Ascletis Announces the Latest Results of the Preclinical Studies of Two Novel Anti-Cancer Drug Candidates, ASC61 and ASC60, to be presented at AACR Annual Meeting 2022

HANGZHOU, China and SHAOXING, China, March 27, 2022 /PRNewswire/ -- Ascletis Pharma Inc. (HKEX:1672) today announces that the latest preclinical research results of the company's two novel anti-cancer drug candidates, ASC61, an oral PD-L1 inhibitor and ASC60, an oral fatty acid synthase (FASN)  inhibitor have been selected for presentations at the American Association for Cancer Research (AACR) Annual Meeting 2022 (the "2022 AACR Annual Meeting"), and the abstracts have already been published on AACR's official website.

The AACR annual meeting is one of the world's largest and long-standing scientific gatherings in the field of cancer research. Covering some of the most cutting-edge advances in all areas of oncology research and innovation, the annual event attracts tremendous interest from the global cancer research community. The AACR annual meeting for this year will be held in New Orleans, Louisiana on April 8 to 13, 2022 CDT.

The abstracts selected for poster presentations at the 2022 AACR Annual Meeting are as follows:

（1） ASC61

Abstract Title: In vivo efficacy evaluation of ASC61, an oral PD-L1 inhibitor, in two tumor mouse models

• Presentation Type: Poster Presentation
• Abstract Number: 5529
• Session Category: Immunology
• Session Title: Preclinical Immunotherapy
• Presentation time: April 8, 2022, 12:00PM – 1:00 PM CDT
• Presenter/Authors: Jinzi J. Wu, Handan He. Ascletis BioScience Co., Ltd.

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. Preclinical studies showed that ASC61 demonstrated significant antitumor efficacies and were well-tolerated in both syngeneic and humanized tumor mouse models. ASC61 was found to have favorably comparable antitumor activities as the U.S. Food and Drug Administration (FDA) approved PD-L1 therapeutic monoclonal antibody (mAb), Atezolizumab. The Phase I study of ASC61 in advanced solid tumors has received the U.S. IND approval by FDA, and the first patient is planned to be enrolled in the second quarter of 2022.

（2） ASC60

Abstract Title: Efficacy of ASC60, an oral fatty acid synthase inhibitor, in two tumor mouse models

• Presentation Type: Poster Presentation
• Abstract Number: 5466
• Session Category: Experimental and Molecular Therapeutics
• Session Title: Small Molecule Therapeutic Agents
• Presentation time: April 8, 2022, 12:00PM – 1:00 PM CDT
• Presenter/Authors: Jinzi J. Wu, Handan He. Ascletis BioScience Co., Ltd.

ASC60 is a potent, selective and safe oral small molecule inhibitor of FASN. ASC60 can disrupt metabolism and tumor-associated signal transduction in tumor cells through inhibition of de novo lipogenesis (DNL). Preclinical studies showed that ASC60 could suppress tumor growth  and enhance the antitumor activities of mPD-1 antibody in tumor mouse models. The application of the Phase I study of ASC60 in patients with advanced solid tumors has been submitted to the Center for Drug Evaluation (CDE) of the National Medical Products Administration of China (NMPA).

"It is our great pleasure to have the research results of our drug candidates selected by the AACR annual meeting," said Dr. Jinzi J. Wu, Founder, Chairman and CEO of Ascletis. "ASC61, an oral PD-L1 inhibitor, and ASC60, an oral FASN inhibitor, have better patient compliance and are easier to be combined with other oral anti-tumor drugs. These studies deepened our understanding of our drug candidates' mechanism of actions and anti-tumor activities in animal models as well as advanced our clinical development of Company's oncology pipelines. As we are advancing the Phase III clinical trial of ASC40, another FASN inhibitor, in combination with Bevacizumab for the treatment of recurrent glioblastoma (rGBM), we are exploring opportunities for all-oral combinations between ASC61 and ASC40 (or ASC60) as well as other oral anti-tumor drugs from our business partners."

About Ascletis
Ascletis is an innovative R&D driven biotech listed on the Hong Kong Stock Exchange (1672.HK), a global platform covering the entire value chain from discovery and development to manufacturing and commercialization. Ascletis is committed to developing and commercializing innovative drugs in the areas of viral diseases, NASH/PBC, and cancer (oral cancer metabolic checkpoint and immune checkpoint inhibitors) to address unmet medical needs both in China and globally. Led by a management team with deep expertise and a proven track record, Ascletis targets those therapeutic areas with unmet medical needs from a global perspective, and efficiently advances the developments of pipelines with an aim of leading in global competition. To date, Ascletis has three marketed products and 20 robust R&D pipelines of drug candidates with global competitiveness, and is actively exploring new therapeutic areas.

1. Viral Diseases: (1) Hepatitis B Virus (functional cure): focus on breakthrough therapies for CHB functional cure with a subcutaneously-injected PD-L1 antibody – ASC22 and Pegasys^® as cornerstone drugs. (2) COVID-19 pipeline: currently includes (i) ritonavir oral tablet (100 mg), an authorized product, (ii) ASC10, an oral RNA dependent RNA polymerase (RdRp) inhibitor and (iii) ASC11, an oral 3-chymotrypsin like protease (3CLpro) inhibitor. (3) HIV/AIDS: ASC22, an immune therapy to restore HIV-specific immune responses and eventually lead to a functional cure of HIV-infected patients. (4) Hepatitis C: successfully launched an all-oral regimen of combining ASCLEVIR^® and GANOVO^® (RDV/DNV regimen).
2. Non-alcoholic Steatohepatitis/Primary Biliary Cholangitis: Gannex, a wholly-owned company of Ascletis, is dedicated to the R&D and commercialization of new drugs in the field of NASH. Gannex has three clinical stage drug candidates against three different targets – FASN, THRβ and FXR, three fixed-dose combinations for NASH and one PBC program targeting FXR.
3. Cancer (oral cancer metabolic checkpoint and immune checkpoint inhibitors): a pipeline of oral inhibitors targeting FASN, which plays a key role in cancer lipid metabolism, and a pipeline of oral PD-L1 small molecule next generation immune checkpoint inhibitors.
4. Exploratory Indications: Acne: Following NASH and recurrent GBM, the third indication for ASC40 has been approved to enter Phase 2 clinical trial. For more information, please visit www.ascletis.com.

SOURCE Ascletis Pharma Inc.