Accession Number
Small Molecule
Approved, Vet approved

Triptorelin is a synthetic decapeptide agonist analog of luteinizing hormone releasing hormone (LHRH). Possessing greater potency than endogenous LHRH, triptorelin reversibly represses gonadotropin secretion. After chronic, continuous administration, this agent effects sustained decreases in LH and FSH production and testicular and ovarian steroidogenesis. Serum testosterone concentrations may fall to levels typically observed in surgically castrated men.

  • (6-D-Tryptophan)luteinizing hormone-releasing hormone
  • (D-Trp6)-GnRH
  • Luteinizing hormone-releasing factor (pig), 6-D-tryptophan
  • pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2
  • Triptorelin
  • Triptorelina
  • Triptoreline
  • Triptorelinum
External IDs
AY-25650 / CL 118,532 / CL-118532 / WY-42462
Product Ingredients
IngredientUNIICASInChI Key
Triptorelin acetate43OFW291R9140194-24-7HPPONSCISKROOD-OYLNGHKZSA-N
Triptorelin pamoate08AN7WA2G0124508-66-3ZBVJFYPGLGEMIN-OYLNGHKZSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DecapeptylSolutionSubcutaneousFerring Pharmaceuticals2012-08-09Not applicableCanada
TrelstarInjection, powder, lyophilized, for suspension11.25 mg/2mLIntramuscularActavis Pharma Company2001-06-292018-10-31Us
TrelstarInjection, powder, for suspension, extended release11.25 mgIntramuscularAllergan Pharma Co.2005-12-15Not applicableCanada
TrelstarInjection, powder, for suspension, extended release3.75 mgIntramuscularAllergan Pharma Co.2005-12-15Not applicableCanada
TrelstarInjection, powder, lyophilized, for suspension3.75 mg/2mLIntramuscularActavis Pharma Company2000-06-152018-10-31Us
TrelstarInjection, powder, for suspension, extended release22.5 mgIntramuscularAllergan Pharma Co.2013-10-16Not applicableCanada
Trelstar22.5 mg/2mLIntramuscularAllergan, Inc.2010-03-11Not applicableUs
Trelstar11.25 mg/2mLIntramuscularAllergan, Inc.2001-06-29Not applicableUs
Trelstar3.75 mg/2mLIntramuscularAllergan, Inc.2000-06-15Not applicableUs
TrelstarKit22.5 mg/2mLIntramuscularActavis Pharma Company2010-03-112018-10-31Us
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
International/Other Brands
Diphereline (Ferring Pharmaceuticals) / Gonapeptyl (Ferring Pharmaceuticals) / Variopeptyl (Varian Darou Pajooh)
CAS number
Average: 1311.473
Monoisotopic: 1310.630874772
Chemical Formula
InChI Key



Triptorelin is indicated for the palliative treatment of advanced prostate cancer.

Associated Conditions
Associated Therapies

The first administration of triptorelin is followed by a transient surge of follicle stimulating hormone (FSH), luteinizing hormone (LH), estradiol,and testosterone. The time, peak and decline of testosterone in the body varies depending on the dose administered. This initial surge is often responsible for worsening of prostate cancer symptoms such as urethral or bladder outlet obstruction, bone pain, spinal cord injury and hematuria in the early stages. A sustained decrease in FSH and LH, and significant reduction of testicular steroidogenesis is usually seen 2-4 weeks post-initiation of therapy. This result is a reduction of serum testosterone to levels which are typically seen in surgically castrated men. Ultimately, tissues and functions that require these hormones become inactive. The effects of triptorelin can usually be reversed once the drug is discontinued.

Mechanism of action

Triptorelin is a synthetic agonist analog of gonadotropin releasing hormone (GnRH). Animal studies comparing triptorelin to native GnRH found that triptorelin had 13 fold higher releasing activity for luteinizing hormone, and 21-fold higher releasing activity for follicle-stimulating hormone.

AGonadotropin-releasing hormone receptor
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

Learn more
Additional Data Available

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

Learn more
Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

Learn more

Following IV administration of triptorelin, triptorelin is completely absorbed.

Volume of distribution

After a single IV dose of 0.5mg, the volume of distribution of triptorelin peptide in healthy males was 30 - 33L.

Protein binding

Triptorelin does not bind to plasma proteins at clinically relevant concentrations.


The metabolism of triptorelin in humans is not well understood; however, metabolism likely does not involve hepatic enzymes such as cytochrome P450. Whether or not triptorelin affects, or how it affects other metabolizing enzymes is also poorly understood. Triptorelin has no identified metabolites.

Route of elimination

Elimination of triptorelin involves both the kidneys and the liver.

Half life

The pharmacokinetics of triptorelin follows a 3 compartment model. The half lives are estimated to be 6 minutes, 45 minutes, and 3 hours respectively.


In healthy male volunteers, total clearance of triptorelin was 211.9 mL/min.


Some of the most commonly reported adverse effects of triptorelin are hot flushes reported in 58.6% of patients, skeletal pain in 12.1%, impotence in 7.1%, and headache in 5.0%. Other reported adverse effects include injection site pain, general body pain, leg pain, fatigue, hypertension, dizziness, diarrhea, vomiting, insomnia, emotional lability, anemia, pruritus, urinary tract infections, and urinary retention. Triptorelin is classified as Pregnancy Category X and contraindicated in pregnant women or in women who may become pregnant. Hormonal changes caused by triptorelin increase the risk for pregnancy loss. Studies done on pregnant rats demonstrated maternal toxicity and embryo-fetal toxicities.

Affected organisms
Not Available
Not Available
Pharmacogenomic Effects/ADRs
Not Available


Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Triptorelin.
AbexinostatThe risk or severity of QTc prolongation can be increased when Triptorelin is combined with Abexinostat.
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Triptorelin.
AcebutololThe risk or severity of QTc prolongation can be increased when Triptorelin is combined with Acebutolol.
AceprometazineThe risk or severity of QTc prolongation can be increased when Triptorelin is combined with Aceprometazine.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Triptorelin.
AcetyldigoxinThe risk or severity of QTc prolongation can be increased when Triptorelin is combined with Acetyldigoxin.
AcrivastineThe risk or severity of QTc prolongation can be increased when Triptorelin is combined with Acrivastine.
AdenosineThe risk or severity of QTc prolongation can be increased when Triptorelin is combined with Adenosine.
AICA ribonucleotideThe therapeutic efficacy of AICA ribonucleotide can be decreased when used in combination with Triptorelin.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity

    A severity rating for each drug interaction, from minor to major.

    Learn more
  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

    Learn more
  • Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

    Learn more
Food Interactions
Not Available


General References
  1. Lahlou N, Carel JC, Chaussain JL, Roger M: Pharmacokinetics and pharmacodynamics of GnRH agonists: clinical implications in pediatrics. J Pediatr Endocrinol Metab. 2000 Jul;13 Suppl 1:723-37. [PubMed:10969915]
  2. Padula AM: GnRH analogues--agonists and antagonists. Anim Reprod Sci. 2005 Aug;88(1-2):115-26. [PubMed:15955640]
External Links
PubChem Compound
PubChem Substance
RxList Drug Page Drug Page
ATC Codes
L02AE04 — Triptorelin
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
FDA label
Download (691 KB)

Clinical Trials

Clinical Trials
1CompletedOtherHealthy Volunteers1
1RecruitingBasic ScienceFemale Infertility1
1, 2RecruitingTreatmentAdenocarcinoma, Prostate / Stage I Prostate Cancer / Stage IIA Prostate Cancer / Stage IIB Prostate Cancer / Stage III Prostate Cancer1
2Active Not RecruitingSupportive CareAdenocarcinoma of the Prostate / Recurrent Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1
2Active Not RecruitingTreatmentProstate Cancer1
2CompletedDiagnosticSystemic Lupus Erythematosus (SLE)1
2CompletedTreatmentFemale Urogenital Diseases1
2CompletedTreatmentInfertility / Poor Ovarian Response2
2CompletedTreatmentInvasive Breast Cancer1
2CompletedTreatmentProstate Cancer2
2RecruitingOtherBreast Cancer1
2RecruitingPreventionBreast Cancer1
2RecruitingTreatmentHuman Immunodeficiency Virus Type 1 (HIV-1) Infection1
2RecruitingTreatmentProstate Cancer2
2RecruitingTreatmentSalivary Gland Cancers1
2TerminatedSupportive CareAdenocarcinoma, Prostate / Malignancies / Prostate Cancer1
2TerminatedSupportive CareBreast Cancer / Hormone Changes / Therapeutic Agent Toxicity1
2TerminatedTreatmentEarly Breast Cancer / Estrogen Receptor-Positive Breast Cancer / HER2-Negative Breast Cancer / Progesterone Receptor-positive Breast Cancer / Stage II Breast Cancer / Stage IIIA Breast Cancer1
2TerminatedTreatmentProstate Cancer2
2, 3Active Not RecruitingTreatmentEwing's Sarcoma (ES) / Malignancies / Malignant Lymphomas / Sarcoma, Osteogenic / Sarcomas / Toxicity Due to Chemotherapy1
2, 3CompletedPreventionAlkylating Agents / Fertility Preservation / Malignant Lymphomas1
2, 3Not Yet RecruitingTreatmentProstate Cancer1
2, 3RecruitingTreatmentCastration-resistant Prostate Cancer Patients With Oligometastases1
2, 3RecruitingTreatmentFemale Infertility1
3Active Not RecruitingTreatmentBreast Cancer2
3Active Not RecruitingTreatmentBreast Cancer / Estrogen Receptor Positive Breast Cancer / Progesterone Receptor Positive Tumor / Recurrent Breast Carcinoma / Stage IA Breast Cancer / Stage IB Breast Cancer / Stage IIA Breast Cancer / Stage IIB Breast Cancer / Stage IIIA Breast Cancer1
3Active Not RecruitingTreatmentGeneral Surgery / Stage, Prostate Cancer1
3Active Not RecruitingTreatmentProstate Cancer4
3CompletedNot AvailableBreast Cancer / Fatigue / Sleep disorders and disturbances1
3CompletedDiagnosticProstate Cancer1
3CompletedSupportive CareBreast Cancer1
3CompletedTreatmentCentral Precocious Puberty (CPP)1
3CompletedTreatmentControlled Ovarian Stimulation1
3CompletedTreatmentInfertility / Polycystic Ovaries Syndrome1
3CompletedTreatmentProstate Cancer3
3CompletedTreatmentProstatic Neoplasms1
3CompletedTreatmentPuberty, Precocious2
3Not Yet RecruitingTreatmentIn-Vitro Fertilization1
3Not Yet RecruitingTreatmentOvarian Hyperstimulation Syndrome1
3RecruitingTreatmentCastration Levels of Testosterone / Metastatic Prostatic Adenocarcinoma / Stage IV Prostate Cancer AJCC v8 / Stage IVA Prostate Cancer AJCC v8 / Stage IVB Prostate Cancer AJCC v81
3RecruitingTreatmentPoor Ovarian Reserve1
3RecruitingTreatmentProstate Cancer2
3SuspendedTreatmentFemale Infertility1
3TerminatedNot AvailableInfertility1
3TerminatedTreatmentBreast Cancer1
3TerminatedTreatmentProstate Cancer1
3Unknown StatusPreventionEndometriosis1
3Unknown StatusTreatmentProstate Cancer2
4Active Not RecruitingTreatmentIdiopathic Short Stature (ISS)1
4CompletedNot AvailableProstate Cancer1
4CompletedTreatmentAssisted Reproduction1
4CompletedTreatmentEndometriosis / Infertility1
4CompletedTreatmentFatty Liver / Hypogonadism / Metabolic Syndromes / Prostate Cancer1
4CompletedTreatmentFemale Infertility1
4CompletedTreatmentInfertility Indicated for ICSI1
4CompletedTreatmentInfertility / Premature Ovarian Failure (POF)1
4CompletedTreatmentInvitro Fertilization1
4CompletedTreatmentOvarian Hyperstimulation Syndrome1
4CompletedTreatmentProstate Cancer1
4Not Yet RecruitingTreatmentFemale Infertility1
4RecruitingBasic ScienceGender Dysphoria1
4RecruitingSupportive CareInfertility2
4RecruitingSupportive CareProstatic Neoplasms1
4RecruitingTreatmentEmbryo Transfer / Luteal Support1
4TerminatedPreventionOvarian Hyperstimulation Syndrome1
4TerminatedTreatmentAssisted Reproductive Technology therapy1
4TerminatedTreatmentProstate Cancer2
4Unknown StatusDiagnosticCentral Precocious Puberty (CPP) / Sexual Precocity1
4Unknown StatusPreventionCentral Precocious Puberty (CPP)1
4Unknown StatusPreventionOvarian Hyperstimulation Syndrome / Polycystic Ovaries Syndrome1
4Unknown StatusTreatmentClomiphene Citrate / GnRH Antagonist / Gonadotropin-releasing Hormone Agonist / IVF / Poor Responders1
4Unknown StatusTreatmentFemale Infertility / Poor Responder1
4Unknown StatusTreatmentInfertility2
Not AvailableActive Not RecruitingTreatmentEndometriosis / Infertility1
Not AvailableCompletedNot AvailableDeep Infiltrating Endometriosis (DIE)1
Not AvailableCompletedNot AvailableIVF / Luteal Phase Defect1
Not AvailableCompletedNot AvailableImplantation, Embryo / Pregnancy1
Not AvailableCompletedNot AvailableNeonates / Pregnancy1
Not AvailableCompletedNot AvailableProstate Cancer1
Not AvailableCompletedSupportive CareHodgkins Disease (HD) / Lymphoma, Hodgkins1
Not AvailableCompletedTreatmentEndometriotic Cysts1
Not AvailableCompletedTreatmentInfertility3
Not AvailableCompletedTreatmentNormal Oocyte Donors1
Not AvailableCompletedTreatmentUterine Leiomyomas1
Not AvailableEnrolling by InvitationScreeningFemale Infertility / Single Nucleotide Polymorphism,GnRH Receptor, IVF1
Not AvailableNot Yet RecruitingNot AvailableInfertility1
Not AvailableNot Yet RecruitingNot AvailableProstate Cancer1
Not AvailableNot Yet RecruitingDiagnosticInvitro Fertilization1
Not AvailableNot Yet RecruitingTreatmentInfertility2
Not AvailableNot Yet RecruitingTreatmentOvulatory Dysfunction / Subfertility, Female1
Not AvailableRecruitingNot AvailableInfertility1
Not AvailableRecruitingNot AvailableProstate Cancer1
Not AvailableRecruitingDiagnosticIVF Treatment1
Not AvailableRecruitingHealth Services ResearchCongenital Uterine Anomalies / Endometriosis / Extrauterine Pregnancy / Female Infertility / Female Infertility - Cervical/Vaginal / Female Infertility Due to Ovulatory Disorder / Female Infertility Due to Tubal Block / Female Infertility Due to Tubal Occlusion / Female Infertility Endocrine / Female Infertility of Other Origin / Female Infertility of Tubal Origin / Hydrosalpinx / Infections Uterine / Leiomyomas / Polycystic Ovaries Syndrome / Premature Ovarian Failure (POF) / Salpingitis1
Not AvailableRecruitingOtherEmbryonic Quality Using MitoScore (DuoStim x Conventional Stimulation Protocol) / Female Infertility / Potential Usefulness of the DuoStim Protocol / Rate of Euploid Embryos Per Cycle (DuoStim x Conventional Stimulation Protocol)1
Not AvailableRecruitingTreatmentAssisted Reproductive Technology therapy / Polycystic Ovaries Syndrome1
Not AvailableRecruitingTreatmentEndometriosis1
Not AvailableRecruitingTreatmentInfertility1
Not AvailableRecruitingTreatmentProstate Cancer1
Not AvailableUnknown StatusPreventionInfertility and at High Risk of OHSS1
Not AvailableUnknown StatusTreatmentInfertility and at High Risk of OHSS1
Not AvailableUnknown StatusTreatmentPregnancy Rate1
Not AvailableUnknown StatusTreatmentWomen With Poor Ovarian Response1


Not Available
Not Available
Dosage forms
Injection, powder, for suspension, extended releaseIntramuscular11.25 mg
Injection, powder, for suspension, extended releaseIntramuscular22.5 mg
Injection, powder, for suspension, extended releaseIntramuscular3.75 mg
Injection, powder, lyophilized, for suspensionIntramuscular11.25 mg/2mL
Injection, powder, lyophilized, for suspensionIntramuscular22.5 mg/2mL
Injection, powder, lyophilized, for suspensionIntramuscular3.75 mg/2mL
KitIntramuscular11.25 mg/2mL
KitIntramuscular22.5 mg/2mL
KitIntramuscular3.75 mg/2mL
Not Available
Patent NumberPediatric ExtensionApprovedExpires (estimated)
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more


Experimental Properties
Not Available
Predicted Properties
Water Solubility0.0305 mg/mLALOGPS
pKa (Strongest Acidic)9.49ChemAxon
pKa (Strongest Basic)11.54ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count17ChemAxon
Hydrogen Donor Count18ChemAxon
Polar Surface Area487.92 Å2ChemAxon
Rotatable Bond Count33ChemAxon
Refractivity352.43 m3·mol-1ChemAxon
Polarizability135.23 Å3ChemAxon
Number of Rings8ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available


Mass Spec (NIST)
Not Available
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available


This compound belongs to the class of organic compounds known as polypeptides. These are peptides containing ten or more amino acid residues.
Organic compounds
Super Class
Organic Polymers
Sub Class
Not Available
Direct Parent
Alternative Parents
Peptides / Tyrosine and derivatives / Phenylalanine and derivatives / Histidine and derivatives / Leucine and derivatives / N-acyl-alpha amino acids and derivatives / Proline and derivatives / Tryptamines and derivatives / Serine and derivatives / Alpha amino acid amides
show 23 more
Polypeptide / Alpha peptide / Tyrosine or derivatives / Phenylalanine or derivatives / Histidine or derivatives / Leucine or derivatives / N-acyl-alpha amino acid or derivatives / Proline or derivatives / Triptan / Alpha-amino acid amide
show 48 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
oligopeptide (CHEBI:63633)


Pharmacological action
General Function
Peptide binding
Specific Function
Receptor for gonadotropin releasing hormone (GnRH) that mediates the action of GnRH to stimulate the secretion of the gonadotropic hormones luteinizing hormone (LH) and follicle-stimulating hormone...
Gene Name
Uniprot ID
Uniprot Name
Gonadotropin-releasing hormone receptor
Molecular Weight
37730.355 Da

Drug created on September 14, 2010 10:21 / Updated on March 30, 2020 22:56

Logo pink
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
Logo pink
Stay in the know!
As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages.