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A Phase I Study of the DNA-PK Inhibitor Peposertib in Combination with Radiotherapy with or without Cisplatin in Patients with Advanced Head and Neck Tumors

Sep 24, 2023 | redjournal.org | Michael N. Samuels |Thomas Jefferson |Johan Falkenius |Voichita Bar-Ad

Abstract DNA-dependent protein kinase (DNA-PK) plays a key role in the repair of DNA double-strand breaks (DSBs) via non-homologous end joining. Inhibition of DNA-PK can enhance the effect of DNA DSB-inducing anticancer therapies. Peposertib (formerly M3814) is an orally administered, potent, and selective small molecule DNA-PK inhibitor that has demonstrated radiosensitizing and antitumor activity in xenograft models and was well-tolerated in monotherapy.

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