Effect of steady-state etravirine on the pharmacokinetics and pharmacodynamics of ethinylestradiol and norethindrone

Contraception

Volumn 80, Issue 1, 2009, Pages 44-52

  Schöller Gyüre, Monika ^a   Kakuda, Thomas N ^b   Woodfall, Brian ^a   Aharchi, Fatima ^a   Peeters, Monika ^a   Vandermeulen, Kati ^a   Hoetelmans, Richard M W ^a  

^a Research and Development   (Belgium)

^b Tibotec Inc   (United States)

Author keywords

Drug drug interaction; Ethinylestradiol; Etravirine; Non nucleoside reverse transcriptase inhibitor; Norethindrone; Oral contraceptives; Pharmacokinetics; TMC125

Indexed keywords

ETRAVIRINE; MESTRANOL PLUS NORETHISTERONE;

ADULT; AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG DETERMINATION; DRUG EFFECT; DRUG EFFICACY; DRUG WITHDRAWAL; FEMALE; FEVER; HEADACHE; HERPES SIMPLEX; HORMONAL CONTRACEPTION; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; LYMPHADENOPATHY; MAXIMUM PLASMA CONCENTRATION; MORNING DOSAGE; MULTIPLE CYCLE TREATMENT; NAUSEA; NORMAL HUMAN; ORAL CONTRACEPTION; PHARMACODYNAMICS; RANDOMIZED CONTROLLED TRIAL; RASH; SIDE EFFECT; STEADY STATE; TIME TO MAXIMUM PLASMA CONCENTRATION; VITAL SIGN;

ADOLESCENT; ADULT; ANTI-HIV AGENTS; CONTRACEPTIVES, ORAL, SYNTHETIC; DRUG INTERACTIONS; ETHINYL ESTRADIOL; FEMALE; HUMANS; NORETHINDRONE; PYRIDAZINES; YOUNG ADULT;

EID: 66549114704     PISSN: 00107824     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.contraception.2009.01.009     Document Type: Article

References (40)

1. UNAIDS annual AIDS epidemic update, 2007, Geneva, Switzerland. Accessed July 3, 2008 at:. http://data.unaids.org/pub/EPISlides/2007/2007_epiupdate_en.pdf
2. Massad L.S., Evans C.T., Wilson T.E., Golub E.T., Sanchez-Keeland L., and Minkoff H. Contraceptive use among U.S. women with HIV. J Womens Health (Larchmt) 16 (2007) 657-666
3. Macqueen K.M., Johnson L., Alleman P., Akumatey B., Lawoyin T., and Nyiama T. Pregnancy prevention practices among women with multiple partners in an HIV prevention trial. J Acquir Immune Defic Syndr 46 (2007) 32-38
4. Mitchell H.S., and Stephens E. Contraception choice for HIV positive women. Sex Transm Infect 80 (2004) 167-173
5. Zhang H., Cui D., Wang B., et al. Pharmacokinetic drug interactions involving 17alpha-ethinylestradiol: a new look at an old drug. Clin Pharmacokinet 46 (2007) 133-157
6. Reed M.J., and Fotherby F. Intestinal absorption of synthetic steroids. J Steroid Biochem 11 (1979) 1107-1112
7. Wang B., Sanchez R.I., Franklin R.B., Evans D.C., and Huskey S.E. The involvement of CYP3A4 and CYP2C9 in the metabolism of 17 alpha-ethinylestradiol. Drug Metab Dispos 32 (2004) 1209-1212
8. Palovaara S., Kivisto K.T., Tapanainen P., Manninen P., Neuvonen P.J., and Laine K. Effect of an oral contraceptive preparation containing ethinylestradiol and gestodene on CYP3A4 activity as measured by midazolam 1′-hydroxylation. Br J Clin Pharmacol 50 (2000) 333-337
9. Palovaara S., Tybring G., and Laine K. The effect of ethinyloestradiol and levonorgestrel on the CYP2C19-mediated metabolism of omeprazole in healthy female subjects. Br J Clin Pharmacol 56 (2003) 232-237
10. LeBel M., Masson E., Guilbert E., et al. Effects of rifabutin and rifampicin on the pharmacokinetics of ethinylestradiol and norethindrone. J Clin Pharmacol 38 (1998) 1042-1050
11. Andries K., Azijn H., Thielemans T., et al. TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1. Antimicrob Agents Chemother 48 (2004) 4680-4686
12. Vingerhoets J., Azijn H., Fransen E., et al. TMC125 displays a high genetic barrier to the development of resistance: evidence from in vitro selection experiments. J Virol 79 (2005) 12773-12782
13. Madruga J.V., Cahn P., Grinsztejn B., et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-1: 24-week results from a randomised, double-blind, placebo-controlled trial. Lancet 370 (2007) 29-38
14. Lazzarin A., Campbell T., Clotet B., et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-2: 24-week results from a randomised, double-blind, placebo-controlled trial. Lancet 370 (2007) 39-48
15. Trottier B., Johnson M., Katlama C., et al. Pooled 48-week analysis of DUET-1 and DUET-2: durable efficacy and safety results of etravirine (ETR; TMC125) in treatment-experienced HIV-infected patients. 17th Annual Canadian Conference on HIV/AIDS Research, April; Montreal, Canada (2008) [Abstract P167]
16. Kakuda T.N., Schöller-Gyüre M., Woodfall B.J., et al. TMC125 in combination with other medications: summary of drug-drug interactions. 8th International Congress on Drug Therapy in HIV Infection, November; Glasgow, United Kingdom (2006) [Abstract PL5.2]
17. Schöller-Gyüre M., Kakuda T.N., Van Solingen R.M., et al. No clinically relevant effect of etravirine (ETR;TMC125) on digoxin pharmacokinetics in HIV-negative volunteers. 9th International Workshop on Clinical Pharmacology in HIV Therapy, April; New Orleans, LA, USA (2008) [Abstract P22]
18. Schöller-Gyüre M., Boffito M., Pozniak A.L., et al. Effect of different meal compositions and fasted state on the oral bioavailability of etravirine. Pharmacotherapy 28 (2008) 1215-1222
19. Sustiva Package Insert (March 2008), Bristol-Myers Squibb Company. http://packageinserts.bms.com/pi/pi_sustiva.pdf Available at:
20. Watts D.H. Teratogenicity risk of antiretroviral therapy in pregnancy. Curr HIV/AIDS Rep 4 (2007) 135-140
21. Intelence Prescribing Information (January 2008), Tibotec, Inc. http://www.intelence-info.com/intelence/assets/pdf/INTELENCE_PI.pdf Available at:
22. Viramune. Package Insert (November 2008), Boehringer Ingelheim Pharmaceuticals, Inc. Available at: http://bidocs.boehringer-ingelheim.com/BIWebAccess/ViewServlet.ser?docBa se=renetnt&folderPath=/Prescribing+Information/PIs/Viramune/Viramune .pdf
23. Scott C., Grover D., and Nelson M. Is there a role for etravirine in patients with nonnucleoside reverse transcriptase inhibitor resistance?. AIDS 22 (2008) 989-990
24. Ortho-Novum 1/35 (norethindrone and ethinyl estradiol) package insert (September 2008), Ortho-McNeil-Janssen Pharmaceuticals, Inc. https://www.ortho-mcneilpharmaceutical.com/ortho-mcneilpharmaceutical/sh ared/pi/orthonov.pdf Available at:
25. Regulatory Compliance Center. Division of AIDS table for grading severity of adult adverse experiences; August 1992. Accessed July 3, 2008. http://rcc.tech-res-intl.com/tox_tables.htm
26. Schöller-Gyüre M., Kakuda T.N., De Smedt G., et al. A pharmacokinetic study of etravirine (TMC125) co-administered with ranitidine and omeprazole in HIV-volunteers. Br J Clin Pharmacol 66 4 (2008) 508-516
27. Peeters M., Janssen K., Kakuda T.N., et al. Etravirine has no effect on QT and corrected QT interval in HIV-negative volunteers. Ann Pharmacother 42 (2008) 757-765
28. Mildvan D., Yarrish R., Marshak A., et al. Pharmacokinetic interaction between nevirapine and ethinyl estradiol/norethindrone when administered concurrently to HIV-infected women. J Acquir Immune Defic Syndr 29 (2002) 471-477
29. Sevinsky H., Eley T., He B., et al. Effect of efavirenz on the pharmacokinetics of ethinyl estradiol and norgestimate in healthy female subjects. 48th Annual ICAAC/IDSA 46th Meeting October; Washington, DC, USA (2008) [Abstract A-958]
30. Hendrix C.W., Jackson K.A., Whitmore E., et al. The effect of isotretinoin on the pharmacokinetics and pharmacodynamics of ethinyl estradiol and norethindrone. Clin Pharmacol Ther 75 (2004) 464-475
31. Ouellet D., Hsu A., Qian J., et al. Effect of ritonavir on the pharmacokinetics of ethinyl oestradiol in healthy female volunteers. Br J Clin Pharmacol 46 (1998) 111-116
32. Liu P., Foster G., Gandelman K., et al. Steady-state pharmacokinetic and safety profiles of voriconazole and ritonavir in healthy male subjects. Antimicrob Agents Chemother 51 (2007) 3617-3626
33. Hilbert J., Messig M., Kuye O., and Friedman H. Evaluation of interaction between fluconazole and an oral contraceptive in healthy women. Obstet Gynecol 98 (2001) 218-223
34. Crixivan (indinavir sulfate) package insert (April 2006), Merck&Co., Inc. http://www.crixivan.com/crixivan/shared/documents/pi.pdf Available at:
35. Lipitor (atorvastatin calcium) package insert (November 2007), Pfizer, Inc. http://www.pfizer.com/files/products/uspi_lipitor.pdf Available at:
36. EMEA CPMP Public assessment report: combined oral contraceptives and venous thromboembolism. Doc.Ref:EMEA/CPMP/2201/01/en/Final 2001.
37. Stanczyk F.Z., Ploszaj S., Gentzschein E., Qian D., and Mishell Jr. D.R. Effect of oral contraceptives containing 20 and 35 micrograms ethinyl estradiol on urinary prostacyclin and thromboxane metabolite levels in smokers and nonsmokers. Contraception 59 (1999) 17-23
38. Lidegaard O., Edstrom B., and Kreiner S. Oral contraceptives and venous thromboembolism: a five-year national case-control study. Contraception 65 (2002) 187-196
39. Moutos D., Smith S., and Zacur H. The effect of monophasic combinations of ethinyl estradiol and norethindrone on gonadotropins, androgens and sex hormone binding globulin: a randomized trial. Contraception 52 (1995) 105-109
40. Kakuda T.N., Schöller-Gyüre M., Peeters M., et al. Pharmacokinetics of etravirine are not affected by sex, age, race, use of enfuvirtide or treatment duration in HIV-infected patients. 9th International Workshop on Clinical Pharmacology in HIV Therapy April; New Orleans, LA (2008) [Abstract P34]