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MedKoo product information:

 Abarelix

MedKoo Code#:  100010

Name:  Abarelix

CAS#:   183552-38-7 　 Synonym:  Synonym: Plenaxis. Code names: PPI-149; R-3827.   IUPAC/Chemical name: acetyl-D-ß-naphthylalanyl- D-4-chlorophenylalanyl-D-3-pyridylalanyl-L-seryl-L- N-methyl-tyrosyl-D-asparagyl-L-leucyl-L-N(e )-isopropyl-lysyl-L-prolyl-D-alanyl-amide.

Chemical structure:

Theoretical analysis

Chemical Formula: C72H95ClN14O14 Exact Mass: 1414.68407 Molecular Weight: 1416.06 m/z: 1414.68407 (100.0%), 1415.68743 (77.9%), 1416.68112 (32.0%), 1416.69078 (29.9%), 1417.68448 (24.9%), 1418.68783 (9.6%), 1417.69414 (7.5%), 1415.68111 (5.2%), 1416.68446 (4.0%), 1416.68832 (2.9%), 1419.69119 (2.4%), 1417.69167 (2.2%), 1417.67816 (1.7%), 1417.68782 (1.5%), 1418.69749 (1.4%), 1418.68151 (1.3%), 1415.69035 (1.1%) Elemental Analysis: C, 61.07; H, 6.76; Cl, 2.50; N, 13.85; O, 15.82

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Abarelix is a synthetic decapeptide and antagonist of naturally occurring gonadotropin-releasing hormone (GnRH). Abarelix directly and competitively binds to and blocks the gonadotropin releasing hormone receptor in the anterior pituitary gland, thereby inhibiting the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. As a result, this may relieve symptoms associated with prostate hypertrophy or prostate cancer, since testosterone is required to sustain prostate growth. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

Abarelix is an 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. It is marketed by Speciality European Pharma as Plenaxis. Plenaxis has received marketing authorisation in Germany. 

Abarelix for injectable suspension (Plenaxis™) is a synthetic decapeptide with potent antagonistic activity against naturally occurring gonadotropin releasing-hormone (GnRH).
Plenaxis™ inhibits gonadotropin and related androgen production by directly and competitively blocking GnRH receptors in the pituitary.

Abarelix is chemically described as acetyl-D-ß-naphthylalanyl- D-4-chlorophenylalanyl-D-3-pyridylalanyl-L-seryl-L- N-methyl-tyrosyl-D-asparagyl-L-leucyl-L-N(e )-isopropyl-lysyl-L-prolyl-D-alanyl-amide. It is initially manufactured as an acetate water complex and converted to a carboxymethylcellulose (CMC) water complex in manufacturing the drug product. The molecular weight for abarelix anhydrous free base is 1416.06. Abarelix for injectable suspension is supplied as a white to off-white sterile dry powder which, when mixed with the diluent, 0.9% Sodium Chloride Injection, USP, becomes a depot suspension intended for intramuscular (IM) injection. The single-dose vial contains 113 mg of anhydrous free base abarelix peptide (net) supplied in an abarelix CMC complex. This complex also contains 19.1 to 31 mg of CMC. After the vial is reconstituted with 2.2 mL of 0.9% sodium chloride injection, 2 mL is administered to deliver a dose of 100 mg of abarelix (net) as the abarelix CMC complex at a pH of 5±1.

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