PMID- 18769500
OWN - NLM
STAT- PubMed-not-MEDLINE
DCOM- 20110714
LR  - 20220310
IS  - 1687-4757 (Print)
IS  - 1687-4765 (Electronic)
VI  - 2008
DP  - 2008
TI  - The Development of INT131 as a Selective PPARgamma Modulator: Approach to a Safer 
      Insulin Sensitizer.
PG  - 936906
LID - 10.1155/2008/936906 [doi]
LID - 936906
AB  - INT131 (formerly T0903131, T131, AMG131) is a potent non-thiazolidinedione (TZD) 
      selective peroxisome proliferator-activated receptor gamma 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 PPARgamma 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 PPARgamma full agonists. As a potent PPARgamma 
      modulator, INT131 binds to PPARgamma 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 PPARgamma 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.
FAU - Higgins, Linda S
AU  - Higgins LS
AD  - InteKrin Therapeutics, Inc., 4300 El Camino Real, Suite 201, Los Altos, CA 94022, 
      USA.
FAU - Mantzoros, Christos S
AU  - Mantzoros CS
LA  - eng
PT  - Journal Article
PL  - United States
TA  - PPAR Res
JT  - PPAR research
JID - 101269101
PMC - PMC2522386
EDAT- 2008/09/05 09:00
MHDA- 2008/09/05 09:01
PMCR- 2008/08/26
CRDT- 2008/09/05 09:00
PHST- 2008/03/18 00:00 [received]
PHST- 2008/06/14 00:00 [accepted]
PHST- 2008/09/05 09:00 [pubmed]
PHST- 2008/09/05 09:01 [medline]
PHST- 2008/09/05 09:00 [entrez]
PHST- 2008/08/26 00:00 [pmc-release]
AID - 10.1155/2008/936906 [doi]
PST - ppublish
SO  - PPAR Res. 2008;2008:936906. doi: 10.1155/2008/936906.