Ascletis Announces IND Approval of Oral RdRp Inhibitor ASC10 for COVID-19 by China NMPA

-- Ascletis is China's first biotech company which has obtained IND approvals of an oral RdRp inhibitor from both China NMPA and the U.S. FDA

-- Ascletis has filed multiple patent applications for ASC10 and its use globally. Compared with molnupiravir, ASC10 has a new and differentiated chemical structure

-- ASC10 is an oral double prodrug. After administration, both ASC10 and molnupiravir are rapidly and completely converted in vivo into the same active metabolite ASC10-A.  Ascletis is actively communicating with regulatory authorities to explore the possibility of further accelerating the clinical development of ASC10

HANGZHOU, China and SHAOXING, China, Aug. 21, 2022 /PRNewswire/ -- Ascletis Pharma Inc. (HKEX: 1672, "Ascletis") today announces that the China National Medical Products Administration (NMPA) has approved the Investigational New Drug (IND) application of ASC10, an oral inhibitor drug candidate targeting RNA-dependent RNA polymerase (RdRp) for COVID-19. Ascletis is China's first biotech company which has obtained IND approvals of an oral RdRp inhibitor from both China NMPA and the U.S. Food and Drug Administration (FDA).

ASC10 is an oral double prodrug which has a new and differentiated chemical structure from the single prodrug molnupiravir. After oral administration, both ASC10 and molnupiravir are rapidly and completely converted in vivo into the same active metabolite ASC10-A, also known as β-D-N4-hydroxycytidine (NHC). ASC10 was discovered and developed in-house. Ascletis has filed multiple patent applications for ASC10 and its use globally. ASC10 oral tablet formulation for the clinical study was developed with in-house proprietary technology of Ascletis.

By applying a double prodrug strategy, ASC10's permeability in Caco-2 cells (human colorectal adenocarcinoma cells) and active metabolite exposure in monkeys reached 3.2-fold and 2.1-fold of molnupiravir's, respectively. In the SARS-CoV-2 infected mouse models, ASC10 at 240 mg/kg twice daily led to a 4.0 log reduction in viral titer in lungs, equivalent to molnupiravir at 500 mg/kg twice daily^[1]. Preclinical studies demonstrated that ASC10-A has potent cellular antiviral activity against Omicron variant (EC₅₀ = 0.3 µM), Delta variant (EC₅₀ = 0.5 µM) and wildtype virus (EC₅₀ = 0.7 µM). It also suggested that there were no drug-drug interactions between ASC10 and other common medicines.

Ascletis is actively communicating with regulatory authorities to explore the possibility of further accelerating the clinical development of ASC10.

"The IND approvals of ASC10 from both China NMPA and U.S. FDA mark a great recognition to our in-house R&D capabilities. As the COVID-19 pandemic continues to cause huge social and economic implications globally, we will continue to advance the clinical development of our proprietary COVID-19 pipeline including ASC10 (RdRp inhibitor) and ASC11 (3CLpro inhibitor) to fight against the pandemic." said Dr. Jinzi J. Wu, Founder, Chairman and CEO of Ascletis.

[1] Wahl, et al., Nature. 2021 March ; 591(7850): 451 -457.

About Ascletis
Ascletis is an innovative R&D driven biotech listed on the Hong Kong Stock Exchange (1672.HK), covering the entire value chain from discovery and development to manufacturing and commercialization. Led by a management team with deep expertise and a 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 rapidly advances its drug pipeline with an aim of leading in global competition. To date, Ascletis has three marketed products, i.e. ritonavir tablets, GANOVO^® and ASCLEVIR^®, and 20 drug candidates in its R&D pipeline. The most advanced drug candidates include ASC22 (CHB functional cure), ASC10 and ASC11(oral small molecules for COVID-19 treatment), ASC40 (recurrent glioblastoma), ASC42 (PBC, primary biliary cholangitis), and ASC40 (acne).

For more information, please visit www.ascletis.com.

SOURCE Ascletis Pharma Inc.