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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: zheng j. 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.
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: zheng j. 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.
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: zheng j. 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.
Long-acting capsid inhibitor protects macaques from repeat SHIV challenges.
Vidal SJ, Bekerman E, Hansen D, Lu B, Wang K, Mwangi J, Rowe W, Campigotto F, Zheng J, Kato D, Chandrashekar A, Barrett J, Patel S, Wan H, Anioke T, Mercado NB, Nkolola JP, Ferguson MJ, Rinaldi WJ, Callebaut C, Blair W, Cihlar T, Geleziunas R, Yant SR, Barouch DH. Vidal SJ, et al. Among authors: zheng j. Nature. 2022 Jan;601(7894):612-616. doi: 10.1038/s41586-021-04279-4. Epub 2021 Dec 7. Nature. 2022. PMID: 34875675 Free PMC article.
Long-acting lenacapavir protects macaques against intravenous challenge with simian-tropic HIV.
Swanstrom AE, Gorelick RJ, Welker JL, Schmidt F, Lu B, Wang K, Rowe W, Breed MW, Killoran KE, Kramer JA, Donohue D, Roser JD, Bieniasz PD, Hatziioannou T, Pyle C, Thomas JA, Trubey CM, Zheng J, Blair W, Yant SR, Lifson JD, Del Prete GQ. Swanstrom AE, et al. Among authors: zheng j. EBioMedicine. 2023 Sep;95:104764. doi: 10.1016/j.ebiom.2023.104764. Epub 2023 Aug 23. EBioMedicine. 2023. PMID: 37625266 Free PMC article.
Lenacapavir Exhibits Atropisomerism-Mechanistic Pharmacokinetics and Disposition Studies of Lenacapavir Reveal Intestinal Excretion as a Major Clearance Pathway.
Zheng J, Lu B, Carr G, Mwangi J, Wang K, Hao J, Staiger KM, Kozon N, Murray BP, Bashir M, Gohdes MA, Tse WC, Schroeder S, Graupe M, Link JO, Yoon J, Chiu A, Rowe W, Smith BJ, Subramanian R. Zheng J, et al. J Pharmacol Exp Ther. 2024 Sep 18;391(1):91-103. doi: 10.1124/jpet.124.002302. J Pharmacol Exp Ther. 2024. PMID: 39117460
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