|Groups||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.
|External IDs||AY-25650 / CL 118,532 / CL-118532 / WY-42462|
|Approved Prescription Products|
|Approved Generic Prescription Products||Not Available|
|Approved Over the Counter Products||Not Available|
|Unapproved/Other Products||Not Available|
|Brand mixtures||Not Available|
|Weight||Average: 1311.473 |
Triptorelin is indicated for the palliative treatment of advanced prostate cancer.
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.
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.
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.
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|
|Pharmacogenomic Effects/ADRs||Not Available|
|Food Interactions||Not Available|
|Synthesis Reference||Not Available|
|ATC Codes||L02AE04 — Triptorelin|
|AHFS Codes||Not Available|
|PDB Entries||Not Available|
|FDA label||Download (691 KB)|
|Experimental Properties||Not Available|
|Predicted ADMET features||Not Available|
|Mass Spec (NIST)||Not Available|
|Description||This compound belongs to the class of organic compounds known as polypeptides. These are peptides containing ten or more amino acid residues.|
|Super Class||Organic Polymers|
|Sub Class||Not Available|
|Alternative Parents||Peptides / Tyrosine and derivatives / Phenylalanine and derivatives / Histidine and derivatives / Leucine and derivatives / Proline and derivatives / N-acyl-alpha amino acids and derivatives / Tryptamines and derivatives / Alpha amino acid amides / Serine and derivatives / 3-alkylindoles / Amphetamines and derivatives / Glycine and derivatives / Pyrrolidinecarboxamides / N-acylpyrrolidines / 1-hydroxy-2-unsubstituted benzenoids / Substituted pyrroles / Pyrrolidine-2-ones / N-acyl amines / Imidazoles / Heteroaromatic compounds / Tertiary carboxylic acid amides / Primary carboxylic acid amides / Lactams / Guanidines / Tertiary amines / Secondary carboxylic acid amides / Propargyl-type 1,3-dipolar organic compounds / Carboximidamides / Azacyclic compounds / Hydrocarbon derivatives / Carbonyl compounds / Primary alcohols / Organic oxides|
|Substituents||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 / Alpha-amino acid amide / Triptan/ Serine or derivatives / Amphetamine or derivatives / Glycine or derivatives / N-substituted-alpha-amino acid / 3-alkylindole / Indole / Indole or derivatives / Pyrrolidine carboxylic acid or derivatives / Pyrrolidine-2-carboxamide / N-acylpyrrolidine / Phenol / 1-hydroxy-2-unsubstituted benzenoid / Pyrrolidone / Benzenoid / N-acyl-amine / Substituted pyrrole / Fatty acyl / Fatty amide / Monocyclic benzene moiety / 2-pyrrolidone / Azole / Heteroaromatic compound / Imidazole / Tertiary carboxylic acid amide / Pyrrole / Pyrrolidine / Secondary carboxylic acid amide / Amino acid or derivatives / Primary carboxylic acid amide / Tertiary amine / Carboxamide group / Guanidine / Lactam / Carboximidamide / Propargyl-type 1,3-dipolar organic compound / Carboxylic acid amide / Carboxylic acid derivative / Organic 1,3-dipolar compound / Azacycle / Organoheterocyclic compound / Amine / Carbonyl group / Hydrocarbon derivative / Alcohol / Organooxygen compound / Organonitrogen compound / Organic nitrogen compound / Primary alcohol / Organic oxygen compound / Organic oxide / Aromatic heteropolycyclic compound|
|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 (FSH). This receptor mediates its action by association with G-proteins that activate a phosphatidylinositol-calcium second messenger system. Isoform 2 may act as an inhibitor of GnRH-R signaling.
- Gene Name:
- Uniprot ID:
- Uniprot Name:
- Gonadotropin-releasing hormone receptor
- Molecular Weight:
- 37730.355 Da