Use of In Vitro to In Vivo Extrapolation to Predict the Optimal Strategy for Patients Switching from Efavirenz to Maraviroc or Nevirapine

Clinical Pharmacokinetics

Volumn 54, Issue 1, 2015, Pages 107-116

  Schipani, Alessandro ^a   Back, David ^a   Owen, Andrew ^a   Davies, Gerry ^a   Khoo, Saye ^a   Siccardi, Marco ^a  

^a UNIVERSITY OF LIVERPOOL   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIRETROVIRUS AGENT; BENZOXAZINE DERIVATIVE; CYCLOHEXANE DERIVATIVE; EFAVIRENZ; HUMAN IMMUNODEFICIENCY VIRUS FUSION INHIBITOR; MARAVIROC; NEVIRAPINE; RNA DIRECTED DNA POLYMERASE INHIBITOR; TRIAZOLE DERIVATIVE;

ADOLESCENT; ADULT; AGED; BIOLOGICAL MODEL; CLINICAL TRIAL (TOPIC); COMPUTER SIMULATION; DOSE RESPONSE; FEMALE; HUMAN; IN VITRO STUDY; MALE; MIDDLE AGED; PROCEDURES; YOUNG ADULT;

ADOLESCENT; ADULT; AGED; ANTI-RETROVIRAL AGENTS; BENZOXAZINES; CLINICAL TRIALS AS TOPIC; COMPUTER SIMULATION; CYCLOHEXANES; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; HIV FUSION INHIBITORS; HUMANS; IN VITRO TECHNIQUES; MALE; MIDDLE AGED; MODELS, BIOLOGICAL; NEVIRAPINE; REVERSE TRANSCRIPTASE INHIBITORS; TRIAZOLES; YOUNG ADULT;

EID: 84939976310     PISSN: 03125963     EISSN: 11791926     Source Type: Journal    
DOI: 10.1007/s40262-014-0184-8     Document Type: Article

References (38)

1. Schouten JT, Krambrink A, Ribaudo HJ, Kmack A, Webb N, Shikuma C, et al. Substitution of nevirapine because of Efavirenz Toxicity in AIDS Clinical Trials Group A5095. Clin Infect Dis. 2010;50(5):787–91.
2. Scourfield A, Zheng J, Chinthapalli S, Waters L, Martin T, Mandalia S, et al. Discontinuation of Atripla as first-line therapy in HIV-1 infected individuals. AIDS. 2012;26(11):1399–401.
3. Cooper DA, Heera J, Goodrich J, Tawadrous M, Saag M, Dejesus E, et al. Maraviroc versus efavirenz, both in combination with zidovudine-lamivudine, for the treatment of antiretroviral-naive subjects with CCR5-tropic HIV-1 infection. J Infect Dis. 2010;201(6):803–13.
4. Best BM, Goicoechea M. Efavirenz–still first-line king? Expert Opin Drug Metab Toxicol. 2008;4(7):965–72.
5. Vrouenraets SM, Wit FW, van Tongeren J, Lange JM. Efavirenz: a review. Expert Opin Pharmacother. 2007;8(6):851–71.
6. Fellay J, Marzolini C, Decosterd L, Golay KP, Baumann P, Buclin T, et al. Variations of CYP3A activity induced by antiretroviral treatment in HIV-1 infected patients. Eur J Clin Pharmacol. 2005;60(12):865–73.
7. Kuritzkes D, Kar S, Kirkpatrick P. Fresh from the pipeline—maraviroc. Nat Rev Drug Discov. 2008;7(1):15–6.
8. Abel S, Back DJ, Vourvahis M. Maraviroc: pharmacokinetics and drug interactions. Antivir Ther. 2009;14(5):607–18.
9. Trancart S, Charreau I, Marchou B, Bocquentin M, Molina JM, Izopet J, et al. Presence of lamivudine or emtricitabine is associated with reduced emergence of nonnucleoside reverse transcriptase inhibitor mutations in an efavirenz-based intermittent antiretroviral treatment regimen. Antimicrob Agents Chemother. 2012;56(3):1655–7.
10. Abel S, van der Ryst E, Rosario MC, Ridgway CE, Medhurst CG, Taylor-Worth RJ, et al. Assessment of the pharmacokinetics, safety and tolerability of maraviroc, a novel CCR5 antagonist, in healthy volunteers. Br J Clin Pharmacol. 2008;65(Suppl 1):5–18.
11. Erickson DA, Mather G, Trager WF, Levy RH, Keirns JJ. Characterization of the in vitro biotransformation of the HIV-1 reverse transcriptase inhibitor nevirapine by human hepatic cytochromes P-450. Drug Metab Dispos. 1999;27(12):1488–95.
12. Cooper CL, van Heeswijk RP. Once-daily nevirapine dosing: a pharmacokinetics, efficacy and safety review. HIV Med. 2007;8(1):1–7.
13. Dufty NE, Barrett S, Taylor S. Switching from efavirenz (EFV) to nevirapine (NVP): a novel pharmacological strategy. 15th Annual conference of the British HIV Association British HIV-AIDS Association (BHIVA); Liverpool, UK; 2009.
14. Gelinck LB, Burger DM. Switching from efavirenz to nevirapine. Clin Infect Dis. 2010;51(3):365 (author reply 365–6).
15. Luo R, Piovoso MJ, Martinez-Picado J, Zurakowski R. Optimal antiviral switching to minimize resistance risk in HIV therapy. Plos One. 2011;6(11):e27047.
16. Ward DJ, Curtin JM. Switch from efavirenz to nevirapine associated with resolution of efavirenz-related neuropsychiatric adverse events and improvement in lipid profiles. AIDS Patient Care STDS. 2006;20(8):542–8.
17. Winston A, Pozniak A, Smith N, Fletcher C, Mandalia S, Parmar D, et al. Dose escalation or immediate full dose when switching from efavirenz to nevirapine-based highly active antiretroviral therapy in HIV-1-infected individuals? AIDS. 2004;18(3):572–4.
18. Chen Y, Jin JY, Mukadam S, Malhi V, Kenny JR. Application of IVIVE and PBPK modeling in prospective prediction of clinical pharmacokinetics: strategy and approach during the drug discovery phase with four case studies. Biopharm Drug Dispos. 2012;33(2):85–98.
19. Siccardi M, Marzolini C, Seden K, Almond L, Kirov A, Khoo S, et al. Prediction of drug-druginteractions between various antidepressants and efavirenz or boosted protease inhibitors using aphysiologically based pharmacokinetic modelling approach. Clin Pharmacokinet. 2013;52(7):583–92.
20. Jamei M, Marciniak S, Feng K, Barnett A, Tucker G, Rostami-Hodjegan A. The Simcyp population-based ADME simulator. Expert Opin Drug Metab Toxicol. 2009;5(2):211–23.
21. Hyland R, Dickins M, Collins C, Jones H, Jones B. Maraviroc: in vitro assessment of drug-drug interaction potential. Br J Clin Pharmacol. 2008;66(4):498–507.
22. Siccardi M, Almond L, Schipani A, Csajka C, Marzolini C, Wyen C, et al. Pharmacokinetic and pharmacodynamic analysis of efavirenz dose reduction using an in vitro-in vivo extrapolation model. Clin Pharmacol Ther. 2012;92(4):494–502.
23. Faucette SR, Zhang TC, Moore R, Sueyoshi T, Omiecinski CJ, LeCluyse EL, et al. Relative activation of human pregnane X receptor versus constitutive androstane receptor defines distinct classes of CYP2B6 and CYP3A4 inducers. J Pharmacol Exp Ther. 2007;320(1):72–80.
24. Waters L, Newell S, Else L, Cevik M, Rockwood N, Jackson A, et al. Pharmacokinetics, efficacy and safety of switching from efavirenz to maraviroc twice-daily in patients suppressed on an efavirenz-containing regimen as initial therapy. European AIDS Conference—EACS; 12–15 Oct 2011; Belgrade, Serbia.
25. Schipani A, Wyen C, Mahungu T, Hendra H, Egan D, Siccardi M, et al. Integration of population pharmacokinetics and pharmacogenetics: an aid to optimal nevirapine dose selection in HIV-infected individuals. J Antimicrob Chemother. 2011;66(6):1332–9.
26. De Buck SS, Sinha VK, Fenu LA, Nijsen MJ, Mackie CE, Gilissen RAHJ. Prediction of human pharmacokinetics using physiologically based modeling: a retrospective analysis of 26 clinically tested drugs. Drug Metab Dispos. 2007;35(10):1766–80.
27. Okoli C, Siccardi M, Thomas-William S, Dufty N, Khonyongwa K, Ainsworth J, et al. Once daily maraviroc 300 mg or 150 mg in combination with ritonavir-boosted darunavir 800/100 mg. J Antimicrob Chemother. 2012;67(3):671–4.
28. Boffito M, Jackson A, Lamorde M, Back D, Watson V, Taylor J, et al. Pharmacokinetics and safety of etravirine administered once or twice daily after 2 weeks treatment with efavirenz in healthy volunteers. J Acquir Immune Defic Syndr. 2009;52(2):222–7.
29. Sadiq ST, Fredericks S, Khoo SH, Rice P, Holt DW. Efavirenz detectable in plasma 8 weeks after stopping therapy and subsequent development of non-nucleoside reverse transcriptase inhibitor-associated resistance. AIDS. 2005;19(15):1716–7.
30. Clifford DB, Evans S, Yang Y, Acosta EP, Goodkin K, Tashima K, et al. Impact of efavirenz on neuropsychological performance and symptoms in HIV-infected individuals. Ann Intern Med. 2005;143(10):714–21.
31. Parienti JJ, Peytavin G, Reliquet V, Verdon R, Coquerel A. Pharmacokinetics of the treatment switch from efavirenz to nevirapine. Clin Infect Dis. 2010;50(11):1547–8.
32. Veldkamp AI, Harris M, Montaner JSG, Moyle G, Gazzard B, Youle M, et al. The steady-state pharmacokinetics of efavirenz and nevirapine when used in combination in human immunodeficiency virus type 1-infected persons. J Infect Dis. 2001;184(1):37–42.
33. Manosuthi W, Sungkanuparph S, Tansuphaswadikul S, Inthong Y, Prasithsirikul W, Chottanapund S, et al. Incidence and risk factors of nevirapine-associated skin rashes among HIV-infected patients with CD4 cell counts <250 cells/μL. Int J STD AIDS. 2007;18(11):782–6.
34. DrugBank. http://www.drugbank.ca. Accessed 22 May 2014.
35. Cheeseman SH, Hattox SE, McLaughlin MM, Koup RA, Andrews C, Bova CA, et al. Pharmacokinetics of nevirapine: initial single-rising-dose study in humans. Antimicrob Agents Chemother. 1993;37(2):178–82.
36. Fayet A, Beguin A, de Tejada BM, Colombo S, Cavassini M, Gerber S, et al. Determination of unbound antiretroviral drug concentrations by a modified ultrafiltration method reveals high variability in the free fraction. Ther Drug Monit. 2008;30(4):511–22.
37. Yazdanian M, Glynn SL, Wright JL, Hawi A. Correlating partitioning and caco-2 cell permeability of structurally diverse small molecular weight compounds. Pharm Res. 1998;15(9):1490–4.
38. Lamson MJ, Sabo JP, MacGregor TR, Pav JW, Rowland L, Hawi A, et al. Single dose pharmacokinetics and bioavailability of nevirapine in healthy volunteers. Biopharm Drug Dispos. 1999;20(6):285–91.