The effect of ravuconazole on the pharmacokinetics of nelfinavir in healthy male volunteers

Journal of Clinical Pharmacology

Volumn 46, Issue 2, 2006, Pages 193-200

  Yan, Jing He ^a,d   Marino, Maria R ^a   Smith, Robert A ^a   Kanamaluru, Vanaja ^a,b   O'Mara, Edward M ^a,c   Grasela, Dennis M ^a  

^a BRISTOL MYERS SQUIBB PHARMACEUTICAL RESEARCH INSTITUTE   (United States)

^b Global Health Outcomes and Market Access   (United States)

^c HOFFMANN LA ROCHE INC   (United States)

^d BRISTOL MYERS SQUIBB   (United States)

Author keywords

Nelfinavir; Pharmacokinetics; Ravuconazole

Indexed keywords

ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; ANTIFUNGAL AGENT; CYTOCHROME P450 3A; NELFINAVIR; PROTEINASE INHIBITOR; RAVUCONAZOLE; TRIAZOLE DERIVATIVE;

ABDOMINAL PAIN; ACCIDENTAL INJURY; ADULT; ANTIFUNGAL ACTIVITY; AREA UNDER THE CURVE; ARTICLE; DIARRHEA; DOSE TIME EFFECT RELATION; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG HALF LIFE; DRUG METABOLISM; DRUG SAFETY; ENZYME INHIBITION; ERYTHEMA; EYE PAIN; HEADACHE; HERPES SIMPLEX; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; MALE; MYASTHENIA; NORMAL HUMAN; OPEN STUDY; PHARYNGITIS; RHINITIS; SIDE EFFECT; SWEATING;

ADOLESCENT; ADULT; ANTI-HIV AGENTS; AREA UNDER CURVE; CYTOCHROME P-450 CYP3A; DRUG INTERACTIONS; HALF-LIFE; HUMANS; MALE; MIDDLE AGED; NELFINAVIR; THIAZOLES; TRIAZOLES;

EID: 31344474550     PISSN: 00912700     EISSN: 15524604     Source Type: Journal    
DOI: 10.1177/0091270005283462     Document Type: Article

References (35)

1. Hata K, Kimura J, Miki H. In vitro and in vivo antifungal activities of ER-30346, a novel oral triazole with a broad antifungal spectrum. Antimicrob Agents Chemother. 1996;40:2237-2242.
2. National Committee for Clinical Laboratory Standards. Reference Method for Broth Dilution Antifungal Susceptibility Testing for Yeasts: Proposed Standard. NCCLS Document M27-P. Wayne, Pa: National Committee for Clinical Laboratory Standards; 1992.
3. Hata K, Kimura J, Miki H. Efficacy of ER-30346, a novel triazole antifungal agent in experimental models of aspergillosis, candidiasis and cryptococcosis. Antimicrob Agents Chemother. 1996;40:2243-2247.
4. Fung-Tomc JC, Minassian B, Huczko E. In vitro antifungal and fungicidal spectra of a new pradimicin derivative, BMS-181184. Antimicrob Agents Chemother. 1995;30:295-300.
5. Fung-Tomc JC, Huczko E, Minassian B, Bonner DP. In vitro activity of a new oral triazol, BMS-207147 (ER-30346). Antimicrob Agents Chemother. 1998;42:313-318.
6. Pfaller MA, Messer SA, Hollis RJ, et al. In vitro susceptibilities of Candida bloodstream isolates to the new triazole antifungal agents BMS-207147, Sch 56592, and voriconazole. Antimicrob Agents Chemother. 1998;42:3242-3244.
7. Diekema DJ, Pfaller MA, Messer SA, et al. In vitro activities of BMS-207147 against over 600 contemporary clinical bloodstream isolates of Candida species from the SENTRY Antimicrobial Surveillance Program in North America and Latin America. Antimicrob Agents Chemother. 1999;43:2236-2239.
8. Yamazumi T, Pfaller MA, Messer SA, Houston A, Hollis RJ, Jones RN. In vitro activities of ravuconazole (BMS-207147) against 541 clinical isolates of Cryptococcus neoformans. Antimicrob Agents Chemother. 2000;44:2883-2886.
9. Pfaller MA, Messer SA, Hollis RJ, Jones RN, Diekema DJ. In vitro activities of ravuconazole and voriconazole compared with those of four approved systemic antifungal agents against 6,970 clinical isolates of Candida spp. Antimicrob Agents Chemother. 2002;46:1723-1727.
10. Laverdiere M, Hoban D, Restieri C, Habel F. In vitro activity of three new triazoles and one echinocandin against Candida bloodstream isolates from cancer patients. J Antimicrob Chemother. 2002;50:119-123.
11. Diekema DJ, Messer SA, Hollis RJ, Jones RN, Pfaller MA. Activities of caspofungin, itraconazole, posaconazole, ravuconazole, voriconazole, and amphotericin B against 448 recent clinical isolates of filamentous fungi. J Clin Microbiol. 2003;41:3623-3626.
12. Pfaller MA, Diekema DJ, Messer SA, Boyken L, Hollis RJ, Jones RN. In vitro susceptibilities of rare Candida bloodstream isolates to ravuconazole and three comparative antifungal agents. Diagn Microbiol Infect Dis. 2004;48:101-105.
13. Gupta AK, Kohli Y, Batra R. In vitro activities of posaconazole, ravuconazole, terbinafine, itraconazole and fluconazole against dermatophyte, yeast and non-dermatophyte species. Med Mycol. 2005;43:179-185.
14. Olsen SJ, Mummaneni V, Rolan P, Norton J, Grasela DM. Ravuconazole single ascending oral dose study in healthy subjects. Presented at: 40th Interscience Conference on Antimicrobial Agents and Chemotherapy; September 17-20, 2000; Toronto, Ontario, Canada. Abstract 838.
15. Grasela DM, Olsen SJ, Mummaneni V, et al. Ravuconazole: multiple ascending oral dose study in healthy subjects. Presented at: 40th Interscience Conference on Antimicrobial Agents and Chemotherapy; September 17-20, 2000; Toronto, Ontario, Canada. Abstract 839.
16. Fortovase (saquinavir) [package insert]. Montvale, NJ: Medical Economics Company; 2001.
17. Piscitelli SC, Flexner C, Minor JR, Polis MA, Masus H. Drug interactions in patients infected with human immunodeficiency virus. Clin Infect Dis. 1996;23:685-693.
18. Moyle G. Saquinavir: a review of its development, pharmacological properties and clinical use. Exp Opin Invest Drugs. 1996;5:166-167.
19. Crixivan (indinavir sulfate) [package insert]. Montvale, NJ: Medical Economics Company; 2001.
20. Kakuda TN, Struble KA, Piscitelli SC. Protease inhibitors for the treatment of human immunodeficiency virus infection. Am J Health-System Pharm. 1998;55:233-254.
21. Reyataz (atazanavir sulfate) [package insert]. Montvale, NJ: Medical Economics Company; 2004.
22. Kerr BM, Yuen GJ, Sandoval T, Wu E, Shetty BV, Anderson R. The pharmacokinetics of nelfinavir administered alone and with ketoconazole in healthy volunteers [abstract]. Presented at: 98th Annual Meeting of the American Society for Clinical Pharmacology and Therapeutics; March 5-8, 1997; San Diego, Calif. Clin Pharmacol Ther. 1997;61:147.
23. Regazzi M, Maserati R, Villani P, et al. Clinical pharmacokinetics of nelfinavir and its metabolite M8 in human immunodeficiency virus (HIV)-positive and HIV-hepatitis C virus-coinfected subjects. Antimicrob Agents Chemother. 2005;49:643-649.
24. Tseng AL, Foisy MM. Management of drug interactions in patients with HIV. Ann Pharmacother. 1997;31:1040-1058.
25. Mummaneni V, Geraldes M, Hadjilambris OW, Ouyang Z, Uderman H, Marino MR. Effect of ravuconazole on the pharmacokinetics of simvastatin in healthy subjects. Presented at: 40th Interscience Conference on Antimicrobial Agents and Chemotherapy; September 17-20, 2000; Toronto, Ontario, Canada. Abstract 841.
26. Neuvonen PJ, Kantola T, Kivisto KT. Simvastatin but not pravastatin is very susceptible to interaction with CYP3A4 inhibitor itraconazole. Clin Pharmacol Ther. 1998;63:332-341.
27. Gibaldi M. Non-compartmental analysis based on statistical moment theory. In: Gibaldi M, Perrier D, eds. Pharmacokinetics. 2nd ed. New York, NY: Marcel Dekker; 1982:409-418.
28. Riegelman S. The application of statistical moment theory to the evaluation of in vivo dissolution time and absorption time. J Pharmacokinet Biopharm. 1980;8:509-534.
29. Statistical Analysis Systems (SAS) [computer program]. Version 6.12. Cary, NC: SAS Institute Inc; 1997.
30. Viracept (nelfinavir mesylate) [package insert]. Montvale, NJ: Medical Economics Company; 2001.
31. Wang JS, Wen X, Backman JT, Taavitsainen P, Neuvonen PJ, Kivisto KT. Midazolam alpha-hydroxylation by human liver microsomes in vitro: inhibition by calcium channel blockers, itraconazole and ketoconazole. Pharmacol Toxicol. 1995;85:157-161.
32. Von Moltke LL, Greenblatt DJ, Schmider J, et al. Midazolam hydroxylation by human liver microsomes in vitro: inhibition by fluoxetine, norfluoxetine, and by azole antifungal agents. J Clin Pharm. 1996;36:783-791.
33. Venkatakrishnan K, von Moltke LL, Greenblatt DJ. Effects of antifungal agents on oxidative drug metabolism: clinical relevance. Clin Pharmacokinet. 2000;38:111-180.
34. Tebas P, Powderly WG. Nelfinavir mesylate. Expert Opin Pharmacother. 2000;1:1429-1440.
35. Bardsley-Elliot A, Plosker GL. Nelfinavir: an update on its use in HIV infection. Drugs. 2000;59:581-620.