The Development of INT131 as a Selective PPARγ Modulator: Approach to a Safer Insulin Sensitizer

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The Development of INT131 as a Selective PPARγ Modulator: Approach to a Safer Insulin Sensitizer

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Title: The Development of INT131 as a Selective PPARγ Modulator: Approach to a Safer Insulin Sensitizer
Author: Higgins, Linda S.; Mantzoros, Christos S.

Note: Order does not necessarily reflect citation order of authors.

Citation: Higgins, Linda S. and Christos S. Mantzoros. 2008. The Development of INT131 as a Selective PPARγ Modulator: Approach to a Safer Insulin Sensitizer. PPAR Research 2008: 936906.
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Abstract: INT131 (formerly T0903131, T131, AMG131) is a potent non-thiazolidinedione (TZD) selective peroxisome proliferator-activated receptor γ modulator (SPPARM) currently in Phase 2 clinical trials for treatment of type-2 diabetes mellitus (T2DM). This new chemical entity represents a second generation SPPARM approach developed after the first generation PPARγ full agonists to address their inherent limitations. INT131 was specifically and carefully designed using preclinical models to exhibit a biological profile of strong efficacy with de minimis side effects compared to PPARγ full agonists. As a potent PPARγ modulator, INT131 binds to PPARγ with high affinity. In pharmacology models of diabetes and in early clinical studies, it achieved a high level of efficacy in terms of antidiabetic actions such as insulin sensitization and glucose and insulin lowering, but had little activity in terms of other, undesired, effects associated with TZD PPARγ full agonists such as edema and adipogenesis. Ongoing clinical development is directed at translating these findings into establishing a novel and effective treatment for T2DM patients with an improved safety profile in relation to that currently available.
Published Version: doi:10.1155/2008/936906
Other Sources: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2522386/pdf/
Terms of Use: This article is made available under the terms and conditions applicable to Other Posted Material, as set forth at http://nrs.harvard.edu/urn-3:HUL.InstRepos:dash.current.terms-of-use#LAA
Citable link to this page: http://nrs.harvard.edu/urn-3:HUL.InstRepos:4891675

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