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An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19.
Owen DR, Allerton CMN, Anderson AS, Aschenbrenner L, Avery M, Berritt S, Boras B, Cardin RD, Carlo A, Coffman KJ, Dantonio A, Di L, Eng H, Ferre R, Gajiwala KS, Gibson SA, Greasley SE, Hurst BL, Kadar EP, Kalgutkar AS, Lee JC, Lee J, Liu W, Mason SW, Noell S, Novak JJ, Obach RS, Ogilvie K, Patel NC, Pettersson M, Rai DK, Reese MR, Sammons MF, Sathish JG, Singh RSP, Steppan CM, Stewart AE, Tuttle JB, Updyke L, Verhoest PR, Wei L, Yang Q, Zhu Y. Owen DR, et al. Among authors: novak jj. Science. 2021 Dec 24;374(6575):1586-1593. doi: 10.1126/science.abl4784. Epub 2021 Nov 2. Science. 2021. PMID: 34726479 Free article.
Mechanistic insights on clearance and inhibition discordance between liver microsomes and hepatocytes when clearance in liver microsomes is higher than in hepatocytes.
Keefer C, Chang G, Carlo A, Novak JJ, Banker M, Carey J, Cianfrogna J, Eng H, Jagla C, Johnson N, Jones R, Jordan S, Lazzaro S, Liu J, Scott Obach R, Riccardi K, Tess D, Umland J, Racich J, Varma M, Visswanathan R, Di L. Keefer C, et al. Among authors: novak jj. Eur J Pharm Sci. 2020 Dec 1;155:105541. doi: 10.1016/j.ejps.2020.105541. Epub 2020 Sep 12. Eur J Pharm Sci. 2020. PMID: 32927071
Evaluation of Fraction Unbound Across 7 Tissues of 5 Species.
Ryu S, Tess D, Chang G, Keefer C, Burchett W, Steeno GS, Novak JJ, Patel R, Atkinson K, Riccardi K, Di L. Ryu S, et al. Among authors: novak jj. J Pharm Sci. 2020 Feb;109(2):1178-1190. doi: 10.1016/j.xphs.2019.10.060. Epub 2019 Nov 5. J Pharm Sci. 2020. PMID: 31704191
Quantitative Characterization of Major Hepatic UDP-Glucuronosyltransferase Enzymes in Human Liver Microsomes: Comparison of Two Proteomic Methods and Correlation with Catalytic Activity.
Achour B, Dantonio A, Niosi M, Novak JJ, Fallon JK, Barber J, Smith PC, Rostami-Hodjegan A, Goosen TC. Achour B, et al. Among authors: novak jj. Drug Metab Dispos. 2017 Oct;45(10):1102-1112. doi: 10.1124/dmd.117.076703. Epub 2017 Aug 2. Drug Metab Dispos. 2017. PMID: 28768682
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