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Page 1
Lenacapavir: A Novel, Potent, and Selective First-in-Class Inhibitor of HIV-1 Capsid Function Exhibits Optimal Pharmacokinetic Properties for a Long-Acting Injectable Antiretroviral Agent.
Subramanian R, Tang J, Zheng J, Lu B, Wang K, Yant SR, Stepan GJ, Mulato A, Yu H, Schroeder S, Shaik N, Singh R, Wolckenhauer S, Chester A, Tse WC, Chiu A, Rhee M, Cihlar T, Rowe W, Smith BJ. Subramanian R, et al. Among authors: stepan gj. Mol Pharm. 2023 Dec 4;20(12):6213-6225. doi: 10.1021/acs.molpharmaceut.3c00626. Epub 2023 Nov 2. Mol Pharm. 2023. PMID: 37917742 Free PMC article.
Preclinical characterization of a non-peptidomimetic HIV protease inhibitor with improved metabolic stability.
Mulato A, Lansdon E, Aoyama R, Voigt J, Lee M, Liclican A, Lee G, Singer E, Stafford B, Gong R, Murray B, Chan J, Lee J, Xu Y, Ahmadyar S, Gonzalez A, Cho A, Stepan GJ, Schmitz U, Schultz B, Marchand B, Brumshtein B, Wang R, Yu H, Cihlar T, Xu L, Yant SR. Mulato A, et al. Among authors: stepan gj. Antimicrob Agents Chemother. 2024 Apr 3;68(4):e0137323. doi: 10.1128/aac.01373-23. Epub 2024 Feb 21. Antimicrob Agents Chemother. 2024. PMID: 38380945 Free PMC article.
Clinical targeting of HIV capsid protein with a long-acting small molecule.
Link JO, Rhee MS, Tse WC, Zheng J, Somoza JR, Rowe W, Begley R, Chiu A, Mulato A, Hansen D, Singer E, Tsai LK, Bam RA, Chou CH, Canales E, Brizgys G, Zhang JR, Li J, Graupe M, Morganelli P, Liu Q, Wu Q, Halcomb RL, Saito RD, Schroeder SD, Lazerwith SE, Bondy S, Jin D, Hung M, Novikov N, Liu X, Villaseñor AG, Cannizzaro CE, Hu EY, Anderson RL, Appleby TC, Lu B, Mwangi J, Liclican A, Niedziela-Majka A, Papalia GA, Wong MH, Leavitt SA, Xu Y, Koditek D, Stepan GJ, Yu H, Pagratis N, Clancy S, Ahmadyar S, Cai TZ, Sellers S, Wolckenhauer SA, Ling J, Callebaut C, Margot N, Ram RR, Liu YP, Hyland R, Sinclair GI, Ruane PJ, Crofoot GE, McDonald CK, Brainard DM, Lad L, Swaminathan S, Sundquist WI, Sakowicz R, Chester AE, Lee WE, Daar ES, Yant SR, Cihlar T. Link JO, et al. Among authors: stepan gj. Nature. 2020 Aug;584(7822):614-618. doi: 10.1038/s41586-020-2443-1. Epub 2020 Jul 1. Nature. 2020. PMID: 32612233 Free PMC article. Clinical Trial.
A highly potent long-acting small-molecule HIV-1 capsid inhibitor with efficacy in a humanized mouse model.
Yant SR, Mulato A, Hansen D, Tse WC, Niedziela-Majka A, Zhang JR, Stepan GJ, Jin D, Wong MH, Perreira JM, Singer E, Papalia GA, Hu EY, Zheng J, Lu B, Schroeder SD, Chou K, Ahmadyar S, Liclican A, Yu H, Novikov N, Paoli E, Gonik D, Ram RR, Hung M, McDougall WM, Brass AL, Sundquist WI, Cihlar T, Link JO. Yant SR, et al. Among authors: stepan gj. Nat Med. 2019 Sep;25(9):1377-1384. doi: 10.1038/s41591-019-0560-x. Epub 2019 Sep 9. Nat Med. 2019. PMID: 31501601 Free PMC article.