Description
TG100-115 is an inhibitor of p110δ PI3K and p110γ PI3K that exhibits anti-inflammatory and anti-asthma activities. TG100-115 decreases pulmonary eosinophil levels and accumulation of IL-13 and mucin in animal models of asthma and chronic obstructive pulmonary disorder (COPD), decreasing inflammation. TH100-115 also inhibits edema and inflammation induced by VEGF and platelet activating factor (PAF) in other animal models, decreasing development of infarcts and improving cardiac function. As a result of its cardioprotective activity, TG100-115 is currently in clinical trials as a potential treatment to reduce acute myocardial infarctions.
References
Doukas J, Eide L, Stebbins K, et al. Aerosolized phosphoinositide 3-kinase gamma/delta inhibitor TG100-115 [3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol] as a therapeutic candidate for asthma and chronic obstructive pulmonary disease. J Pharmacol Exp Ther. 2009 Mar;328(3):758-65. PMID: 19056934.
Doukas J, Wrasidlo W, Noronha G, et al. Isoform-selective PI3K inhibitors as novel therapeutics for the treatment of acute myocardial infarction. Biochem Soc Trans. 2007 Apr;35(Pt 2):204-6. PMID: 17371238.
Doukas J, Wrasidlo W, Noronha G, et al. Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury. Proc Natl Acad Sci U S A. 2006 Dec 26;103(52):19866-71. PMID: 17172449.
