Abarelix
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Abarelix
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CAS No:
183552-38-7
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Formula:
C72H95ClN14O14
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Chemical Name:
Abarelix
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Synonyms:
PPI-149;Abarelix Acetate;Abarelix;Plenaxis;R 3827;Ac-DNal-DCpa-DPal-Ser-NαMeTyr-DAsp-Leu-Ilys-Pro-DAl-NH2;Abarelix Acetate(Plenaxis)
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CAS No:
Description
ChEBI: A polypeptide compound composed of ten natural and non-natural amino acid resiudes in a linear sequence.Abarelix is an antagonist of the gonadotropin releasing-hormone (Gn RH) receptor, and it was launched as an intramuscular injection for the palliative treatment of advanced symptomatic prostate cancer. Hormonal therapy of prostate cancer is based on the modulation of testosterone to achieve medical castration levels. The inhibition of GnRH activity causes the suppression of luteini
Abarelix is a polypeptide compound composed of ten natural and non-natural amino acid resiudes in a linear sequence. It has a role as a hormone antagonist and an antineoplastic agent.|Synthetic decapeptide antagonist to gonadotropin releasing hormone (GnRH). It is marketed by Praecis Pharmaceuticals as Plenaxis. Praecis announced in June 2006 that it was voluntarily withdrawing the drug from the market.
Abarelix Basic Attributes
1416.08
1414.684082
1592732-453-0
DTXSID20171443
L - Antineoplastic and immunomodulating agents
Characteristics
425
5.18
1.286±0.06 g/cm3(Predicted)
1688.4±65.0 °C(Predicted)
974.9±34.3 °C
1.601
0mmHg at 25°C
Toxicity
The 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.
96-99%
Drug Information
For palliative treatment of advanced prostate cancer.|FDA Label
Used in the palliative treatment of advanced prostate cancer. Abarelix is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis.
Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites. (See all compounds classified as Hormone Antagonists.)
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.
In 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.
13.2 ± 3.2 days
Abarelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion.
abarelix
Abarelix Use and Manufacturing
Gonad-stimulating principle; antagonist (LHRH).
Human drugs -> Rare disease (orphan)|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients
Computed Properties
Molecular Weight:1416.1
XLogP3:3.7
Hydrogen Bond Donor Count:13
Hydrogen Bond Acceptor Count:16
Rotatable Bond Count:38
Exact Mass:1414.6840715
Monoisotopic Mass:1414.6840715
Topological Polar Surface Area:425
Heavy Atom Count:101
Complexity:2770
Defined Atom Stereocenter Count:10
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes
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