Ascletis Announces First Patient Dosed in the Phase II Clinical Trial of FASN Inhibitor ASC40 for Treatment of Moderate to Severe Acne

Ascletis Pharma Inc. (HKEX: 1672) today announces the dosing of the first patient in the Phase II clinical trial of ASC40 for moderate to severe acne. ASC40 is an oral, selective inhibitor of fatty acid synthase (FASN), a key enzyme which regulates de novo lipogenesis. Human sebum production requires de novo lipogenesis, which is increased in acne and suppressed by the FASN inhibitor ASC40.

The Phase II trial is a randomized, double-blind, placebo-controlled, multicenter clinical trial in China to evaluate the safety and efficacy of ASC40 for the treatment of patients with moderate to severe acne. About 180 patients will be randomized into three active treatment arms or one placebo control arm at the ratio of 1:1:1:1 and receive ASC40 (25 mg, 50 mg or 75 mg) or matching placebo orally once a day for 12 weeks. The primary outcomes include percentage change of total lesion count at week 12 compared to baseline and ratio of subjects, whose Investigator's Global Assessment (IGA) grades are decreased by ≥2 grades at week 12 compared to baseline.

Acne is the eighth most prevalent disease in the world and affects more than 640 million people globally. The onset of acne often coincides with pubertal hormonal changes, and the condition affects approximately 85% of adolescents and young adults aged 12 to 25 years. However, acne can also persist into or develop during adulthood.

Current first-line treatments for acne include topical creams such as topical retinoids and androgen receptor inhibitor, oral isotretinoin, and antibiotics. A report published by Allied Market Research indicated that the global acne medication market size was US$11.86 billion in 2019, and is projected to reach US$13.35 billion by 2027.

"As a candidate for acne treatment with novel mechanism of action, The dosing of the first patient with ASC40 is the first step for the clinical development in China, and we are looking forward to the trial results," said by Prof. Leihong Xiang, principal investigator of ASC40 Phase II trial for moderate to severe acne vulgaris, chief physician of Dermatological Department, Huashan Hospital, Fudan University, executive deputy director of Institute of Dermatology, Fudan University, deputy director of Dermatology Division of Chinese Medical Doctor Association.

"We have observed that ASC40 inhibited human facial sebum production in the Phase I clinical study. Based on the underlying mechanism of action of ASC40, I am looking forward to the data from this phase II study for the treatment of acne." said Dr. Jinzi J. Wu, Founder, Chairman and CEO of Ascletis.

About Ascletis

Ascletis is an innovative R&D driven biotech listed on the Hong Kong, S.A.R., China 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.