduction	1
cellular response to gonadotropin-releasing hormone	1

Indications & clinical

Indications

15 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
neoplasm	4	MONDO:0005070	EFO:0000616
infertility disorder	3	MONDO:0005047	EFO:0000545
endometriosis	3	MONDO:0005133	EFO:0001065
breast carcinoma	3	MONDO:0004989	EFO:0000305
prostate adenocarcinoma	3	MONDO:0005082	EFO:0000673
central precocious puberty	3	MONDO:0019165	EFO:0009029
precocious puberty	3	MONDO:0000088	MONDO:0000088
breast neoplasm	3	MONDO:0021100	MONDO:0007254
metastatic prostate carcinoma	3	MONDO:0004956	EFO:0000196
prostate carcinoma	3	MONDO:0005159	EFO:0001663
ovarian hyperstimulation syndrome	3	MONDO:0011972	MONDO:0011972
lymphoma	2	MONDO:0005062	EFO:0000574
HIV infectious disease	2	MONDO:0005109	EFO:0000180
salivary gland cancer	2	MONDO:0004669	MONDO:0004669

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 118.

Phase distribution

Phase	Trials
PHASE3	32
PHASE4	30
Not specified	26
PHASE2	21
PHASE2/PHASE3	4
PHASE1/PHASE2	2
PHASE1	2
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06487143	PHASE4	NOT_YET_RECRUITING	Efficacy, Metabolism and BMD of the 3-month TP Compared to the 1-month TP in ICPP
NCT06763926	PHASE4	NOT_YET_RECRUITING	Intranasal Nafarelin For Triggering Oocyte Maturation
NCT00415792	PHASE4	UNKNOWN	Comparison Between hCG and GnRH Agonist for Ovulation Induction in Patients With High Response to IVF Drugs
NCT00503217	PHASE4	COMPLETED	GnRH Agonist and Intrauterine Insemination
NCT00735852	PHASE4	COMPLETED	Decapeptyl SR With Livial Add Back Therapy in the Management of Chronic Cyclical Pelvic Pain in Pre Menopausal Women
NCT00840944	PHASE4	UNKNOWN	A 4 Year Combination Therapy of Growth Hormone and (GnRH) Agonist in Children With a Short Predicted Height
NCT01500863	PHASE4	COMPLETED	Endometrial Receptivity After GnRH Agonist Triggering
NCT01581359	PHASE4	COMPLETED	The Effect of Pre-treatment With GnRH Analogues Prior in Vitro Fertilization in Patients With Endometriosis
NCT01607203	PHASE4	COMPLETED	Trial Comparing hCG Triggering Versus hCG Associated With GnRH Agonist
NCT01638026	PHASE4	COMPLETED	Final Oocyte Maturation Via Administration of GnRH Agonists Followed By Luteal Support With hCG
NCT01714648	PHASE4	TERMINATED	Can GnRH Agonist Trigger Prevent Ovarian Hyperstimulation Syndrome?
NCT01753297	PHASE4	COMPLETED	A Study of Immediate 9 Months Adjuvant Hormone Therapy With Triptorelin 11.25 mg Versus Active Surveillance After Radical Prostatectomy in High Risk Prostate Cancer Patients.
NCT02070198	PHASE4	UNKNOWN	Long Acting FSH Plus Antagonist Versus Daily FSH Plus Antagonist Versus Short Agonist Protocol in Poor Responders Undergoing IVF
NCT02102646	PHASE4	COMPLETED	MRI Substudy; Metabolic Changes Due to Iatrogenic Hypogonadism
NCT02312076	PHASE4	UNKNOWN	GnRHa for Luteal Phase Support in Long GnRHa Protocol Cycles
NCT02312089	PHASE4	UNKNOWN	GnRHa for Luteal Phase Support in GnRH Antagonist Protocol Cycles
NCT02620124	PHASE4	COMPLETED	GnRH Agonist as Luteal Support in FET Cycles
NCT02655146	PHASE4	UNKNOWN	the Effects of GnRHa Add up to Routine Luteal Phase Support on Frozen Embryo Implantation in Frozen Embryo Transfer .
NCT02715232	PHASE4	UNKNOWN	Effects of Sex Steroids on the Serotonin System
NCT02825290	PHASE4	UNKNOWN	Modified Luteal Support for Frozen-Thawed Embryo Transfer - A Prospective Study
NCT03115307	PHASE4	COMPLETED	Luteal Phase Support in Insemination Cycles
NCT03118830	PHASE4	COMPLETED	Long Protocol and Freeze All Embryos vs Antagonist Protocol With Fresh Embryo Transfer in PCOS Patients Undergoing ICSI
NCT03169166	PHASE4	COMPLETED	The Use of GnRH Agonist Trigger for Final Follicle Maturation in Women Undergoing Assisted Reproductive Technologies
NCT03809221	PHASE4	UNKNOWN	The Effectiveness and Safety of the Prolonged Down-regulation Protocol for Controlled Ovarian Hyperstimulation
NCT04248621	PHASE4	UNKNOWN	Androgen Deprivation Therapy on Bone Mineral Density Change in Prostate Cancer Patients
NCT04724343	PHASE4	COMPLETED	Effect of GnRH Agonist vs GnRH Antagonist on IVF/ICSI Outcomes.
NCT04724486	PHASE4	COMPLETED	Effect of GnRH Agonist vs GnRH Antagonist on Oocyte Morphology During IVF/ICSI
NCT04727671	PHASE4	COMPLETED	Effect of GnRH Agonist vs GnRH Antagonist on IVF/ICSI Outcomes in Polycystic Ovary Syndrome Patients.
NCT04727684	PHASE4	COMPLETED	Effect of GnRH Agonist vs GnRH Antagonist on Oocyte Morphology in Polycystic Ovary Syndrome Patients During IVF/ICSI
NCT05321511	PHASE4	UNKNOWN	Comparison of Triggers in Double Ovarian Stimulation (DuoStim).
NCT02685397	PHASE2/PHASE3	ACTIVE_NOT_RECRUITING	Management of Castration-Resistant Prostate Cancer with Oligometastases
NCT03678025	PHASE3	RECRUITING	Standard Systemic Therapy With or Without Definitive Treatment in Treating Participants With Metastatic Prostate Cancer
NCT04064840	PHASE3	RECRUITING	GnRH Agonist for Dual Trigger in IVF and for Luteal Phase Support in FET
NCT04242017	PHASE2/PHASE3	RECRUITING	Long-term Better Than Short-term ADT With Salvage RT
NCT04423211	PHASE3	RECRUITING	Treating Prostate Cancer That Has Come Back After Surgery With Apalutamide and Targeted Radiation Based on PET Imaging
NCT04484818	PHASE3	ACTIVE_NOT_RECRUITING	Testing the Addition of Darolutamide to Hormonal Therapy (Androgen Deprivation Therapy [ADT]) After Surgery for Men With High-Risk Prostate Cancer, The ERADICATE Study
NCT04513717	PHASE3	ACTIVE_NOT_RECRUITING	Two Studies for Patients With High Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a High Gene Risk Score, The PREDICT-RT Trial
NCT05050084	PHASE3	ACTIVE_NOT_RECRUITING	Two Studies for Patients With Unfavorable Intermediate Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a Higher Gene Risk Score, The Guidance Trial
NCT05781217	PHASE3	RECRUITING	Short Versus Long-term Androgen Deprivation Therapy With Salvage Radiotherapy in Prostate Cancer. URONCOR 0624
NCT00003026	PHASE3	COMPLETED	Hormone Therapy in Treating Patients With Advanced Prostate Cancer

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

13 molecules share ≥1 primary target. Top 13 by shared-target count:

Molecule	Source	Status	Shared targets
CETRORELIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
DEGARELIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
ELAGOLIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
GANIRELIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
RELUGOLIX	ChEMBL + PubChem	Phase 4 (approved)	GNRHR
ABARELIX	ChEMBL	Phase 4 (approved)	GNRHR
GONADORELIN	ChEMBL	Phase 4 (approved)	GNRHR
LEUPROLIDE	ChEMBL	Phase 4 (approved)	GNRHR
LINZAGOLIX	ChEMBL	Phase 4 (approved)	GNRHR
ACYLINE	ChEMBL	Phase 2	GNRHR
SUFUGOLIX	ChEMBL	Phase 2	GNRHR
Belzutifan	PubChem	Approved	GNRHR
Deslorelin	PubChem	Approved	GNRHR