4526. Goserelin

Nomenclature

CAS number: 65807-02-5
6-[O-(1,1-Dimethylethyl)-d-serine]-10-deglycinamideluteinizing hormone-releasing factor (pig) 2-(aminocarbonyl)hydrazide; d-Ser(But)6Azgly10-gonadorelin; d-Ser(But)6Azgly10-luliberin; ICI-118630.
C59H84N18O14; mol wt 1269.41.
C 55.82%, H 6.67%, N 19.86%, O 17.65%.

Description and references

Synthetic peptide agonist analog of LH-RH, q.v. Prepn: A. S. Dutta et al., DE 2720245; eidem, US 4100274 (1977, 1978 both to I.C.I.); eidem, J. Med. Chem. 21, 1018 (1978). Radioimmunoassay in serum: R. N. Clayton et al., Clin. Endocrinol. 22, 453 (1985). Endocrine effects in women: C. P. West, D. T. Baird, ibid. 26, 213 (1987). Review of pharmacokinetics and therapeutic efficacy in sex hormone related disorders: P. Chrisp, K. L. Goa, Drugs 41, 254-288 (1991). Clinical trial in treatment of uterine fibroids: J. Gerris et al., Horm. Res. 45, 279 (1996); in prostate cancer: M. Bolla et al., N. Engl. J. Med. 337, 295 (1997).

Chemical structure

Derivative

Acetate.

Nomenclature

Zoladex (AstraZeneca).

Description and references

C59H84N18O14.xC2H4O2, where x = 1 to 2.4.

Properties

Off-white powder. Freely sol in acetic acid; sol in water, 0.1M HCl, 0.1M NaCl, DMF, DMSO. Insol in acetone, chloroform, ether.

Therapeutic Category

Antineoplastic (hormonal).

Keywords

Antineoplastic (Hormonal); LH-RH Analogs; LH-RH Agonist