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Dayan Elshan, N. G. R.; Wolff, Karen C.; Riva, Laura; Woods, Ashley K.; Grabovyi, Gennadii; Wilson, Katy; Pedroarena, James; Ghorai, Sourav; Nazarian, Armen; Weiss, Frank; Liu, Yuyin; Mazumdar, Wrickban; Song, Lirui; Okwor, Neechi; Malvin, Jacqueline; Bakowski, Malina A.; Beutler, Nathan; Kirkpatrick, Melanie G.; Gebara-Lamb, Amal; Huang, Edward; Nguyen-Tran, Vân T. B.; Chi, Victor; Li, Shuangwei; Rogers, Thomas F.; McNamara, Case W.; Gupta, Anil Kumar; Rahimi, Alireza; Chen, Jian Jeffrey; Joseph, Sean B.; Schultz, Peter G.; Chatterjee, Arnab K.
Journal of medicinal chemistry, 02/2024, Letnik: 67, Številka: 4Journal Article
There remains a need to develop novel SARS-CoV-2 therapeutic options that improve upon existing therapies by an increased robustness of response, fewer safety liabilities, and global-ready accessibility. Functionally critical viral main protease (Mpro, 3CLpro) of SARS-CoV-2 is an attractive target due to its homology within the coronaviral family, and lack thereof toward human proteases. In this disclosure, we outline the advent of a novel SARS-CoV-2 3CLpro inhibitor, CMX990, bearing an unprecedented trifluoromethoxymethyl ketone warhead. Compared with the marketed drug nirmatrelvir (combination with ritonavir = Paxlovid), CMX990 has distinctly differentiated potency (∼5× more potent in primary cells) and human in vitro clearance (>4× better microsomal clearance and >10× better hepatocyte clearance), with good in vitro-to-in vivo correlation. Based on its compelling preclinical profile and projected once or twice a day dosing supporting unboosted oral therapy in humans, CMX990 advanced to a Phase 1 clinical trial as an oral drug candidate for SARS-CoV-2.
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Vir: Osebne bibliografije
in: SICRIS
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