INT 131

05/01/2011 - "This study was conducted to determine short-term efficacy and safety of INT131 besylate in patients with Type 2 diabetes mellitus (T2DM). "
03/01/2012 - "If these data are confirmed in humans, INT131 could be used for treating type 2 diabetes without loss in bone mass."
03/13/2009 - "INT131 is currently being evaluated in a clinical setting as a therapeutic agent for the treatment of type 2 diabetes."
07/01/2014 - "This placebo-controlled study compared the efficacy and side effects of INT131 besylate versus 45 mg pioglitazone HCl in subjects with type 2 diabetes (T2D). "
04/01/2009 - "INT-131, a PPARgamma agonist for the treatment of type 2 diabetes."

04/01/2009 - "INT-131 also compared favorably with TZDs in 6-month toxicity studies in rats and monkeys, exhibiting no increases in body or organ weights, and no relevant observations of edema or other fluid retention, which has been associated with congestive heart failure in TZDs. "
07/01/2014 - "With the 1-mg dose, INT131 provided significant improvements in glycemic control (HbA1c 0.8 ± 0.12; P < 0.001 vs. placebo) but with less edema, weight gain, and hemodilution than observed with 45 mg pioglitazone. "
04/01/2012 - "Early phase human studies with INT131 look promising with changes in plasma lipids and glucose being equal or better than what is seen with rosiglitazone and pioglitazone treatment but without evidence of edema. "

02/15/2013 - "Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity."
03/01/2012 - "In preclinical studies and a phase II clinical trial, INT131 has been shown to lower glucose levels and ameliorate insulin resistance without typical TZD side effects. "
03/01/2012 - "Treatment with INT131 enhanced systemic insulin sensitivity, as revealed by lower insulin levels in the fasted state and an increase in the area above the curve during an insulin tolerance test. "
03/13/2009 - "In adipocytes, INT131 showed minimal stimulation of adipocyte differentiation and partially activated PPAR gamma target genes involved in adipogenesis and, at the same time, showed more agonistic activity on another set of target genes that may influence insulin sensitivity directly. "
05/01/2011 - "INT131 besylate is a potent non-thiazolidinedione selective peroxisome proliferator-activated receptor γ (PPARγ) modulator (SPPARM) designed to improve insulin sensitivity and glucose metabolism while minimizing the side effects of full agonist thiazolidinediones. "

01/01/2020 - " goal of this study was to examine the effect of INT131 in the context of EcoHIV-induced inflammation in vitro, in primary cultures of mouse glial cells and in vivo, in a mouse model of EcoHIV-associated brain inflammation, as well as characterize its pharmacokinetic properties and brain penetration. "

05/01/2011 - "This was a 4-week randomized, double-blind, placebo-controlled multi-center study with 1 or 10mg INT131 besylate or placebo daily in subjects with T2DM not receiving pharmacotherapy for their hyperglycemia. "