Target: Chk-1 | Indication: Solid Tumors

Introduction / Brief Description

GDC-0575 is a highly selective small-molecule Chk-1 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.

Chk-1 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, Chk-1 blocks cell cycle progression in order to allow for repair of damaged DNA, thereby limiting the efficacy of chemotherapeutic agents. Inhibiting Chk-1 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.


GDC-0575 / Cancer


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.

GDC-0575 / Cancer


American Association for Cancer Research Annual Meeting

Chk1 inhibition and Wee1 inhibition combine synergistically to inhibit cellular proliferation

K. D. Davies, et al.

GDC-0575 / Cancer


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.