- Molecular NameAbarelix
- Synonymabarelix
- Weight1416.09
- Drugbank_IDDB00106
- ACS_NO183552-38-7
- Show 2D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)N/A
- pkaN/A
- LogD (pH=7, predicted)N/A
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)N/A
- LogSw (predicted, AB/LogsW2.0)N/A
- Sw (mg/ml) (predicted, ACD/Labs)N/A
- No.of HBond DonorsN/A
- No.of HBond AcceptorsN/A
- No.of Rotatable BondsN/A
- TPSAN/A
- StatusFDA approved
- AdministrationInjection
- PharmacologyAn injectable gonadotropin-releasing hormone antagonist (GnRH antagonist). It is primarily used in oncology to reduce the amount of testosterone made in patients with advanced symptomatic prostate cancer for which no other treatment options are available. It belongs to the family of drugs called Gonadotropin-releasing hormone antagonists.
- Absorption_valueN/A
- Absorption (description)Following IM administration of 100 mg, abarelix is absorbed slowly with a mean peak concentration of 43.4 ng/mL observed approximately 3 days after the injection.
- Caco_2N/A
- BioavailabilityN/A
- Protein binding97.5
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmIn vitro hepatocyte (rat, monkey, human) studies and in vivo studies in rats and monkeys showed that the major metabolites of abarelix were formed via hydrolysis of peptide bonds. No significant oxidative or conjugated metabolites of abarelix were found either in vitro or in vivo. There is no evidence of cytochrome P-450 involvement in the metabolism of abarelix.
- Half life13.2 days
- ExcretionN/A
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityThe maximum tolerated dose of abarelix has not been determined. The maximum dose used in clinical studies was 150 mg. There have been no reports of accidental overdose with abarelix.
- LD50 (rat)N/A
- LD50 (mouse)N/A