On January 3, 2022 Ascletis Pharma Inc. (HKEX: 1672) reported the filing of the U.S. Investigational New Drug (IND) application for in-house developed oral PD-L1 small molecule inhibitor, ASC61, for the treatment of advanced solid tumors (Press release, Ascletis, JAN 3, 2022, View Source [SID1234598446]).

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ASC61 is an oral potent and highly selective PD-L1 small molecule inhibitor and blocks PD-1/PD-L1 interaction through inducing PD-L1 dimerization and internalization. As a single agent, ASC61 demonstrated significant antitumor efficacy in multiple animal models such as the humanized mouse model. Preclinical studies showed ASC61 has good safety and pharmacokinetic profiles in animal models. ASC61 oral tablets, which will be used in the clinical trial, were developed with the in-house proprietary technology.

Compared to injectable PD-1/PD-L1 antibodies, ASC61, as an oral PD-L1 inhibitor, has the following benefits: (1) ease of dosing and no need for hospital visits for injections; (2) all-oral combinations with other oral anti-tumor drugs; and (3) rapid titration of doses for better management of immune-related adverse events (irAEs).

"We are excited about filing U.S. IND of ASC61." said Dr. Jinzi J. Wu, Founder, Chairman and CEO of Ascletis. "As we are advancing the phase III clinical trial of ASC40, a fatty acid synthase (FASN) inhibitor, in combination with Bevacizumab for the treatment of recurrent glioblastoma (rGBM), ASC61, as an oral PD-L1 small molecule inhibitor, will further strengthen the Company’s oncology pipeline."