3. Abarelix

Nomenclature

CAS number: 183552-38-7
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; Ac-d-Nal1-4-Cl-d-Phe2-d-Pal3-N-Me-Tyr5-d-Asn6-Lys(iPr)8-d-Ala10-LH-RH; PPI-149; Plenaxis (Praecis).
C72H95ClN14O14; mol wt 1416.06.
C 61.07%, H 6.76%, Cl 2.50%, N 13.85%, O 15.82%.

Description and 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) DOI PubMed. Clinical pharmacology: S. L. Wong et al., Clin. Pharmacol. Ther. 73, 304 (2003) DOI PubMed; of depot formulation: eidem, J. Clin. Pharmacol. 44, 495 (2004) DOI PubMed. Review of clinical development: P. Mongiat-Artus, P. Teillac, Expert Opin. Pharmacother. 5, 2171-2179 (2004) DOI PubMed.

Properties

White solid. Sol in water.

Therapeutic Category

Antineoplastic (hormonal).

Keywords

Antineoplastic (Hormonal); LH-RH Analogs