Announcement of Availability for Darolutamide

December 07, 2020

The Cancer Therapy Evaluation Program (CTEP) is accepting Letters of Intent (LOIs) to conduct clinical studies using darolutamide, a nonsteroidal androgen receptor (AR) antagonist, which is being developed by CTEP as an anticancer agent in collaboration with Bayer. CTEP will also consider requests to supply darolutamide for nonclinical studies. All clinical and nonclinical researchers possessing an interest in working with the agent are welcome to apply. Proposals for clinical trials should be supported by a strong rationale and robust preclinical data (see “Components of a Competitive Letter of Intent” at http://ctep.cancer.gov/protocolDevelopment/lois_concepts.htm).

Darolutamide is a nonsteroidal synthetic compound that binds with high affinity and selectivity to AR (Moilanen et al., 2015. Sci Rep. 5:12007; Fizazi et al. 2013. J Clin Oncol. 31:A65). Darolutamide strongly inhibits androgen-mediated nuclear translocation of AR and is also active against the AR mutants AR(F876L), AR(W742L), and AR(T877A). In preclinical studies, it demonstrates negligible blood-brain barrier penetration (Moilanen et al., 2015. Sci Rep. 5:12007; Zurth et al., 2018. J Clin Oncol. 36:A345). Darolutamide showed significant anti-tumor activity and tumor growth inhibition in AR-overexpressing VCaP prostate cancer cells both in vitro and in castration-resistant VCap murine xenograft model. In July 2019, FDA approved darolutamide (Nubeqa) to treat non-metastatic castration-resistant prostate cancer (nmCRPC) in conjunction with surgical or medical castration based on metastasis free survival (MFS) primary endpoint of the ARAMIS trial (NCT02200614).

All proposals approved by CTEP will be sent to the industry collaborator for a commitment to supply drug for the study.

For more information please see related documents below.