TG100801

TG100801 is a topically applied small molecule prodrug developed for the treatment of ocular diseases characterized by angiogenesis, vascular leakage, and inflammation. It is administered as an eye drop and is converted in the eye to its active form, TG100572. The drug acts as a multi-targeted kinase inhibitor, specifically inhibiting vascular endothelial growth factor receptors (VEGFR1/2/3) and Src family kinases. By blocking these targets, TG100801 suppresses VEGF-mediated retinal leakage and choroidal neovascularization—key pathological features of age-related macular degeneration (AMD), diabetic retinopathy (DR), diabetic macular edema (DME), and proliferative diabetic retinopathy (PDR). Preclinical studies demonstrated that topical administration leads to therapeutic levels in posterior ocular tissues with minimal systemic exposure. Clinical trials showed that it was well tolerated when applied twice daily for up to 14 days[1][2][6][8].

Other names

4-chloro-3-(5-methyl-3-((4-(2-pyrrolidin-1-ylethoxy)phenyl)amino)-1,2,4-benzotriazin-7-yl)phenol