Title: Abarelix
CAS Registry Number: 183552-38-7
CAS Name: N-Acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparaginyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-D-alaninamide
Additional Names: Ac-D-Nal1-4-Cl-D-Phe2-D-Pal3-N-Me-Tyr5-D-Asn6-Lys(iPr)8-D-Ala10-LH-RH
Manufacturers' Codes: PPI-149
Trademarks: Plenaxis (Praecis)
Molecular Formula: C72H95ClN14O14
Molecular Weight: 1416.06
Percent Composition: C 61.07%, H 6.76%, Cl 2.50%, N 13.85%, O 15.82%
Literature References: Decapeptide LH-RH antagonist. Prepn: R. W. Roeske, WO 9640757 (1996 to Indiana Univ. Found.); idem, US 5843901 (1998 to Adv. Res. Technol. Inst.). Pharmacology and suppression of plasma gonadotropins: C. J. Molineaux et al., Mol. Urol. 2, 265 (1998). Clinical comparison with leuprolide in prostate cancer: J. Trachtenberg et al., J. Urol. 167, 1670 (2002). Clinical pharmacology: S. L. Wong et al., Clin. Pharmacol. Ther. 73, 304 (2003); of depot formulation: eidem, J. Clin. Pharmacol. 44, 495 (2004). Review of clinical development: P. Mongiat-Artus, P. Teillac, Expert Opin. Pharmacother. 5, 2171-2179 (2004).
Properties: White solid. Sol in water.
Therap-Cat: Antineoplastic (hormonal).
Keywords: Antineoplastic (Hormonal); LH-RH Analogs. |