Ascletis Announces First Patient Dose in U.S. Phase I Clinical Trial of Oral Small Molecule PD-L1 Inhibitor Prodrug ASC61 for the Treatment of Advanced Solid Tumors

–ASC61 is an in-house developed oral small molecule PD-L1 inhibitor prodrug that has shown significant antitumor efficacy in preclinical studies as a single agent in multiple animal models

–ASC61-A treatment induces IFNγ secretion in a concentration-dependent manner with CE50 of 2.86 nM. Peak levels of IFNγ induced by ASC61-A were similar to those induced by Keytruda

–The U.S. Phase I clinical trial of ASC61 is being conducted by Nebraska Cancer Specialists and California Cancer Centers and is expected to be completed by March 2023

HANGZHOU and SHAOXING, China, August 7, 2022 /PRNewswire/ — Ascletis Pharma Inc. (HKEX: 1672, “Ascletis”) today announces the completion of first patient administration in the U.S. Phase I clinical trial of ASC61 , an oral small molecule PD-L1 inhibitor prodrug, for the treatment of solid tumors.

This Phase I trial in the United States is a dose-escalation study to assess the safety and tolerability of ASC61 as well as to define the maximum tolerated dose (MTD) and the recommended phase 2 dose (RP2D) of ASC61 in patients with advanced solid tumors who have disease progression during or after standard therapy.

ASC61 is an oral small molecule inhibitory prodrug. Its active metabolite, ASC61-A, is a potent and highly selective inhibitor that blocks the PD-1/PD-L1 interaction by inducing the dimerization and internalization of PD-L1. As a single agent, ASC61 demonstrated significant antitumor efficacy in several animal models, including a humanized mouse model. Preclinical studies have shown that ASC61 exhibits good safety and pharmacokinetic profiles in animal models. The ASC61 oral tablets used in the clinical trial were developed with proprietary Ascletis technology.

In a direct comparison study using human PD-L1-expressing cells and the fresh peripheral blood mononuclear cell (PBMC) co-culture assay, ASC61-A treatment induced IFNγ secretion in a cell-dependent manner. concentration, with an EC50 of 2.86 nM. Peak levels of IFNγ induced by ASC61-A were similar to those induced by Keytruda.

Compared to PD-1/PD-L1 antibody injections, the oral PD-L1 inhibitor ASC61 has the following advantages: (1) greater patient compliance with easy and safe administration without the need for hospital visits for injections; (2) the ease of all oral therapeutic combinations with other oral antitumor drugs; (3) easier to manage immune system-related adverse events (IRAEs) with dose adjustment; (4) relatively lower cost; and (5) greater permeability to distribute to targeted tissues.

“Immunogenicity and low permeability of tumor tissues are the main disadvantages of therapeutic antibodies, which can lead to low PD-1/PD-L1 antibody response rate. As a highly differentiated small molecule PD-L1 inhibitor , ASC61 has several advantages over antibodies, and has shown a promising preliminary efficacy and safety profile in preclinical studies. These advances of ASC61 on advanced solid tumors have further demonstrated the ability and execution Ascletis’ global R&D efforts.We plan to advance studies of ASC61 to provide more options for patients with advanced solid tumors.” says dr. Jinzi J. WuFounder, Chairman and CEO of Ascletis.

About Ascletis

Ascletis is an innovative, R&D-driven biotech company listed on the Hong Kong Stock Exchange (1672.HK), spanning the entire value chain from discovery and development to manufacturing and commercialization. Led by a management team with deep expertise and proven track record, Ascletis focuses on three therapeutic areas with unmet medical needs from a global perspective: viral diseases, non-alcoholic steatohepatitis (NASH ) and oncology. Through excellent execution, Ascletis is rapidly advancing its drug pipeline with the aim of dominating the global competition. To date, Ascletis markets three products, namely ritonavir tablets, GANOVO® and ASCLEVIR®, and 20 drug candidates in its R&D pipeline. The most advanced drug candidates include ASC22 (functional HBV cure), ASC10 and ASC11 (oral small molecules for the treatment of COVID-19), ASC40 (recurrent glioblastoma), ASC42 (PBC, primary biliary cholangitis) and ASC40 (acne ).

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SOURCEAscletis Pharma Inc.

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