Serum and cellular ribavirin pharmacokinetic and concentration-effect analysis in HCV patients receiving sofosbuvir plus ribavirin

Journal of Antimicrobial Chemotherapy

Volumn 70, Issue 8, 2015, Pages 2322-2329

  Rower, Joseph E ^a   Meissner, Eric G ^b,d   Jimmerson, Leah C ^a   Osinusi, Anu ^b,c   Sims, Zayani ^b   Petersen, Tess ^b   Bushman, Lane R ^a   Wolfe, Pamela ^a   McHutchison, John G ^c   Kottilil, Shyamasundaran ^b   Kiser, Jennifer J ^a  

^a UNIVERSITY OF COLORADO   (United States)

^b NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES   (United States)

^c GILEAD SCIENCES   (United States)

^d MEDICAL UNIVERSITY OF SOUTH CAROLINA   (United States)

Author keywords

Anaemia; Interferon free therapy; Red blood cells; Ribavirin monophosphate; SVR

Indexed keywords

HEMOGLOBIN; RIBAVIRIN; SOFOSBUVIR; ANTIVIRUS AGENT;

ADULT; AGED; ANEMIA; AREA UNDER THE CURVE; ARTICLE; CONCENTRATION AT STEADY-STATE; CONTROLLED STUDY; CORRELATION COEFFICIENT; DRUG BLOOD LEVEL; DRUG DOSE REDUCTION; DRUG HALF LIFE; EVENING DOSAGE; FEMALE; GLOMERULUS FILTRATION RATE; HEPATITIS C; HEPATITIS C VIRUS GENOTYPE 1; HUMAN; LIVER FIBROSIS; MAJOR CLINICAL STUDY; MALE; MORNING DOSAGE; NONHUMAN; OPEN STUDY; PHASE 2 CLINICAL TRIAL; PREDICTIVE VALUE; RANDOMIZED CONTROLLED TRIAL; RECEIVER OPERATING CHARACTERISTIC; SENSITIVITY AND SPECIFICITY; SEX DIFFERENCE; STATISTICAL SIGNIFICANCE; TREATMENT OUTCOME; CHEMICALLY INDUCED; CHEMISTRY; CLASSIFICATION; CLINICAL TRIAL; ERYTHROCYTE; GENETICS; GENOTYPE; HEPACIVIRUS; HEPATITIS C, CHRONIC; ISOLATION AND PURIFICATION; MIDDLE AGED; SERUM; VIROLOGY; VIRUS LOAD;

ADULT; AGED; ANEMIA; ANTIVIRAL AGENTS; ERYTHROCYTES; FEMALE; GENOTYPE; HEPACIVIRUS; HEPATITIS C, CHRONIC; HUMANS; MALE; MIDDLE AGED; RIBAVIRIN; SERUM; SOFOSBUVIR; TREATMENT OUTCOME; VIRAL LOAD;

EID: 84939531387     PISSN: 03057453     EISSN: 14602091     Source Type: Journal    
DOI: 10.1093/jac/dkv122     Document Type: Article

References (35)

1. Brillanti S, Mazzella G, Roda E. Ribavirin for chronic hepatitis C: and the mystery goes on. Dig Liver Dis 2011; 43: 425-30.
2. Page T, Connor JD. The metabolism of ribavirin in erythrocytes and nucleated cells. Int J Biochem 1990; 22: 379-83.
3. Lau JY, Tam RC, Liang TJ et al. Mechanism of action of ribavirin in the combination treatment of chronic HCV infection. Hepatology 2002; 35: 1002-9.
4. Homma M, Matsuzaki Y, Inoue Yet al.Marked elevation of erythrocyte ribavirin levels in interferon and ribavirin-induced anemia. Clin Gastroenterol Hepatol 2004; 2: 337-9.
5. D'Avolio A, De Nicolo A, Simiele M et al. Development and validation of a useful HPLC-UV method for quantification of total and phosphorylatedribavirin in blood and erythrocytes of HCV+ patients. J Pharm Biomed Anal 2012; 66: 376-80.
6. Wu L, Rower J, Burton J et al. Population pharmacokinetic modeling of plasma and intracellular ribavirin concentrations in patients with chronic hepatitis C virus. Antimicrob Agents Chemother 2015; 59: 2179-88.
7. Afdhal N, Reddy KR, Nelson DR et al. Ledipasvir and sofosbuvir for previously treated HCV genotype 1 infection. New Engl J Med 2014; 370: 1483-93.
8. Everson GT, Sims KD, Rodriguez-Torres M et al. Efficacy of an interferonand ribavirin-free regimen of daclatasvir, asunaprevir, and BMS-791325 in treatment-naive patients with HCV genotype 1 infection. Gastroenterology 2014; 146: 420-9.
9. Lawitz E, Sulkowski MS, Ghalib R et al. Simeprevir plus sofosbuvir, with or without ribavirin, to treat chronic infection with hepatitis C virus genotype 1 in non-responders to pegylated interferon and ribavirin and treatmentnaive patients: the COSMOS randomised study. Lancet 2014; 384: 1756-65.
10. Hezode C, Serfaty L, Vierling J et al. Safety and efficacy of the all-oral regimen of MK-5172/MK-8742 plus/minus ribavirin in treatment-naive, non-cirrhotic patients with hepatitis C virus genotype 1 infection: the C-WORTHy study. In: Abstracts of The International Liver Congress 2014, London, UK, 2014. Abstract O10. European Association for the Study of the Liver, Geneva, Switzerland.
11. AASLD/IDSA/IAS-USA. Recommendations for Testing, Managing, and Treating Hepatitis C. http://www.hcvguidelines.org.
12. Poordad F, Hezode C, Trinh R et al. ABT-450/r-ombitasvir and dasabuvir with ribavirin for hepatitis C with cirrhosis. New Engl J Med 2014; 370: 1973-82.
13. Zeuzem S, Jacobson IM, Baykal T et al. Retreatment of HCV with ABT-450/r-ombitasvir and dasabuvir with ribavirin. New Engl J Med 2014; 370: 1604-14.
14. Curry MP, Forns X, Chung RT et al. Sofosbuvir and ribavirin prevent recurrence of HCV infection after liver transplantation: an open-label study. Gastroenterology 2015; 148: 100-7.e1.
15. Osinusi A, Meissner EG, Lee YJ et al. Sofosbuvir and ribavirin for hepatitis C genotype 1 in patients with unfavorable treatment characteristics: a randomized clinical trial. JAMA 2013; 310: 804-11.
16. Jimmerson LC, Ray ML, Bushman LR et al. Measurement of intracellular ribavirin mono-, di-and triphosphate using solid phase extraction and LC-MS/MS detection. J Chromatogr B Analyt Technol Biomed Life Sci 2015; 978-979: 163-72.
17. Thompson AJ, Fellay J, Patel K et al. Variants in the ITPA gene protect against ribavirin-induced hemolytic anemia and decrease the need for ribavirin dose reduction. Gastroenterology 2010; 139: 1181-9.e2.
18. Meissner EG, Bon D, Prokunina-Olsson L et al. IFNL4-DG genotype is associated with slower viral clearance in hepatitis C, genotype-1 patients treated with sofosbuvir and ribavirin. J Infect Dis 2014; 209: 1700-4.
19. Bruchfeld A, Lindahl K, Schvarcz R et al. Dosage of ribavirin in patients with hepatitis C should be based on renal function: a population pharmacokinetic analysis. Ther Drug Monit 2002; 24: 701-8.
20. Kamar N, Chatelut E, Manolis E et al. Ribavirin pharmacokinetics in renal and liver transplant patients: evidence that it depends on renal function. Am J Kidney Dis 2004; 43: 140-6.
21. Wade JR, Snoeck E, Duff F et al. Pharmacokinetics of ribavirin in patients with hepatitis C virus. Br J Clin Pharmacol 2006; 62: 710-4.
22. Levey A, Bosch J, Lewis J et al. A more accurate method to estimate glomerular filtration rate from serum creatinine: a new prediction equation. Modification of Diet in Renal Disease Study Group. Ann Intern Med 1999; 130: 461-70.
23. Preston SL, Drusano GL, Glue P et al. Pharmacokinetics and absolute bioavailability of ribavirin in healthy volunteers as determined by stableisotope methodology. Antimicrob Agents Chemother 1999; 43: 2451-6.
24. Jin R, Fossler MJ, McHutchison JG et al. Population pharmacokinetics and pharmacodynamics of ribavirin in patients with chronic hepatitis C genotype 1 infection. AAPS J 2012; 14: 571-80.
25. Gupta SK, Kantesaria B, Glue P. Pharmacokinetics, safety, and tolerability of ribavirin in hemodialysis-dependent patients. Eur J Clin Pharmacol 2012; 68: 415-8.
26. Jin R, Cai L, Tan M et al. Optimum ribavirin exposure overcomes racial disparity in efficacy of peginterferon and ribavirin treatment for hepatitis C genotype 1. Am J Gastroenterol 2012; 107: 1675-83.
27. Hitomi Y, Cirulli ET, Fellay J et al. Inosine triphosphate protects against ribavirin-induced adenosine triphosphate loss by adenylosuccinate synthase function. Gastroenterology 2011; 140: 1314-21.
28. Fellay J, Thompson AJ, Ge D et al. ITPA gene variants protect against anaemia in patients treated for chronic hepatitis C. Nature 2010; 464: 405-8.
29. D'Avolio A, Ciancio A, Siccardi M et al. Inosine triphosphatase polymorphisms and ribavirin pharmacokinetics as determinants of ribavirin-associate anemia in patients receiving standard anti-HCV treatment. Ther Drug Monit 2012; 34: 165-70.
30. Homma M, Inoue Y, Hasegawa Y et al. Blood ribavirin concentration in high-dose ribavirin for adenovirus-induced haemorrhagic cystitis-a case report. J Clin Pharm Ther 2008; 33: 75-8.
31. Feld JJ, Hoofnagle JH. Mechanism of action of interferon and ribavirin in treatment of hepatitis C. Nature 2005; 436: 967-72.
32. Jensen D, O'Leary J, Pockros P et al. Safety and efficacy of sofosbuvircontaining regimens for hepatitis C: real-world experience in a diverse, longitudinal observational cohort. In: Abstracts of the Liver Meeting, Boston, MA, 2012. Abstract 45. American Association for the Study of Liver Diseases, Alexandria, VA, USA.
33. Gane EJ, Stedman CA, Hyland RH et al. Once daily sofosbuvir (GS-7977) regimens in HCVgenotype 1-3: the ELECTRON trial. In: Abstracts of the Liver Meeting, Boston, MA, 2014. Abstract 229. American Association for the Study of Liver Diseases, Alexandria, VA, USA.
34. Lawitz E, Mangia A, Wyles D et al. Sofosbuvir for previously untreated chronic hepatitis C infection. NewEngl JMed 2013; 368: 1878-87.
35. Jimmerson LC, Zheng JH, Bushman LR et al. Development and validation of a dried blood spot assay for the quantification of ribavirin using liquid chromatography coupled to mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 2014; 944: 18-24.