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DATA GRAPHICS | Product Development

Companies aiming for PARP-1 selectivity

A second generation of PARP inhibitors focused on PARP-1 selectivity starts to make progress

May 12, 2023 9:58 PM UTC

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...

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