Rilpivirine, a novel non-nucleoside reverse transcriptase inhibitor for the management of HIV-1 infection: A systematic review

Antiviral Therapy

Volumn 17, Issue 8, 2012, Pages 1495-1502

  Schafer, Jason J ^a   Short, William R ^b  

^a THOMAS JEFFERSON UNIVERSITY   (United States)

^b THOMAS JEFFERSON UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ABACAVIR PLUS LAMIVUDINE; ATORVASTATIN; DARUNAVIR PLUS RITONAVIR; DIDANOSINE; EFAVIRENZ; EMTRICITABINE PLUS RILPIVIRINE PLUS TENOFOVIR DISOPROXIL; EMTRICITABINE PLUS TENOFOVIR DISOPROXIL; ETHINYLESTRADIOL PLUS NORETHISTERONE; FAMOTIDINE; KETOCONAZOLE; LAMIVUDINE PLUS ZIDOVUDINE; LOPINAVIR PLUS RITONAVIR; METHADONE; NEVIRAPINE; OMEPRAZOLE; PLACEBO; RIFABUTIN; RIFAMPICIN; RILPIVIRINE; TENOFOVIR;

ABDOMINAL PAIN; ABNORMAL DREAMING; AREA UNDER THE CURVE; DEPRESSION; DIZZINESS; DRUG ABSORPTION; DRUG EFFICACY; DRUG ERUPTION; DRUG EXCRETION; DRUG FORMULATION; DRUG HALF LIFE; DRUG INDUCED HEADACHE; DRUG MECHANISM; DRUG METABOLISM; DRUG POTENTIATION; DRUG SAFETY; DRUG SUBSTITUTION; DRUG WITHDRAWAL; FATIGUE; GASTROINTESTINAL DISEASE; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS 1 INFECTION; INSOMNIA; MAXIMUM PLASMA CONCENTRATION; MENTAL DISEASE; NAUSEA; NEUROLOGIC DISEASE; PHASE 3 CLINICAL TRIAL (TOPIC); PRIORITY JOURNAL; QT PROLONGATION; REVIEW; SKIN DISEASE; SYSTEMATIC REVIEW; VIROLOGY; VIRUS LOAD; VIRUS MUTATION; VIRUS RESISTANCE; VIRUS STRAIN; VOMITING;

ANTI-HIV AGENTS; BENZOXAZINES; CLINICAL TRIALS AS TOPIC; DRUG INTERACTIONS; DRUG RESISTANCE, VIRAL; DRUG SUBSTITUTION; HIV INFECTIONS; HIV-1; HUMANS; NITRILES; PYRIMIDINES; REVERSE TRANSCRIPTASE INHIBITORS;

EID: 84871907142     PISSN: 13596535     EISSN: 20402058     Source Type: Journal    
DOI: 10.3851/IMP2254     Document Type: Review

References (38)

1. Wheeler WH, Ziebell RA, Zabina H, et al. Prevalence of transmitted drug resistance associated mutations and HIV-1 subtypes in new HIV-1 diagnoses, US-2006. AIDS 2010; 24:1203-1212.
2. Edurant (rilpivirine). Package insert, 2011. Tibotec Pharmaceuticals, Raritan, NJ, USA.
3. Arastéh K, Rieger A, Yeni P, et al. Short term randomized proof-of-principle trial of TMC278 in patients with HIV type-1 who have previously failed antiretroviral therapy. Antivir Ther 2009; 14:713-722.
4. Complera (emtricitabine, rilpivirine, tenofovir). Package insert, 2011. Gilead Sciences, Foster City, CA, USA.
5. Baert L, van 't Klooster G, Dries W, et al. Development of a long-acting injectable formulation with nanoparticles of rilpivirine (TMC278) for HIV treatment. Eur J Pharm Biopharm 2009; 72:502-508.
6. Lansdon EB, Brendza KM, Hung M, et al. Crystal structures of HIV-1 reverse transcriptase with etravirine (TMC125) and rilpivirine (TMC278): implications for drug design. J Med Chem 2010; 53:4295-4299.
7. Das K, Bauman JD, Clark AD, et al. High-resolution structures of HIV-1 reverse transcriptase/TMC278 complexes: strategic flexibility explains potency again resistance mutations. Proc Natl Acad Sci U S A 2007; 105:1466-1471. (Pubitemid 351346537)
8. De Bethune M-P, Andries K, Azijn H, et al. TMC278, a new potent NNRTI with an increased barrier to resistance and good pharmacokinetic profile. 12th Conference on Retroviruses and Opportunistic Infections. 22-25 February 2005, Boston, MA, USA. Abstract 556.
9. Goebel F, Yakovlev A, Pozniak AL, et al . Short term antiviral activity of TMC278 -a novel NNRTI -in treatment-naive HIV-1 infected subjects. AIDS 2006; 20:1721-1726. (Pubitemid 44299363)
10. Crauwels HM, van Heeswijk R, Bollen A, et al. The effect of different types of food on the bioavailability of TMC278, an investigational NNRTI. 9th International Workshop on Pharmacology of HIV Therapy. 7-9 April 2008, New Orleans, LA, USA. Abstract 32.
11. Pea F, Viale P, Pavan F, Furlanut M. Pharmacokinetic considerations for antimicrobial therapy in patients receiving renal replacement therapy. Clin Pharmacokinet 2007; 46:997-1038. (Pubitemid 350136909)
12. Nelson M, Amaya G, Clumeck N, et al. Efficacy and safety of TMC278 in treatment-naïve, HIV-1-infected patients with HBV/HCV co-infection enrolled in the Phase III ECHO and THRIVE trials. J Int AIDS Soc 2010; 13 Suppl 4:210.
13. van Heeswijk RPG, Hoetelmans RMW, Kestens D, et al. The pharmacokinetic (PK) interaction between TMC278, a next-generation NNRTI, and once-daily (qd) darunavir/ritonavir (DRV/r) in HIV-negative volunteers. 47th Interscience Conference on Antimicrobial Agents and Chemotherapy. 17-20 September 2007, Chicago, IL, USA. Abstract H1042.
14. Hoetelmans R, van Heeswijk R, Kestens D, et al. Pharmacokinetic interaction between TMC278, an investigational non-nucleoside reverse transcriptase inhibitor (NNRTI) and lopinavir/ritonavir (LPV/r) in healthy volunteers. 10th European AIDS Conference. 17-20 November 2005, Dublin, Ireland. Abstract PE4.3/1.
15. Hoetelmans R, van Heeswijk R, Kestens D, et al. Pharmacokinetic interaction between the novel non-nucleoside reverse transcriptase inhibitor (NNRTI) TMC278 and tenofovir disoproxil fumerate (TDF) in healthy volunteers. 3rd International AIDS Society Conference on Pathogenesis, Treatment, and Prevention. 24-27 July 2005, Rio de Janeiro, Brazil. Abstract WePe3.3C16.
16. Crauwels H, van Heeswijk R, Kestens D, et al. The pharmacokinetic (PK) interaction between rifabutin and TMC278, an investigational non-nucleoside reverse transcriptase inhibitor (NNRTI). 17th International AIDS Conference. 3-8 August 2008, Mexico City, Mexico. Abstract TUPE0080.
17. Van Heeswijk R, Hoetelmans RMW, Kestens D, et al. The effects of CYP3A4 modulation on the pharmacokinetics of TMC278, an investigational non-nucleoside reverse transcriptase inhibitor (NNRTI). 7th International Workshop of Clinical Pharmacology. 20-22 April 2006, Lisbon, Portugal. Abstract 74.
18. Crauwels HM, van Heeswijk RPG, Kestens D, et al. The pharmacokinetic (PK) interaction between omeprazole and TMC278, a next generation non-nucleoside reverse transcriptase inhibitor (NNRTI). 9th International Congress on Drug Therapy in HIV Infection. 9-13 November 2008, Glasgow, UK. Abstract P239.
19. Van Heswijk R, Hoetelmans RM, Kestens D, et al. The pharmacokinetic (PK) interaction between famotidine and TMC278, a next generation non-nucleoside reverse transcriptase inhibitor (NNRTI), in HIV-negative volunteers. 4th International AIDS Society Conference on HIV Pathogenesis. 22-25 July 2007, Sydney, Australia. Abstract TUPDB01.
20. Van Heeswijk RPG, Hoetelmans RMW, Aharchi F, et al. The pharmacokinetic (PK) interaction between atorvastatin (AVS) and TMC278, a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI), in HIV-negative volunteers. 11th European AIDS Conference. 24-27 October 2007, Madrid, Spain. Abstract P4.3/04.
21. Crauwels HM, van Heeswijk RPG, Cornelis L, et al. Pharmacokinetic interaction study between TMC278, an NNRTI, and the contraceptives norethindrone plus ethinylestradiol. 12th European AIDS Conference/EACS. 11-14 November 2009, Cologne, Germany. Abstract PE4.3/3.
22. Van Heeswijk RP, Hoetelmans RM, Kestens D, et al. The pharmacokinetic interaction between ketoconazole and TMC278, an investigational nonnucleoside reverse transcriptase inhibitor in healthy, HIV-negative subjects. 16th International AIDS Conference. 13-18 August 2006, Toronto, ON, Canada. Abstract TUPE0087.
23. Crauwels HM, Van Heeswijk RPG, Stevens T, et al. The effect of TMC278, a next generation NNRTI, on CYP3A activity in vivo. 10th International Workshop on Clinical Pharmacology of HIV Therapy. 15-17 April 2009, Amsterdam, the Netherlands. Abstract P22.
24. Crauwels HM, van Heeswijk RPG, Vandevoorde A, et al. Pharmacokinetic interaction study between TMC278, a next generation NNRTI, and methadone. 18th International AIDS Conference. July 18-23, 2010, Vienna, Austria. Abstract THLBB206.
25. Pozniak AL, Morales-Ramirez J, Katabira E, et al. Efficacy and safety of TMC278 in antiretroviral-naive HIV-1 patients: week 96 results of a Phase IIb randomized trial. AIDS 2010; 24:55-65.
26. Molina JM, Cahn P, Grinsztejn B, et al. Rilpivirine versus efavirenz with tenofovir and emtracitabine in treatment-naive adults infected with HIV-1 (ECHO): a Phase 3 randomised double-blind active controlled trial. Lancet 2011; 378:238-246.
27. Cohen CJ, Villanueva JA, Clotet B, et al. Rilpivirine versus efavirenz with two background nucleoside or nucleotide reverse transcriptase inhibitors in treatment-naive adults infected with HIV-1 (THRIVE): a Phase 3, randomised, non-inferiority trial. Lancet 2011; 378:229-237.
28. Center for Drug Evaluation and Research. Statistical review and evaluation: clinical studies. TMC278 (rilpivirine), a diarylpyrimidine derivative, NNRTI, 25 mg qd. (Updated 1 July 2010. Accessed 1 November 2012.). Available from http://www.accessdata.fda.gov/drugsatfda-docs/nda/2011/ 202022Orig1s000StatR.pdf
29. Vanveggel S, Buelens A, Crauwels HM, et al. TMC278 25 mg qd has no effect on corrected QT interval in a study in HIV-negative volunteers. 12th European AIDS Conference. 11-14 November 2009, Cologne, Germany. Abstract PE7.1/2.
30. Cohen C, Molina JM, Cahn P, et al. Pooled week 48 safety and efficacy results from the ECHO and THRIVE phase III trials comparing TMC278 vs EFV in treatment-naive, HIV-1 infected patients. 10th International Congress on Drug Therapy in HIV Infection. 7-11 November 2010, Glasgow, UK. Abstract P210.
31. Cohen CJ, Molina JM, Cassetti I, et al. Pooled week 96 efficacy, resistance, and safety results from the double-blind, randomised, Phase III trials comparing rilpivirine versus efavirenz in treatment naive, HIV-1 infected adults. 6th International AIDS Society Conference on HIV Pathogenesis, Treatment, and Prevention. 17-20 July 2011, Rome, Italy. Abstract TULBPE032.
32. Panel on Antiretroviral Guidelines for Adults and Adolescents. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents. Department of Health and Human Services. (Updated 14 October 2011. Accessed 16 January 2012.) Available from http://www.aidsinfo.nih.gov/ContentFiles/ AdultandAdolescentGL.pdf
33. Crauwels H, Vingerhoets J, Ryan R, Witek J, Anderson D. Pharmacokinetic parameters of once-daily rilpivirine following administration of efavirenz in healthy subjects. Antivir Ther 2012; 17:439-446.
34. Mills A, Cohen C, Dejesus E, et al. Switching from efavirenz/ emtricitabine/tenofovir disoproxil fumarate (EFV/FTC/TDF) single tablet regimen (STR) to emtricitabine/rilpivirine/tenofovir disoproxil fumarate (FTC/RPV/TDF) STR in virologically suppressed, HIV-1 infected subjects. 51st Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC). 17-20 September 2011, Chicago, IL, USA. Abstract H2-974c.
35. Desmidt M, Willems B, Donn P, et al. Absence of a teratogenic potential from a novel next-generation NNRTI, TMC278. 12th European AIDS Clinical Society Conference. 11-14, November 2009, Cologne, Germany. Abstract PE7.1/4.
36. Azijn H, Tirry I, Vingerhoets J, et al. TMC278, a next generation NNRTI, active again wild-type and NNRTI-resistant HIV-1. Antimicrob Agents Chemother 2010; 54:718-727.
37. Rimsky L, Vingerhoets J, Van Eygen V, et al. Genotypic and phenotypic characterization of HIV-1 isolates obtained from patients on rilpivirine therapy experiencing virologic failure in the phase 3 ECHO and THRIVE studies: 48-week analysis. J Acquir Immune Defic Syndr 2012; 59:39-46.
38. Kulkarni R, Babaoglu K, Lansdon EB, et al. The HIV-1 reverse transcriptase M184I mutation enhances the E138K associated resistance to rilpivirine and decreases viral fitness. J Acquir Immune Defic Syndr 2012; 59:47-54.