Ascletis Pharma Inc. has revealed that the U.S. Food and Drug Administration (FDA) has approved the investigational new drug (IND) application of ASC11, an oral inhibitor drug candidate targeting 3-chymotrypsin like protease (3CLpro) for Covid-19.
The FDA has approved Ascletis to study the safety, tolerability and pharmacokinetics of ASC11 at various doses in healthy subjects co-dosed with 100 mg ritonavir tablets. Both ASC11 and ritonavir tablets are manufactured by Ascletis.
The phase I clinical trial will consist of three cohorts in healthy subjects, including single- and multiple-dose escalation studies and food effect study. The objective of phase I trial is to find the right dose to move into a pivotal phase II/III in Covid-19 patients.
In antiviral cellular assays with infectious SARS-CoV-2, ASC11 demonstrated much higher potency against SARS-CoV-2 than other 3CLpro inhibitors including Nirmatrelvir, S-217622, PBI-0451 and EDP-235. ASC11 remains potent antiviral activity against various popular Omicron variants such as BA.1 and BA.5. In the animal model with infectious SARS-CoV-2, ASC11 also showed potent antiviral activity.
ASC11 is an in-house discovered oral small molecule drug candidate using various proprietary technologies including molecular docking. Ascletis has filed global patent applications for ASC11 and related compounds and their use in viral disease.
“In addition to safety data, this phase I trial will confirm whether ASC11 needs to be boosted with ritonavir or not,” said Jinzi J. Wu, founder, chairman and CEO of Ascletis,
“We are excited that our proprietary Covid-19 pipeline, including ASC10 (RdRp inhibitor) and ASC11 (3CLpro inhibitor), have all entered into clinical development in the U.S., which marks a great recognition to our in-house R&D capabilities. As Covid-19 pandemic causes persistent huge social and economic implications globally, Ascletis is dedicated to leveraging our global clinical development expertise in viral diseases to fight against the pandemic.”