lartesertib

Lartesertib is an orally bioavailable, small molecule ATP-competitive inhibitor of ataxia telangiectasia mutated kinase (ATM), a serine/threonine protein kinase that plays a critical role in the DNA damage response. By binding to and inhibiting ATM, lartesertib disrupts ATM-mediated signaling, prevents activation of DNA damage checkpoints, impairs DNA repair mechanisms, and induces apoptosis in tumor cells—particularly those overexpressing ATM. This mechanism also sensitizes cancer cells to chemotherapy and radiotherapy. Lartesertib is being investigated for the treatment of various advanced solid tumors and has shown synergy with PARP inhibitors, topoisomerase inhibitors, and ATR inhibitors in preclinical models. The drug is currently under clinical investigation with its maximum trial phase reported as Phase II[1][3][4][5][6].

Other names

lartesertib