8238. Ritonavir

Nomenclature

CAS number: 155213-67-5
(5S,8S,10S,11S)-10-Hydroxy-2-methyl-5-(1-methylethyl)-1-[2-(1-methylethyl)-4-thiazolyl]-3,6-dioxo-8,11-bis(phenylmethyl)-2,4,7,12-tetraazatridecan-13-oic acid 5-thiazolylmethyl ester; (2S,3S,5S)-5-[N-[N-[[N-methyl-N-[(2-isopropyl-4-thiazolyl)methyl]amino]carbonyl]valinyl]amino]-2-[N-[(5-thiazolyl)methoxycarbonyl]amino]-1,6-diphenyl-3-hydroxyhexane; A-84538; Abbott 84538; ABT-538; Norvir (Abbott).
C37H48N6O5S2; mol wt 720.94.
C 61.64%, H 6.71%, N 11.66%, O 11.10%, S 8.90%.

Description and references

Peptidomimetic HIV-1 protease inhibitor. Prepn: D. J. Kempf et al., WO 9414436; eidem, US 5541206 (1994, 1996 both to Abbott). Antiretroviral spectrum, pharmacokinetics: idem et al., Proc. Natl. Acad. Sci. USA 92, 2484 (1995). Structural model for drug resistance: M. Markowitz et al., J. Virol. 69, 701 (1995). HPLC determn in biological fluids: R. M. W. Hoetelmans et al., J. Chromatogr. B 705, 119 (1998). Review of clinical experience: A. P. Lea, D. Faulds, Drugs 52, 541-546 (1996). Clinical trial with nucleoside analogs in HIV-infected children: S. A. Nachman et al., J. Am. Med. Assoc. 283, 492 (2000). Clinical trial with lopinavir, q.v., in HIV infection: S. Walmsley et al., N. Engl. J. Med. 346, 2039 (2002).

Chemical structure

Therapeutic Category

Antiretroviral.

Keywords

HIV Protease Inhibitor; Antiretroviral; Protease Inhibitors