9748. Triptorelin

Nomenclature

CAS number: 57773-63-4
6-d-Tryptophanluteinizing hormone-releasing factor (pig); 6-d-tryptophan-LH-RH; d-trp6-LHRH; d-Trp6LRH; d-trp6-gonadorelin; détryptoréline; AY-25650; Wy-42462; Wy-42422.
C64H82N18O13; mol wt 1311.45.
C 58.61%, H 6.30%, N 19.22%, O 15.86%.

Description and references

Synthetic peptide agonist analog of LH-RH, q.v. Prepn: A. V. Schally, D. H. Coy, DE 2625843; eidem, US 4010125 (1976, 1977); D. H. Coy et al., J. Med. Chem. 19, 423 (1976). Comparison with LH-RH of in vitro activity: D. H. Coy et al., Biochem. Biophys. Res. Commun. 67, 576 (1975). Pharmacokinetics and metabolism in humans: J. L. Barron et al., J. Clin. Endocrinol. Metab. 54, 1169 (1982). HPLC analysis: D. C. Serti et al., J. Liq. Chromatogr. 4, 1135 (1981). RIA in human serum: M. Mason-Garcia et al., Proc. Natl. Acad. Sci. USA 82, 1547 (1985). Clinical trial for in vitro fertilization: A. Hazout et al., Fertil. Steril. 59, 596 (1993). Clinical trial in prostate cancer: C. F. Heyns et al., BJU Int. 92, 226 (2003); in severe endometriosis: A. Y. K. Wong, L. Tang, Fertil. Steril. 81, 1522 (2004).

Chemical structure

Properties

Fluffy, white solid. [α]D23 58.8° (c = 0.33 in acetic acid).

Derivative

Acetate.

Nomenclature

CAS number: 140194-24-7
Gonapeptyl (Ferring).
C64H82N18O13.C2H4O2; mol wt 1371.50.
C 57.80%, H 6.32%, N 18.38%, O 17.50%.

Derivative

Pamoate.

Nomenclature

CAS number: 124508-66-3
Decapeptyl (Ipsen); Trelstar (Watson).
C64H82N18O13.C23H16O6; mol wt 1699.82.
C 61.47%, H 5.81%, N 14.83%, O 17.88%.

Therapeutic Category

Antineoplastic (hormonal); in treatment of endometriosis and infertility.

Keywords

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