Method for evaluating therapeutic efficacy
US6875576B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Feb 15, 2002 |
| Grant date | Apr 5, 2005 |
| Priority date | — |
| Expiry date | Aug 12, 2022 |
Classification
- Technology area (CPC G)Physics
- CPC primaryG01N2500/00
- WIPO fieldMeasurement
- WIPO sectorInstruments
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 method comprises: (i) determining a potency value for a compound against its target receptor; (ii) determining a desensitization value for the compound against its target receptor; and (iii) comparing the potency value with the desensitization value. If the desired action of a compound is as a receptor agonist, then 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.