Ascletis Pharma Inc. has introduced optimistic topline outcomes from its section I a number of ascending dose (MAD) research in wholesome topics for oral RNA-dependent RNA polymerase (RdRp) inhibitor ASC10 for COVID-19 remedy.
Ascletis’ ASC10 is an progressive orally obtainable double prodrug, which has a brand new and differentiated chemical construction from the only prodrug molnupiravir. After oral dosing, each ASC10 and molnupiravir are quickly and fully transformed in vivo into the identical energetic drug ASC10-A, also referred to as β-D-N4-hydroxycytidine (NHC). Double prodrug method considerably elevated oral bioavailability of energetic drug ASC10-A.
Ascletis section I knowledge
The section I knowledge demonstrated that each one doses of ASC10 together with 800 mg twice every day had been secure and properly tolerated in Chinese language topics. Security profiles between ASC10 and placebo remedies had been comparable. The publicity of energetic drug ASC10-A after twice every day dosing 800 mg double prodrug ASC10 in Chinese language topics was 94% of that after twice every day dosing 800 mg single prodrug molnupiravir in Japanese topics.
The plasma concentrations of the double prodrug ASC10 in Chinese language topics had been beneath detection restrict (0.2 ng/mL) after 800 mg dosing. Equally, the plasma concentrations of the only prodrug molnupiravir in American topics had been negligible after 800 mg dosing.
After physique weight normalization, the exposures of energetic drug ASC10-A are additionally equal between 800 mg double prodrug ASC10 in Chinese language topics and 800 mg single prodrug molnupiravir in American topics.
Meals had no impact on ASC10-A’s publicity, indicating that ASC10 could be taken with or with out meals.
Approvals
Molnupiravir has been authorized or approved to be used in lots of nations together with Japan and the U.S. Ascletis stated current publications present molnupiravir demonstrated thrilling medical efficacy in opposition to omicron infections in Chinese language sufferers.
Based mostly on the corporate’s section I outcomes of ASC10 and molnupiravir’s medical efficacy knowledge in American, Japanese and Chinese language sufferers, 800 mg twice every day has been chosen for the registrational trial.
The energetic drug ASC10-A has potent antiviral exercise in opposition to varied Omicron variants reminiscent of BA.5 and BA.2.75. Ascletis has filed a number of patent functions for ASC10 and its use globally.
“Based mostly on Part I outcomes, ASC10 may be very secure in Chinese language topics and its druggability is excessive. I consider ASC10 has potential to play an essential function in combating in opposition to COVID-19 pandemic,” stated Yunqing Qiu, vp of the First Affiliated Hospital, College of Drugs, Zhejiang College and principal investigator of ASC10 section I research.
“The section I medical knowledge have confirmed the druggability of ASC10 for COVID-19. With the worldwide patent filings, we anticipate that ASC10 will make a contribution to combating in opposition to COVID-19 pandemic inside and outdoors China,” stated Jinzi J. Wu, founder, chairman and CEO of Ascletis.
