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Patent Searching and Data


Title:
METHOD FOR EVALUATING THERAPEUTIC EFFICACY
Document Type and Number:
WIPO Patent Application WO2002064092
Kind Code:
A3
Abstract:
The present invention relates to in vitro methods for evaluating compounds that better correlate with therapeutic efficiency than evaluating compounds based on potency alone. In general, the inventive methods comprises: (i) determining a potency value for a compound against its target receptor; (ii) determining a potency value for a compound against its target receptor; and (iii) comparing the potency value wit the desensitization value. If the desired action of a compound is as a receptor agonist, the compound's desensitization value should be larger than the compound's potency value. This ensures that the concentration of a compound required for potency will not also cause the receptor to desensitize at the same time, thus in an essence nullifying the desired effect. The inventive methods are used to evaluate novel motilide compounds as well as ABT-229 and EM-574, two motilide compounds for which clinical trials have been initiated.

Inventors:
CARRERAS CHRISTOPHER (US)
DILLON SUSAN (US)
Application Number:
PCT/US2002/004462
Publication Date:
March 06, 2003
Filing Date:
February 15, 2002
Export Citation:
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Assignee:
KOSAN BIOSCIENCES INC (US)
CARRERAS CHRISTOPHER (US)
DILLON SUSAN (US)
International Classes:
A61K31/7048; A61P1/00; A61P1/04; A61P1/08; A61P1/10; A61P1/14; A61P43/00; C07H17/00; C07H17/08; C07H21/04; C07K14/72; C12N5/08; C12N5/10; C12N15/09; C12Q1/02; G01N33/15; G01N33/50; G01N33/566; G01N33/74; (IPC1-7): G01N33/53; G01N33/566; G01N33/567
Other References:
CHIDIAC ET AL.: "Agonist-induced modulation of inverse agonist efficacy at the beta2-adrenergic receptor", MOLECULAR PHARMACOLOGY, vol. 50, 1996, pages 662 - 669, XP002956492
FEIGHNER ET AL.: "Receptor for motilin identified in the human gastrointestinal system", SCIENCE, vol. 284, 25 June 1999 (1999-06-25), pages 2184 - 2188, XP001088406
KOVOOR ET AL.: "Agonist induced homologous desensitization of mu-opioid receptors mediated by G protein-coupled receptor kinases is dependant on agonist efficacy", MOLECULAR PHARMACOLOGY, vol. 54, 1998, pages 704 - 711, XP002956491
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