The impact of CYP3A5∗3 polymorphism on sirolimus pharmacokinetics: Insights from predictions with a physiologically-based pharmacokinetic model

British Journal of Clinical Pharmacology

Volumn 80, Issue 6, 2015, Pages 1438-1446

  Emoto, Chie ^a,b   Fukuda, Tsuyoshi ^a,b   Venkatasubramanian, Raja ^a   Vinks, Alexander A ^a,b  

^a CINCINNATI CHILDREN'S HOSPITAL MEDICAL CENTER   (United States)

^b UNIVERSITY OF CINCINNATI COLLEGE OF MEDICINE   (United States)

Author keywords

CYP3A4; CYP3A5 3 polymorphism; PBPK model; sirolimus

Indexed keywords

CYTOCHROME P450 3A5; RAPAMYCIN; ZOTAROLIMUS; CYP3A5 PROTEIN, HUMAN; CYTOCHROME P450 3A; IMMUNOSUPPRESSIVE AGENT;

ARTICLE; COMPUTER MODEL; CONTROLLED STUDY; DRUG METABOLISM; ELIMINATION RATE CONSTANT; ENZYME POLYMORPHISM; GENETIC DIFFERENCE; HUMAN; HUMAN CELL; HUMAN TISSUE; IN VITRO STUDY; INTRINSIC CLEARANCE; LIVER MICROSOME; PHARMACOGENETICS; PHARMACOKINETICS; PRIORITY JOURNAL; STEADY STATE; BIOLOGICAL MODEL; GENETIC POLYMORPHISM; GENETICS; INTESTINE; LIVER; METABOLISM; RETROSPECTIVE STUDY;

CYTOCHROME P-450 CYP3A; HUMANS; IMMUNOSUPPRESSIVE AGENTS; INTESTINES; LIVER; MODELS, BIOLOGICAL; MODELS, GENETIC; POLYMORPHISM, GENETIC; RETROSPECTIVE STUDIES; SIROLIMUS;

EID: 84957439242     PISSN: 03065251     EISSN: 13652125     Source Type: Journal    
DOI: 10.1111/bcp.12743     Document Type: Article

References (25)

1. Meric-Bernstam F, Gonzalez-Angulo AM,. Targeting the mTOR signaling network for cancer therapy. J Clin Oncol 2009; 27: 2278-87.
2. Yost SE, Byrne R, Kaplan B,. Transplantation: mTOR inhibition in kidney transplant recipients. Nat Rev Nephrol 2011; 7: 553-5.
3. MacDonald A, Scarola J, Burke JT, Zimmerman JJ,. Clinical pharmacokinetics and therapeutic drug monitoring of sirolimus. Clini Ther 2000; 22 (Suppl B): B101-21.
4. Jacobsen W, Serkova N, Hausen B, Morris RE, Benet LZ, Christians U,. Comparison of the in vitro metabolism of the macrolide immunosuppressants sirolimus and RAD. Transplant Proc 2001; 33: 514-5.
5. Kuehl P, Zhang J, Lin Y, Lamba J, Assem M, Schuetz J, Watkins PB, Daly A, Wrighton SA, Hall SD, Maurel P, Relling M, Brimer C, Yasuda K, Venkataramanan R, Strom S, Thummel K, Boguski MS, Schuetz E,. Sequence diversity in CYP3A promoters and characterization of the genetic basis of polymorphic CYP3A5 expression. Nat Genet 2001; 27: 383-91.
6. Moes DJ, Swen JJ, den Hartigh J, van der Straaten T, van der Heide JJ, Sanders JS, Bemelman FJ, de Fijter JW, Guchelaar HJ,. Effect of CYP3A4∗22, CYP3A5∗3, and CYP3A combined genotypes on cyclosporine, everolimus, and tacrolimus pharmacokinetics in renal transplantation. CPT: Pharmacometrics Syst Pharmacol 2014; 3: e100.
7. Anglicheau D, Legendre C, Beaune P, Thervet E,. Cytochrome P450 3A polymorphisms and immunosuppressive drugs: an update. Pharmacogenomics 2007; 8: 835-49.
8. Birdwell KA, Decker B, Barbarino JM, Peterson JF, Stein CM, Sadee W, Wang D, Vinks AA, He Y, Swen JJ, Leeder JS, van Schaik RH, Thummel KE, Klein TE, Caudle KE, MacPhee IA,. Clinical pharmacogenetics implementation consortium (CPIC) guidelines for CYP3A5 genotype and tacrolimus dosing. Clin Pharmacol Ther 2015; 98: 19-24. doi: 10.1002/cpt.113.
9. Le Meur Y, Djebli N, Szelag JC, Hoizey G, Toupance O, Rerolle JP, Marquet P,. CYP3A5∗3 influences sirolimus oral clearance in de novo and stable renal transplant recipients. Clin Pharmacol Ther 2006; 80: 51-60.
10. Miao LY, Huang CR, Hou JQ, Qian MY,. Association study of ABCB1 and CYP3A5 gene polymorphisms with sirolimus trough concentration and dose requirements in Chinese renal transplant recipients. Biopharm Drug Dispos 2008; 29: 1-5.
11. Anglicheau D, Le Corre D, Lechaton S, Laurent-Puig P, Kreis H, Beaune P, Legendre C, Thervet E,. Consequences of genetic polymorphisms for sirolimus requirements after renal transplant in patients on primary sirolimus therapy. Am J Transplant 2005; 5: 595-603.
12. Mourad M, Mourad G, Wallemacq P, Garrigue V, Van Bellingen C, Van Kerckhove V, De Meyer M, Malaise J, Eddour DC, Lison D, Squifflet JP, Haufroid V,. Sirolimus and tacrolimus trough concentrations and dose requirements after kidney transplantation in relation to CYP3A5 and MDR1 polymorphisms and steroids. Transplantation 2005; 80: 977-84.
13. Renders L, Frisman M, Ufer M, Mosyagin I, Haenisch S, Ott U, Caliebe A, Dechant M, Braun F, Kunzendorf U, Cascorbi I,. CYP3A5 genotype markedly influences the pharmacokinetics of tacrolimus and sirolimus in kidney transplant recipients. Clin Pharmacol Ther 2007; 81: 228-34.
14. Emoto C, Fukuda T, Cox S, Christians U, Vinks AA,. Development of a physiologically-based pharmacokinetic model for sirolimus: predicting bioavailability based on intestinal CYP3A content. CPT: Pharmacometrics Syst Pharmacol 2013; 2: e59.
15. Walsky RL, Obach RS,. Validated assays for human cytochrome P450 activities. Drug Metab Dispos 2004; 32: 647-60.
16. Walsky RL, Obach RS, Gaman EA, Gleeson JP, Proctor WR,. Selective inhibition of human cytochrome P4502C8 by montelukast. Drug Metab Dispos 2005; 33: 413-8.
17. Obach RS,. Prediction of human clearance of twenty-nine drugs from hepatic microsomal intrinsic clearance data: An examination of in vitro half-life approach and nonspecific binding to microsomes. Drug Metab Dispos 1999; 27: 1350-9.
18. Youdim KA, Zayed A, Dickins M, Phipps A, Griffiths M, Darekar A, Hyland R, Fahmi O, Hurst S, Plowchalk DR, Cook J, Guo F, Obach RS,. Application of CYP3A4 in vitro data to predict clinical drug-drug interactions; predictions of compounds as objects of interaction. Br J Clin Pharmacol 2008; 65: 680-92.
19. Barter ZE, Perrett HF, Yeo KR, Allorge D, Lennard MS, Rostami-Hodjegan A,. Determination of a quantitative relationship between hepatic CYP3A5∗1/∗3 and CYP3A4 expression for use in the prediction of metabolic clearance in virtual populations. Biopharm Drug Dispos 2010; 31: 516-32.
20. Paine MF, Khalighi M, Fisher JM, Shen DD, Kunze KL, Marsh CL, Perkins JD, Thummel KE,. Characterization of interintestinal and intraintestinal variations in human CYP3A-dependent metabolism. J Pharmacol Exp Ther 1997; 283: 1552-62.
21. Paine MF, Hart HL, Ludington SS, Haining RL, Rettie AE, Zeldin DC,. The human intestinal cytochrome P450 'pie'. Drug Metab Dispos 2006; 34: 880-6.
22. Picard N, Djebli N, Sauvage FL, Marquet P,. Metabolism of sirolimus in the presence or absence of cyclosporine by genotyped human liver microsomes and recombinant cytochromes P450 3A4 and 3A5. Drug Metab Dispos 2007; 35: 350-5.
23. Williams JA, Ring BJ, Cantrell VE, Jones DR, Eckstein J, Ruterbories K, Hamman MA, Hall SD, Wrighton SA,. Comparative metabolic capabilities of CYP3A4, CYP3A5, and CYP3A7. Drug Metab Dispos 2002; 30: 883-91.
24. Picard N, Rouguieg-Malki K, Kamar N, Rostaing L, Marquet P,. CYP3A5 genotype does not influence everolimus in vitro metabolism and clinical pharmacokinetics in renal transplant recipients. Transplantation 2011; 91: 652-6.
25. Amundsen R, Asberg A, Ohm IK, Christensen H,. Cyclosporine A- and tacrolimus-mediated inhibition of CYP3A4 and CYP3A5 in vitro. Drug Metab Dispos 2012; 40: 655-61.