Rilpivirine: A novel non-nucleoside reverse transcriptase inhibitor

Expert Opinion on Investigational Drugs

Volumn 18, Issue 7, 2009, Pages 1035-1041

  Garvey, Lucy ^a   Winston, Alan ^a  

^a IMPERIAL COLLEGE HEALTHCARE NHS TRUST   (United Kingdom)

Author keywords

Antiretroviral therapy; Non nucleoside reverse transcriptase inhibitor; Rilpivirine; TMC278

Indexed keywords

ABACAVIR PLUS LAMIVUDINE; ANTACID AGENT; ATAZANAVIR; ATAZANAVIR PLUS RITONAVIR; CIMETIDINE; DAPIVIRINE; EFAVIRENZ; EFAVIRENZ PLUS EMTRICITABINE PLUS TENOFOVIR DISOPROXIL; ELVITEGRAVIR; EMTRICITABINE PLUS TENOFOVIR DISOPROXIL; ETRAVIRINE; FAMOTIDINE; INDINAVIR; KETOCONAZOLE; LAMIVUDINE PLUS ZIDOVUDINE; LANSOPRAZOLE; LOPINAVIR; NEVIRAPINE; OMEPRAZOLE; PLACEBO; PROTEINASE INHIBITOR; RALTEGRAVIR; RANITIDINE; RDEA 806; RIFABUTIN; RILPIVIRINE; RITONAVIR PLUS SAQUINAVIR; RNA DIRECTED DNA POLYMERASE INHIBITOR; SAQUINAVIR; UK 453061; UNCLASSIFIED DRUG;

ANTIVIRAL ACTIVITY; ANTIVIRAL RESISTANCE; AREA UNDER THE CURVE; BODY BUILD; CLINICAL TRIAL; DIZZINESS; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG ERUPTION; DRUG HALF LIFE; DRUG INDUCED HEADACHE; DRUG MECHANISM; DRUG SAFETY; DRUG TOLERABILITY; DRUG WITHDRAWAL; ECG ABNORMALITY; FOOD DRUG INTERACTION; GASTROINTESTINAL SYMPTOM; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS 1 INFECTION; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; LIPOATROPHY; MAXIMUM PLASMA CONCENTRATION; MENTAL DISEASE; MOOD DISORDER; NEUROLOGIC DISEASE; NONHUMAN; QT INTERVAL; REVIEW; SIDE EFFECT; VIRUS MUTATION; VIVID DREAM;

ANIMALS; FOOD-DRUG INTERACTIONS; HIV INFECTIONS; HIV REVERSE TRANSCRIPTASE; HUMANS; NITRILES; PYRIMIDINES; REVERSE TRANSCRIPTASE INHIBITORS;

EID: 67650456668     PISSN: 13543784     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543780903055056     Document Type: Review

References (42)

1. Available from: http://www.unaids.com
2. Mocroft A, Ledergerber B, Katlama C, et al. EuroSIDA study group. Decline in the AIDS and death rates in the EuroSIDA study: an observational study. Lancet 2003;362(9377):22-9
3. HIV in the United Kingdom: 2008 report. Health Protection Agency. Available from: www.hpa.org
4. Temesgen Z. Antiretroviral drugs in development. Expert Opin Investig Drugs 2009;18(4):549-53
5. Gazzard BG. BHIVA Treatment Guidelines Writing Group. British HIV Association Guidelines for the treatment of HIV-1-infected adults with antiretroviral therapy 2008. HIV Med 2008;9(8):563-608
6. Hammer SM, Eron JR JJ, Reiss P, et al. Antiretroviral treatment of adult HIV infection 2008 recommendations of the international AIDS society-USA panel. JAMA 2008;300(5):555-70
7. Clumeck N, Pozniak A, Raffi F; EACS Executive Committee. European AIDS Clinical Society (EACS) guidelines for the clinical management and treatment of HIV-infected adults. HIV Med 2008;9(2):65-71
8. Riddler SA, Haubrich R, et al. Class-sparing regimens for initial treatment of HIV-1 infection. N Engl J Med 2008;358(20):2095-106
9. Markowitz M, Nguyen BY, et al. Rapid and durable antiretroviral effect of the HIV-1 Integrase inhibitor raltegravir as part of combination therapy in treatment-naive patients with HIV-1 infection: results of a 48-week controlled study. J Acquir Immune Defic Syndr 2007;46(2):125-33
10. Saag M, Ive P, Heera J, et al. A multicentre, randomised, double-blind, comparative trial of a novel CCR5 antagonist, maraviroc versus efavirenz, both in combination with Combivir (zidovudine [ZDV]/lamivudine [3TC]), for the treatment of antiretroviral naive subjects infected with R5 HIV-1: week 48 results of the MERIT study [abstract WESS104]. 4th IAS conference, Sydney, 2007
11. Delaugerre C, Rohban R, Simon A, et al. Resistance profile and cross-resistance of HIV-1 among patients failing a non-nucleoside reverse transcriptase inhibitor-containing regimen. J Med Virol 2001;65(3):445-8
12. TM (efavirenz) capsules and tablets package insert. Available from: www.bms.com/pi-sustiva.pdf
13. Martin A, Smith DE, Carr A, et al. Reversibility of lipoatrophy in HIV-infected patients 2 years after switching from a thymidine analogue to abacavir: the MITOX Extension Study. AIDS 2004;18(7):1029-36
14. Poveda E, de Mendoza C, Pattery T, et al. Phenotypic impact of resistance mutations on etravirine susceptibility in HIV patients with prior failure to nonnucleoside analogues. AIDS 2008;22(17):2395-8
15. Madruga JV, Cahn P, Grinsztejn B, et al.; DUET-1 study group. 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 2007;370(9581):29-38
16. IntelenceTM (etravirine) tablets product information. Available from: www.medicines.org.uk/etravirine
17. Mori J, Corbau R, et al. In vitro characterization of UK-453,061, a non-nucleoside reverse transcriptase inhibitor. 15th Conference on Retroviruses and Opportunistic Infections, February 3-6 2008, Boston, USA. F-134
18. Davis J, Jenkins T, Asken E, et al. Safety, toleration and pharmacokinetics of single and multiple oral doses of UK 453,061, a novel NNRTi, in healthy male subjects. 4th IAS Conference, July 2007, Sydney, Australia
19. Fätkenheuer G, Staszewski S, Plettenburg A, et al. Short-term monotherapy with UK-453,061, a novel NNRTI, reduces viral load in HIV infected patients. 4th IAS Conference, July 2007, Sydney, Australia
20. G.Moyle, M. Boffito, K. Manhard, B. Sheedy V, Hingorani L-T, Yeh B. Quart. Antiviral activity of RDEA806, a novel HIV non-nucleoside reverse transcriptase inhibitor, in treatment of Näive HIV patients. XVII International AIDS Conference, 3-8 August 2008, Mexico City
21. Janssen PA, Lewi PJ, Arnold E, et al. In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2- cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine). J Med Chem 2005;48(6):1901-9
22. de Béthune MP, Andries K, Azijn H, et al. TMC278, a new potent NNRTI, with an increased barrier to resistance and favourable pharmacokinetic profile. Presented at the 12th Conference on Retroviruses and Opportunistic Infections (CROI), Boston, USA, 22-25 February 2005, #556
23. Joe D, Bauman K, Das M, et al. Structures of HIV-1 reverse transcriptase complexed with NNRTI TMC278: conformational and positional adaptability overcomes resistance mutations. 14th Conference on Retroviruses and Opportunistic Infections, Los Angeles, February 25-28 2007, #88
24. Crauwels HM, van Heeswijk RPG, Kestens D, Stevens M. The pharmacokinetic interaction between rifabutin and TMC278, an investigational NNRTI [abstract TUPE0080]. XVIIth International Aids Conference, Mexico City, Mexico, August 3-8 2008
25. de Bethune MP, Azijn H, Guillemont J, et al. In vitro characterization of TMC278, a novel potent NNRTI with an increased genetic barrier to the development of resistance. Third European HIV Drug Resistance Workshop [abstract 93]. March 30-April 1, 2005. Athens
26. 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(13):1721-6
27. Pozniak A, Morales-Ramirez J, Mohapi L, et al. 48-Week primary analysis of trial TMC278-C204: TMC278 demonstrates potent and sustained efficacy in ART-naïve patients [abstract 144LB]. 14th Conference on Retroviruses and Opportunistic Infections, Los Angeles, February 25-28 2007
28. Santoscoy M, Cahn P, Gonsalez C, et al. TMC278 (rilpivirine), a next-generation NNRTI, demonstrates long-term efficacy and tolerability in ARV-naïve patients: 96-week results of study C204 [abstract TUAB0103]. XVIIth International Aids Conference, Mexico City, Mexico, August 3-8 2008
29. Hoetelmans R, Kestens D, et al. Effect of food and multiple dose pharmacokinetics of TMC278 as an oral tablet formulation [abstract TuPe3.1B10]. 3rd IAS Conf HIV Pathogenesis and Treatment Jul 24-27 2005
30. van Heeswijk RPG, Hoetelmans RMW, Kestens D, et al. The pharmacokinetic interaction between ketoconazole and TMC278, an investigational NNRTI, in healthy HIV-negative volunteers [abstract TUPE0087]. XVI International AIDS Conference, Toronto, Canada, 13-18 August 2006
31. van Heeswijk R, Hoetelmans R, Kestens D, et al. The pharmacokinetic interaction between famotidine and TMC278, a next-generation NNRTI, in HIV-negative volunteers [abstract TUPDB01]. 4th IAS Conference on HIV Pathogenesis, Treatment and Prevention, Sydney, Australia, 22-25 July 2007
32. Tappouni HL, Rublein JC, Donovan BJ, et al. Effect of omeprazole on the plasma concentrations of indinavir when administered alone and in combination with ritonavir. Am J Health Syst Pharm 2008;65(5):422-8
33. Tomilo DL, Smith PF, Ogundele AB, et al. Inhibition of atazanavir oral absorption by lansoprazole gastric acid suppression in healthy volunteers. Pharmacotherapy 2006;26(3):341-6
34. Luber AD, Brower R, Kim D, et al. Steady-state pharmacokinetics of once-daily fosamprenavir/ritonavir and atazanavir/ritonavir alone and in combination with 20 mg omeprazole in healthy volunteers. HIV Med 2007;8(7):457-64
35. Klein CE, Chiu YL, Cai Y, et al. Effects of acid-reducing agents on the pharmacokinetics of lopinavir/ritonavir and ritonavir-boosted atazanavir. J Clin Pharmacol 2008;48(5):553-62
36. Winston A, Back D, Fletcher C, et al. Effect of omeprazole on the pharmacokinetics of saquinavir-500 mg formulation with ritonavir in healthy male and female volunteers. AIDS 2006;20(10):1401-6
37. Boffito M, Carriero P, Trentini L, et al. Pharmacokinetics of saquinavir co-administered with cimetidine. J Antimicrob Chemother 2002;50(6):1081-4
38. Iwamoto M, Wenning LA, Moreau AR, et al. Omeprazole Increases Plasma Levels of Raltegravir (RAL) in Healthy Subjects. 48th ICAAC/46th IDSA meeting, Washington, October 2008. A-963
39. Ramanathan S, Shen G, Hinkle J, et al. Pharmacokinetic evaluation of drug interactions with ritonavir-boosted HIV integrase inhibitor GS-9137 (elvitegravir) and acid-reducing agents. 8th international workshop on clinical pharmacology of HIV therapy, Budapest, Hungary. 16 - 18 April 2007. Abstract 69
40. Winston A, Bloch M, Carr A, et al. Atazanavir trough plasma concentration monitoring in a cohort of HIV-1-positive individuals receiving highly active antiretroviral therapy. Antimicrob Chemother 2005;56(2):380-7
41. Boly L, Cafaro V, Dyner T. Depressive symptoms predict increased incidence of neuropsychiatric side effects in patients treated with efavirenz. J Acquir Immune Defic Syndr 2006;42(4):514-5
42. Sabin CA, Worm SW, Weber R, et al. Use of nucleoside reverse transcriptase inhibitors and risk of myocardial infarction in HIV-infected patients enrolled in the D:A:D study: a multi-cohort collaboration. Lancet 2008;371(9622):1417-26