Companies aiming for PARP-1 selectivity
A second generation of PARP inhibitors focused on PARP-1 selectivity starts to make progress
At least 11 companies aim to improve on the foundation laid by first-generation PARP inhibitors by creating PARP-1 selective compounds that dial out the hematopoietic toxicity that comes with PARP-2 inhibition.
Five PARP inhibitors have been approved globally since the FDA approval of Lynparza olaparib in 2014, but all of them target both PARP-1 and PARP-2. The latter is now recognized as non-essential for the class’ antitumor activity, while being the driver of its hematopoietic toxicity...