China-based Ascletis Pharma Inc., (HKG: 1672) announced the positive topline results from its Phase I multiple ascending dose (MAD) study (NCT05523141) in healthy subjects for the oral RNA-dependent RNA polymerase (RdRp) inhibitor ASC10 being developed as treatment for COVID-19. The Phase I data demonstrated that all doses of ASC10, including 800 mg twice daily, were safe and well-tolerated in Chinese subjects. Safety profiles between ASC10 and placebo treatments were comparable.
ASC10: Innovative Double Prodrug
ASC10 is an innovative orally available double prodrug, which has a new and differentiated chemical structure from the single prodrug molnupiravir. After oral dosing, both ASC10 and molnupiravir are rapidly and completely converted in vivo into the same active drug ASC10-A, also known as β-D-N4-hydroxycytidine (NHC). The double prodrug approach significantly increased the oral bioavailability of the active drug ASC10-A.
Clinical Trial Results
The exposure of the active drug ASC10-A after twice daily dosing of 800 mg of the double prodrug ASC10 in Chinese subjects was 94% of that after twice daily dosing of 800 mg of the single prodrug molnupiravir in Japanese subjects. After body weight normalization, the exposures of active drug ASC10-A are also equivalent between 800 mg double prodrug ASC10 in Chinese subjects and 800 mg single prodrug molnupiravir in American subjects. The food had no effect on ASC10-A’s exposure, indicating that ASC10 can be taken with or without food.
Global Patent Filings and Clinical Trials
Ascletis has filed multiple patent applications for ASC10 and its use globally, alongside a clinical trial filing in the US for the treatment of monkeypox in October this year.-Fineline Info & Tech
