GnRH antagonist decapeptides

Details GnRH antagonist decapeptides GnRH antagonist decapeptides

1997-04-11

1998-10-13

Tsang, Cecilia J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530328, A61K 3809, C07K 706

Patent

active

058212302

ABSTRACT:
Peptides are provided which have improved duration of GnRH antagonistic properties and/or which can be synthesized more economically. These antagonists may be used in the same manner as the compounds of which they are analogs to regulate fertility and to treat steroid-dependent tumors and for other short-term and long-term treatment indications. One particularly effective peptide, a decapeptide analog of the GnRH antagonist Acyline, has the formula: Ac-D-2Nal-D-4Cpa-D-Dpr(methylcarbamoyl)-Ser-4Aph(acetyl)-D-4Aph(acetyl)-Le u-Lys(isopropyl)-Pro-D-Ala-NH.sub.2. It continues to exhibit very substantial suppression of LH secretion at 96 hours following injection. Other economically attractive and pharmacologically effective analogs have the formulas: Ac-D-2Nal-D-4Cpa-Xaa.sub.3 -Ser-4Aph(acetyl)-D-4Aph(acetyl)-Leu-Lys(isopropyl)-Pro-D-Ala-NH.sub.2 ; and Ac-D-2Nal-D-4Cpa-Xaa.sub.3 -Ser-4Aph(hydroorotyl)-D-4Aph(acetyl)-Leu-Lys(isopropyl)-Pro-D-Ala-NH.sub. 2, wherein Xaa.sub.3 is D-Gln or Gln.

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