Artios Announces ATR Inhibitor, ART0380, Development On Track and Progressing Into Phase 1b Evaluation


  • Phase 1a dose escalation of ART0380 defined initial regimen to be evaluated in Phase 1b setting.
  • Phase 1a dose escalation demonstrated a predictable safety profile and no unexpected safety findings supported by data from over 35 patients.
  • Dose-dependent target engagement in tumor cells but not normal mononuclear cells supported by gH2AX DNA damage biomarker data (poster presentation at AACR 2022 will feature biomarker and pharmacokinetic data supporting clinical dose selection of ART0380).
  • Rapid absorption and elimination with dose proportional increases in exposure provides dosing flexibility across different administration schedules.
  • Dose escalation shows ART0380 to have clinical activity and supports initiation of Phase 1b dose expansion study targeting ATM deficient tumors. Data from the Phase 1b dose expansion study is expected in the first half of 2023.

Artios Pharma Limited (Artios), a clinical-stage biotech company pioneering the development of novel small molecule therapeutics that target the DNA damage response (“DDR”) process in order to treat patients suffering from a broad range of cancers, announces that the development of its ataxia telangiectasia and Rad3-related (“ATR”) Inhibitor, ART0380, has progressed into a Phase 1b dose expansion study targeting ATM deficient tumors.

Artios also announces a poster presentation at the upcoming American Association for Cancer Research (AACR) Annual Meeting, taking place April 8-13, 2022, in New Orleans, Louisiana featuring biomarker and pharmacokinetic data supporting the clinical dose selection of ART0380.

Dr. Niall Martin, Chief Executive Officer at Artios, said: “As a strong regulator of DNA repair, ATR inhibition can effectively suppress tumor growth across a broad range of cancers harboring genetic defects. However, durability and long-term use with first-generation ATR inhibitors has been limited by challenges with toxicity and tolerability. The pharmacokinetic profile of ART0380 has the potential to allow reliable and predictable dosing. We are highly encouraged with the initial dose escalation data which demonstrates that ART0380 is engaging the desired cancer pharmacodynamic targets, has a predictable and manageable safety profile and is clinically active in tumors predicted to be sensitive to ATR inhibition. We look forward to additional data from the dose expansion Phase 1b study targeting ATM deficient tumors in the first half of 2023.”

Melissa Johnson, MD, Program Director, Lung Cancer Research, Sarah Cannon Research Institute at Tennessee Oncology, Principal Investigator for the trial, said: “Following the successful completion of the intermittent monotherapy dose escalation, ART0380 has progressed to the dose expansion phase for evaluation in patients with cancers expressing low levels of the ATM protein. We also continue to explore the therapeutic potential of ART0380 in combination with gemcitabine and irinotecan.”

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Article published: 05.04.22