Safety, pharmacokinetics, and efficacy of (+/-)-β-2′,3′- dideoxy-5-fluoro-3′-thiacytidine with efavirenz and stavudine in antiretroviral-naïve human immunodeficiency virus-infected patients

Antimicrobial Agents and Chemotherapy

Volumn 49, Issue 7, 2005, Pages 2828-2833

  Herzmann, C ^a   Arasteh K ^a   Murphy, R L ^b   Schulbin, H ^a   Kreckel, P ^a   Drauz, D ^a   Schinazi, R F ^c   Beard, A ^d   Cartee, L ^d   Otto, M J ^d  

^a Vivantes Auguste Viktoria Klinikum   (Germany)

^b NORTHWESTERN UNIVERSITY   (United States)

^c EMORY UNIVERSITY SCHOOL OF MEDICINE   (United States)

^d PHARMASSET INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIRETROVIRUS AGENT; EFAVIRENZ; EMTRICITABINE; STAVUDINE;

ADULT; ARTICLE; CLINICAL ARTICLE; COMMON COLD; DIZZINESS; DRUG EFFICACY; DRUG SAFETY; DRUG TOLERABILITY; ENANTIOMER; EYE PAIN; FATIGUE; FEMALE; HEADACHE; HEARTBURN; HIGHLY ACTIVE ANTIRETROVIRAL THERAPY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; MALE; NAUSEA; PLASMA CLEARANCE; PRIORITY JOURNAL; SIDE EFFECT; VIRUS LOAD; VOMITING; WILD TYPE;

ADMINISTRATION, ORAL; ADULT; ANTI-HIV AGENTS; DRUG THERAPY, COMBINATION; HIV INFECTIONS; HIV-1; HUMANS; MIDDLE AGED; OXAZINES; PLASMA; REVERSE TRANSCRIPTASE INHIBITORS; RNA, VIRAL; STAVUDINE; URINE; ZALCITABINE;

EID: 21444447772     PISSN: 00664804     EISSN: None     Source Type: Journal    
DOI: 10.1128/AAC.49.7.2828-2833.2005     Document Type: Article

References (12)

1. Abobo, C. V., L. Ni, R. F. Schinazi, D. C. Liotta, and F. D. Boudinot. 1994. Pharmacokinetics of 2′,3′-dideoxy-5-fluoro-3′- thiacytidine in rats. J. Pharm. Sci. 83:96-99.
2. Chang, C. N., S. L. Doong, J. H. Zhou, J. W. Beach, L. S. Jeong, C. K. Chu, C. H. Tsai, Y. C. Cheng, D. Liotta, and R. Schinazi. 1992. Deoxycytidine deaminase-resistant stereoisomer is the active form of (+/-)-2′,3′- dideoxy-3′-thiacytidine in the inhibition of hepatitis B virus replication. J. Biol. Chem. 267:13938-13942.
3. Cui, L., R. F. Schinazi, G. Gosselin, J. L. Imbach, C. K. Chu, R. F. Rando, G. R. Revankar, and J. P. Sommadossi. 1996. Effect of β-enantiomeric and racemic nucleoside analogues on mitochondrial functions in HepG2 cells. Biochem. Pharmacol. 52:1577-1584.
4. Frick, L. W., L. St. John, L. C. Taylor, G. R. Painter, P. A. Furman, D. C. Liotta, E. S. Furfine, and D. J. Nelson 1993. Pharmacokinetics, oral bioavailability, and metabolic disposition in rats of (-)-cis-5-fluoro-1-[2- (hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine, a nucleoside analog active against human immunodeficiency virus and hepatitis B virus. Antimicrob. Agents Chemother. 37:2285-2292.
5. Furman, P. A., M. Davis, D. C. Liotta, M. Paff, L. W. Frick, D. J. Nelson, R. E. Dornsife, J. A. Wurster, L. J. Wilson, J. A. Fyfe, J. V. Tuttle, W. H. Miller, L. Condreay, D. R. Averett, R. F. Schinazi, and G. R. Painter. 1992. The anti-hepatitis B virus activities, cytotoxicities, and anabolic profiles of the (-) and (+) enantiomers of cis-5-fluoro-1-[2-(hydroxymethyl)-1, 3-oxathiolan-5-yl]cytosine. Antimicrob. Agents Chemother. 36:2686-2692.
6. Mansour, T. S., H. Jin, W. Wang, E. U. Hooker, C. Ashman, N. Cammack, H. Salomon, A. R. Belmonte, and M. A. Wainberg. 1995. Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2′-deoxy-3′-oxa-4′-thiocytidine and their 5-fluoro analogues in vitro. J. Med. Chem. 38:1-4.
7. Schinazi, R. F., A. McMillan, D. Cannon, R. Mathis, R. M. Lloyd, A. Peck, J. P. Sommadossi, M. St. Clair, J. Wilson, P. A. Furman, G. Painter, W.-B. Choi, and D. C. Liotta. 1992. Selective inhibition of human immunodeficiency viruses by racemates and enantiomers of cis-5-fluoro-1-[2-(hydroxymethyl)-1,3- oxathiolan-5-yl]cytosine. Antimicrob. Agents Chemother. 36:2423-2431.
8. Schinazi, R. F., F. D. Boudinot, S. S. Ibrahim, C. Manning, H. M. McClure, and D. C. Liotta. 1992. Pharmacokinetics and metabolism of racemic 2′,3′-dideoxy-5-fluoro-3′-thiacytidine in rhesus monkeys. Antimicrob. Agents Chemother. 36:2432-2438.
9. Schinazi, R. F., R. M. Lloyd, Jr., M. H. Nguyen, D. L. Cannon, A. McMillan, N. Ilksoy, C. K. Chu, D. C. Liotta, H. Z. Bazmi, and J. W. Mellors. 1993. Characterization of human immunodeficiency viruses resistant to oxathiolane-cytosine nucleosides. Antimicrob. Agents Chemother. 37:875-881.
10. Schinazi, R. F., A. McMillan, R. L. Lloyd, Jr., S. Schlueter-Wirtz, D. C. Liotta, and C. K. Chu. 1997. Molecular properties of HIV-1 resistant to (+)-enantiomers and racemates of oxathiolane cytosine nucleosides and their potential for the treatment of HIV and HBV infections. Antivir. Res. 34:A42.
11. Shewach, D. S., D. C. Liotta, and R. F. Schinazi. 1993. Affinity of the antiviral enantiomers of oxathiolane cytosine nucleosides for human 2′-deoxycytidine kinase. Biochem. Pharmacol. 45:1540-1543.
12. Styrt, B. A., T. D. Piazza-Hepp, and G. K. Chikami. 1996. Clinical toxicity of antiretroviral nucleoside analogs. Antivir. Res. 31:121-135.