CLR457

CLR457 (also known as NVP-CLR457 or compound 40) is an orally bioavailable, balanced pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor developed for the treatment of advanced solid tumors with PI3K pathway activation. It inhibits all class I PI3K isoforms (p110α, p110β, p110δ, and p110γ), leading to apoptosis and growth inhibition in tumor cells overexpressing PI3K. The drug was designed to minimize central nervous system penetration and off-target microtubule effects seen with earlier inhibitors like buparlisib. Despite demonstrating dose-dependent antitumor activity in preclinical models and early clinical trials, CLR457's development was terminated due to poor tolerability and limited efficacy in patients[1][2][4][6][7].

Other names

compound 40compound40compound-40