Overcoming resistance to PARP inhibitors, polymerase theta inhibitors entered the clinic for the first time

On September 28, 2021, Artios Pharma announced that its highly selective DNA polymerase theta (Polθ) inhibitor ART4215 has been administered to the first patient in a phase 1/2a clinical trial

This open-label, multi-center clinical trial will evaluate the safety, tolerability, pharmacokinetics and clinical effects of oral ART4215 as a single agent or in combination with other anti-cancer drugs in patients with advanced or metastatic solid tumors It is planned to enroll 206 patients, and it is expected that mid-term safety and tolerability data will be obtained in 2022

Artios is actively developing a promising product line of potential "best-in-class" and "first-in-class" DNA damage response (DDR) therapy, which can inhibit new types of DNA repair in tumors with weakened DNA damage response.

As a DNA polymerase, Polθ participates in repairing DNA double-strand breaks

Reference materials:

[1] Artios Doses First Patient in Phase 1/2a Study of Polθ Inhibitor ART4215.

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