Drug intelligence / Profile preview

art4215

Development stage
Phase 1
Lead developer
Artios Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

ART4215 is a first-in-class, selective, orally bioavailable small molecule inhibitor of DNA polymerase theta (Polθ). Polθ is a tumor-specific DNA damage response (DDR) target involved in microhomology-mediated end joining (MMEJ), a DNA repair pathway that is overexpressed in many tumors and found at low levels in healthy tissue. By inhibiting Polθ, ART4215 causes DNA damage in cancer cells, preventing them from dividing and multiplying. The drug has shown broad potential clinical utility based on preclinical studies and is being evaluated as monotherapy and in combination with PARP inhibitors such as talazoparib for the treatment of advanced or metastatic solid tumors, including BRCA-deficient breast cancer. ART4215 was originally developed by Artios Pharma after being in-licensed from Cancer Research Technology (now Cancer Research Horizons)[1][3][7].

Other names
ART-4215ART4215ART 4215
02

Targets

POLQ (DNA polymerase theta)

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