Target: Chk1 | Disease State: Solid Tumors

Introduction / Brief Description

GDC-0575 is a highly selective small-molecule Chk1 inhibitor invented by Array and licensed to Genentech. Genentech is responsible for all clinical development and commercialization activities. Array received an upfront payment of $28 million and is eligible to receive clinical and commercial milestone payments up to $380 million and up to double-digit royalties on sales.

Chk1 is a protein kinase that regulates the tumor cell's response to DNA damage often caused by treatment with chemotherapy. In response to DNA damage, Chk1 blocks cell cycle progression in order to allow for repair of damaged DNA, thereby limiting the efficacy of chemotherapeutic agents. Inhibiting Chk1 in combination with chemotherapy can enhance tumor cell death by preventing these cells from recovering from DNA damage. GDC‑0575 is designed to enhance the efficacy of some chemotherapeutic agents. GDC-0575 is currently advancing in a Phase 1 trial in patients with lymphoma or solid tumors.

Clinical Trials

To learn more about GDC-0575 clinical trials, click here.

Publications and Presentations



Oncology Research Featuring Preclinical and Clinical Cancer Therapeutics

Single-Agent Inhibition of Chk1 Is Antiproliferative in Human Cancer Cell Lines In Vitro and Inhibits Tumor Xenograft Growth In Vivo

K. D. Davies, et al.



American Association for Cancer Research Annual Meeting

Chk1 inhibition and Wee1 inhibition combine synergistically to inhibit cellular proliferation

K. D. Davies, et al.



International Symposium on Targeted Anticancer Therapies

Preclinical characterization of ARRY-575: A potent, selective, and orally bio-available small molecule inhibitor of Chk1

M. J. Humphries, et al.

To view all publications, click here.

These compounds and their uses are investigational and have not been approved by the U.S. Food and Drug Administration. This information is presented only for purposes of providing a general overview of our clinical trials.