Effect of cobicistat on glomerular filtration rate in subjects with normal and impaired renal function

Journal of Acquired Immune Deficiency Syndromes

Volumn 61, Issue 1, 2012, Pages 32-40

  German, Polina ^a   Liu, Hui C ^a   Szwarcberg, Javier ^a   Hepner, Mischa ^a   Andrews, Jessica ^a   Kearney, Brian P ^a   Mathias, Anita ^a  

^a GILEAD SCIENCES   (United States)

Author keywords

COBI; GFR; iohexol; renal dysfunction; transporters

Indexed keywords

AMYLASE; ATAZANAVIR; COBICISTAT; CREATININE; DARUNAVIR; ELVITEGRAVIR; IOHEXOL; RITONAVIR; TRIACYLGLYCEROL LIPASE;

ABDOMINAL DISTENSION; ADULT; AGED; AMYLASE BLOOD LEVEL; ARTICLE; ASTHENIA; CLINICAL ARTICLE; COHORT ANALYSIS; CONTROLLED STUDY; CREATININE BLOOD LEVEL; DIARRHEA; DISEASE SEVERITY; DOUBLE BLIND PROCEDURE; DRUG EFFECT; DRUG ELIMINATION; FEMALE; GLOMERULUS FILTRATION RATE; GLUCOSURIA; HEADACHE; HUMAN; KIDNEY DYSFUNCTION; KIDNEY FUNCTION; KIDNEY TUBULE FUNCTION; MALE; NAUSEA; NUTRITIONAL INTOLERANCE; PHASE 3 CLINICAL TRIAL; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SIDE EFFECT; TREATMENT DURATION; TRIACYLGLYCEROL LIPASE BLOOD LEVEL;

ADULT; CARBAMATES; COHORT STUDIES; CREATININE; CYTOCHROME P-450 CYP3A; ENZYME INHIBITORS; FEMALE; GLOMERULAR FILTRATION RATE; HUMANS; KIDNEY; MALE; METABOLIC CLEARANCE RATE; PLACEBOS; THIAZOLES;

EID: 84865714929     PISSN: 15254135     EISSN: 10779450     Source Type: Journal    
DOI: 10.1097/QAI.0b013e3182645648     Document Type: Article

References (52)

1. Stevens LA, Coresh J, Greene T, et al. Assessing kidney function-measured and estimated glomerular filtration rate. N Engl J Med. 2006; 354:2473-2483.
2. Luke DR, Halstenson CE, Opsahl JA, et al. Validity of creatinine clearance estimates in the assessment of renal function. Clin Pharmacol Ther. 1990;48:503-508.
3. Tett SE, Kirkpatrick CM, Gross AS, et al. Principles and clinical application of assessing alterations in renal elimination pathways. Clin Pharmacokinet. 2003;42:1193-1211.
4. Perrone RD, Madias NE, Levey AS. Serum creatinine as an index of renal function: new insights into old concepts. Clin Chem. 1992;38: 1933-1953.
5. Brater DC. Measurement of renal function during drug development. Br J Clin Pharmacol. 2002;54:87-95.
6. Shannon JA. The renal excretion of creatinine in man. J Clin Invest. 1935;14:403-410.
7. Levey AS. Measurement of renal function in chronic renal disease. Kidney Int. 1990;38:167-184.
8. Berglund F, Killander J, Pompeius R. Effect of trimethoprim- sulfamethoxazole on the renal excretion of creatinine in man. J Urol. 1975;114: 802-808.
9. Burgess E, Blair A, Krichman K, et al. Inhibition of renal creatinine secretion by cimetidine in humans. Ren Physiol. 1982;5:27-30.
10. Opravil M, Keusch G, Luthy R. Pyrimethamine inhibits renal secretion of creatinine. Antimicrob Agents Chemother. 1993;37:1056-1060.
11. RANEXA-(ranolazine) extended-release tablets. US Prescribing Information. Foster City, CA: Gilead Sciences, Inc. Revised July 2011.
12. Min S, Carrod A, Curtis L, et al. Safety profile of dolutegravir (DTG, S/GSK1349572), in combination with other antiretrovirals in antiretroviral (ART)-naïve and ART-experienced adults from two phase IIb studies [poster exhibition TUPE238]. Presented at: the 6th IAS Conference on HIV Pathogenesis, Treatment and Prevention; July 17-20, 2011; Rome, Italy.
13. Center for Drug Evaluation and Research. Application number: 202022Orig1s000-Rilpivirine: cross-discipline team leader review. 2011:1-23.
14. Andreev E, Koopman M, Arisz L. A rise in plasma creatinine that is not a sign of renal failure: which drugs can be responsible? J Intern Med. 1999;246:247-252.
15. Ixkes MC, Koopman MG, van Acker BA, et al. Cimetidine improves GFR-estimation by the Cockcroft and Gault formula. Clin Nephrol. 1997;47:229-236.
16. Kabat-Koperska J, Safranow K, Golembiewska E, et al. Creatinine clearance after cimetidine administration: is it useful in the monitoring of the function of transplanted kidney? Ren Fail. 2007;29:667-672.
17. Kemperman FA, Silberbusch J, Slaats EH, et al. Estimation of the glomerular filtration rate in NIDDM patients from plasma creatinine concentration after cimetidine administration. Diabetes Care. 1998;21:216-220.
18. Gilead Sciences Inc. Gilead's second pivotal phase 3 clinical study of the investigational antiretroviral Quad regimen meets 48-week primary objective. Foster City, CA. September 19, 2011.
19. Gilead Sciences, Inc. Gilead's boosting agent, cobicistat, meets 48-week primary objective in pivotal phase 3 study. Foster City, CA, December 5, 2011 (Press Release).
20. Cohen C, Elion R, Ruane P, et al. Randomized, phase 2 evaluation of two single-tablet regimens elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate versus efavirenz/emtricitabine/tenofovir disoproxil fumarate for the initial treatment of HIV infection. AIDS. 2011;25:F7-F12.
21. Elion R, Cohen C, Gathe J, et al. Phase 2 study of cobicistat versus ritonavir each with once-daily atazanavir and fixed-dose emtricitabine/tenofovir df in the initial treatment of HIV infection. AIDS. 2011;25: 1881-1886.
22. K/DOQI clinical practice guidelines for chronic kidney disease: evaluation, classification, and stratification. AmJ Kidney Dis. 2002;39:S1-S266. Available at: http://www.kidney.org/professionals/kdoqi/guidelines-ckd/toc.htm. Accessed May 22, 2012.
23. OMNIPAQUE (iohexol) injection. US Prescribing Information. Princeton, NJ. GE Healthcare, Inc; 2008.
24. Stevens LA, Levey AS. Measured GFR as a confirmatory test for estimated GFR. J Am Soc Nephrol. 2009;20:2305-2313.
25. Lindblad HG, Berg UB. Comparative evaluation of iohexol and inulin clearance for glomerular filtration rate determinations. Acta Paediatr. 1994;83:418-422.
26. Lundqvist S, Hietala SO, Karp K. Experimental studies comparing iohexol and 51Cr-EDTA for glomerular filtration rate measurements. Acta Radiol. 1995;36:58-63.
27. Brown SC, O'Reilly PH. Iohexol clearance for the determination of glomerular filtration rate in clinical practice: evidence for a new gold standard. J Urol. 1991;146:675-679.
28. Division of AIDS (DAIDS) Table of Grading Severity of Adult and Pediatric Adverse Events. 2004. Available at: http://www.niaid.nih.gov/LabsAndResources/ resources/DAIDSClinRsrch/Documents/daidsaegradingtable.pdf. Accessed April 29, 2010.
29. German P, Warren D, West S, et al. Pharmacokinetics and bioavailability of an integrase and novel pharmacoenhancer-containing single-tablet fixed-dose combination regimen for the treatment of HIV. J Acquir Immune Defic Syndr. 2010;55:323-329.
30. Mathias A, Murray BP, Iwata Q, et al. Metabolism and excretion in humans of the pharmacoenhancer GS-9350 [oral presentation/powerpoint]. Presented at: International Workshop on Clinical Pharmacology of HIV Therapy; April 7-9, 2010; Sorrento, Italy.
31. German P, Wei X, Mizuno V, et al. Pharmacokinetics of elvitegravir and cobicistat in subjects with severe renal impairment [poster P38]. Presented at: 13th International Workshop on Clinical Pharmacology of HIV Therapy; April 16-18, 2012; Barcelona, Spain.
32. Walser M. Assessing renal function from creatinine measurements in adults with chronic renal failure. Am J Kidney Dis. 1998;32:23-31.
33. Masereeuw R, Russel FG. Therapeutic implications of renal anionic drug transporters. Pharmacol Ther. 2010;126:200-216.
34. Wright SH. Role of organic cation transporters in the renal handling of therapeutic agents and xenobiotics. Toxicol Appl Pharmacol. 2005;204: 309-319.
35. Koepsell H, Lips K, Volk C. Polyspecific organic cation transporters: structure, function, physiological roles, and biopharmaceutical implications. Pharm Res. 2007;24:1227-1251.
36. Berkhin EB, Humphreys MH. Regulation of renal tubular secretion of organic compounds. Kidney Int. 2001;59:17-30.
37. Bonate PL, Reith K, Weir S. Drug interactions at the renal level. Implications for drug development. Clin Pharmacokinet. 1998;34: 375-404.
38. Lepist EI, Ray AS. Renal drug-drug interactions: what we have learned and where we are going. Expert Opin Drug Metab Toxicol. 2012;8:433-448.
39. Kremer JM, Hamilton RA. The effects of nonsteroidal antiinflammatory drugs on methotrexate (MTX) pharmacokinetics: impairment of renal clearance of MTX at weekly maintenance doses but not at 7.5 mg. J Rheumatol. 1995;22:2072-2077.
40. Abel S, Nichols DJ, Brearley CJ, et al. Effect of cimetidine and ranitidine on pharmacokinetics and pharmacodynamics of a single dose of dofetilide. Br J Clin Pharmacol. 2000;49:64-71.
41. Kosoglou T, Rocci ML Jr, Vlasses PH. Trimethoprim alters the disposition of procainamide and N-acetylprocainamide. Clin Pharmacol Ther. 1988;44:467-477.
42. +)-organic cation antiporters. Biochem Pharmacol. 2007;74:359-371.
43. Urakami Y, Kimura N, Okuda M, et al. Creatinine transport by basolateral organic cation transporter hOCT2 in the human kidney. Pharm Res. 2004;21:976-981.
44. Okuda M, Kimura N, Inui K. Interactions of fluoroquinolone antibacterials, DX-619 and levofloxacin, with creatinine transport by renal organic cation transporter hOCT2. Drug Metab Pharmacokinet. 2006; 21:432-436.
45. Imamura Y,Murayama N, Okudaira N, et al. Prediction of fluoroquinoloneinduced elevation in serum creatinine levels: a case of drug-endogenous substance interaction involving the inhibition of renal secretion. Clin Pharmacol Ther. 2011;89:81-88.
46. Lepist E-I, Murray BP, Tong L, et al. Effect of cobicistat and ritonavir on proximal renal tubular cell uptake and efflux transporters [poster A1-1724]. Presented at: 51st Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC); September 17-20, 2011; Chicago, IL.
47. VIREAD-(tenofovir disoproxil fumarate) tablets. US Prescribing Information. Foster City, CA: Gilead Sciences, Inc. May 2007.
48. Ray AS, Cihlar T, Robinson KL, et al. Mechanism of active renal tubular efflux of tenofovir. Antimicrob Agents Chemother. 2006;50:3297-3304.
49. Ito S, Kusuhara H, Yokochi M, et al. Competitive inhibition of the luminal efflux by multidrug and toxin extrusions, but not basolateral uptake by organic cation transporter 2, is the likely mechanism underlying the pharmacokinetic drug-drug interactions caused by cimetidine in the kidney. J Pharmacol Exp Ther. 2012;340:393-403.
50. Ito S, Kusuhara H, Kuroiwa Y, et al. Potent and specific inhibition of mMate1-mediated efflux of type I organic cations in the liver and kidney by pyrimethamine. J Pharmacol Exp Ther. 2010;333:341-350.
51. Tsuda M, Terada T, Ueba M, et al. Involvement of human multidrug and toxin extrusion 1 in the drug interaction between cimetidine and metformin in renal epithelial cells. J Pharmacol Exp Ther. 2009;329:185-191.
52. Meyer zu Schwabedissen HE, Verstuyft C, Kroemer HK, et al. Human multidrug and toxin extrusion 1 (MATE1/SLC47A1) transporter: functional characterization, interaction with OCT2 (SLC22A2), and single nucleotide polymorphisms. Am J Physiol Renal Physiol. 2010;298:F997-F1005.