Next-generation oral preexposure prophylaxis: Beyond tenofovir

Current Opinion in HIV and AIDS

Volumn 7, Issue 6, 2012, Pages 600-606

  Abraham, Bisrat K ^a   Gulick, Roy ^a  

^a WEILL CORNELL MEDICAL CENTER   (United States)

Author keywords

HIV preexposure prophylaxis; ibalizumab; maraviroc; raltegravir; rilpivirine; S GSK1265744

Indexed keywords

ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; ATOVAQUONE PLUS PROGUANIL; CHLOROQUINE; DOLUTEGRAVIR; DOXYCYCLINE; EFAVIRENZ; EMTRICITABINE PLUS TENOFOVIR DISOPROXIL; IBALIZUMAB; MARAVIROC; MEFLOQUINE; PLACEBO; PRIMAQUINE; RALTEGRAVIR; RILPIVIRINE; S GSK 1265744; TENOFOVIR; UNCLASSIFIED DRUG;

ABNORMAL DREAMING; ABSENCE OF SIDE EFFECTS; ANTIVIRAL ACTIVITY; ANTIVIRAL THERAPY; CHEMOPROPHYLAXIS; DIZZINESS; DRUG APPROVAL; DRUG BLOOD LEVEL; DRUG DOSE ESCALATION; DRUG EFFICACY; DRUG ERUPTION; DRUG HALF LIFE; DRUG SAFETY; DRUG TOLERABILITY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; INFECTION PREVENTION; MALARIA; MONOTHERAPY; NIGHTMARE; PHASE 3 CLINICAL TRIAL (TOPIC); PREEXPOSURE PROPHYLAXIS; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL (TOPIC); REVIEW; UNSPECIFIED SIDE EFFECT;

ADMINISTRATION, ORAL; ANTI-HIV AGENTS; CHEMOPREVENTION; HIV INFECTIONS; HUMANS;

EID: 84868465370     PISSN: 1746630X     EISSN: 17466318     Source Type: Journal    
DOI: 10.1097/COH.0b013e328358b9ce     Document Type: Review

References (54)

1. Grant RM, Lama JR, Anderson PL, et al. Preexposure chemoprophylaxis for HIV prevention in men who have sex with men. N Engl J Med 2010; 363:2587-2599.
2. Baeten JM, Donnell D, Ndase P, et al. Antiretroviral prophylaxis for HIV prevention in heterosexual men and women. N Engl J Med 2012; 367: 399-410.
3. Thigpen MC, Kebaabetswe PM, Paxton LA, et al. Antiretroviral preexposure prophylaxis for heterosexual HIV transmission in Botswana. N Engl J Med 2012; 367:423-434.
4. Viread [package insert]. Foster City, CA: Gilead Sciences, Inc.; 2012.
5. 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. March 27 2012. http://www. aidsinfo.nih.gov/contentfiles/lvguidelines/adultandadolescentgl.pdf. [Accessed 19 July 2012].
6. Centers for Disease Control and Prevention. Choosing a drug to prevent malaria. http://www.cdc.gov/malaria/travelers/drugs.html. [Accessed 19 July 2012].
7. Department of Health and Human Services. Next Generation PrEP II (R01). http://grants.nih.gov/grants/guide/rfa-files/RFA-AI-11-023.html. [Accessed 19 July 2012].
8. Gulick RM, Lalezari J, Goodrich J, et al. Maraviroc for previously treated patients with R5 HIV-1 infection. N Engl J Med 2008; 359:1429-1441.
9. Fatkenheuer G, NelsonM, Lazzarin A, et al. Subgroup analyses of maraviroc in previously treated R5 HIV-1 infection. N Engl J Med 2008; 359:1442- 1455.
10. Cooper DA, Heera J, Goodrich J, et al. Maraviroc versus efavirenz, both in combination with zidovudine-lamivudine, for the treatment of antiretroviralnaive subjects with CCR5-tropic HIV-1 infection. J Infect Dis 2010; 201: 803-813.
11. Walmsley S, Campo R, Goodrich J, editors. Low risk of malignancy with maraviroc in treatment-experienced and treatment-naive patients across the maraviroc clinical development program [abstract TUPE0157]. In: Abstracts of the XVIII International AIDS Conference; 18-23 July 2010; Vienna, Austria.
12. Ayoub A, Alston S, Goodrich J, et al. Hepatic safety and tolerability in the maraviroc clinical development program. AIDS 2010; 24:2743-2750.
13. Gulick R, Fatkenheuer G, Burnside R, et al., editors. 5-year safety evaluation of maraviroc in HIV-1-infected, treatment-experienced patients [abstract TUPE029]. In: Abstracts of the XIX International AIDS Conference; 22- 27 July 2012; Washington, DC.
14. Fleishaker DL, Garcia Meijide JA, Petrov A, et al. Maraviroc, a chemokine receptor-5 antagonist, fails to demonstrate efficacy in the treatment of patients with rheumatoid arthritis in a randomized, double-blind placebocontrolled trial. Arthritis Res Ther 2012; 14:R11.
15. Telenti A. Safety concerns about CCR5 as an antiviral target. Curr Opin HIV AIDS 2009; 4:131-135.
16. Rosario MC, Jacqmin P, Dorr P, et al. Population pharmacokinetic/ pharmacodynamic analysis of CCR5 receptor occupancy by maraviroc in healthy subjects and HIV-positive patients. Br J Clin Pharmacol 2008; 65 (Suppl 1):86-94.
17. Fatkenheuer G, Pozniak AL, Johnson MA, et al. Efficacy of short-term monotherapy with maraviroc, a new CCR5 antagonist, in patients infected with HIV-Nat Med 2005; 11:1170-1172.
18. Dumond JB, Patterson KB, Pecha AL, et al. Maraviroc concentrates in the cervicovaginal fluid and vaginal tissue of HIV-negative women. J Acquir Immune Defic Syndr 2009; 51:546-553.
19. Brown KC, Patterson KB, Malone SA, et al. Single and multiple dose pharmacokinetics of maraviroc in saliva, semen, and rectal tissue of healthy HIV-negative men. J Infect Dis 2011; 203:1484-1490.
20. Selzentry [package insert]. Freiburg, Germany: ViiV Healthcare; 2010.
21. Soulie C, Malet I, Lambert-Niclot S, et al. Primary genotypic resistance of HIV-1 to CCR5 antagonists in CCR5 antagonist treatment-naive patients. AIDS 2008; 22:2212-2214.
22. Neff CP, Ndolo T, Tandon A, et al. Oral preexposure prophylaxis by antiretrovirals raltegravir and maraviroc protects against HIV-1 vaginal transmission in a humanized mouse model. PLoS One 2010; 5:e15257.
23. National Institutes of Health. Evaluating the safety and tolerability of antiretroviral drug regimens used as pre-exposure prophylaxis to prevent HIV infection in men who have sex with men. http://www.clinicaltrials.gov/ct2/show/ NCT01505114. [Accessed 19 July 2012].
24. Lennox JL, DeJesus E, Lazzarin A, et al. Safety and efficacy of raltegravirbased versus efavirenz-based combination therapy in treatment-naive patients with HIV-1 infection: a multicentre, double-blind randomised controlled trial. Lancet 2009; 374:796-806.
25. Steigbigel RT, Cooper DA, Kumar PN, et al. Raltegravir with optimized background therapy for resistant HIV-1 infection. N Engl J Med 2008; 359:339-354.
26. DeJesus E, Rockstroh J, Lennox J, et al., editors. Raltegravir-based therapy demonstrates superior virologic suppression and immunologic response compared with efavirenz-based therapy, with a favorable metabolic profile through 4 years in treatment-nave patients: 192 week results from STARTMRK [abstract 405]. In: Abstracts of The Infectious Diseases Society of America Annual Meeting; 20-23 October 2011; Boston.
27. Mayer KH, Mimiaga MJ, Gelman M, Grasso C. Raltegravir, tenofovir DF, and emtricitabine for postexposure prophylaxis to prevent the sexual transmission of HIV: safety, tolerability, and adherence. J Acquir Immune Defic Syndr 2012; 59:354-359.
28. Molto J, Valle M, Back D, et al. Plasma and intracellular (peripheral blood mononuclear cells) pharmacokinetics of once-daily raltegravir (800 milligrams) in HIV-infected patients. Antimicrob Agents Chemother 2011; 55:72-75.
29. Eron JJ Jr, Rockstroh JK, Reynes J, et al. Raltegravir once daily or twice daily in previously untreated patients with HIV- a randomised, active-controlled, phase 3 noninferiority trial. Lancet Infect Dis 2011; 11:907-915.
30. Jones A, Talameh J, Patterson K, et al. First-dose and steady-state pharmacokinetics (PK) of raltegravir (RAL) in the genital tract (GT) of HIV uninfected women [abstract O-06]. In: Abstracts of the 10th International Workshop on Clinical Pharmacology of HIV Therapy; 15-17 April 2009; Amsterdam, The Netherlands.
31. Patterson K, Stevens T, Prince H, et al. Antiretrovirals for prevention: pharmacokinetics of raltegravir in gut-associated lymphoid tissue (GALT) of healthy male volunteers [abstract O-11]. In: Abstracts of the 13th International Workshop on Clinical Pharmacology of HIV Therapy; 16-18 April 2012; Barcelona, Spain.
32. Isentress [package insert]. Whitehouse Station, NJ: Merck Sharp & Dohme Corp.; 2011.
33. Cooper DA, Steigbigel RT,Gatell JM, et al. Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection. N Engl J Med 2008; 359:355- 365.
34. Goethals O, Vos A, Van Ginderen M, et al. Primary mutations selected in vitro with raltegravir confer large fold changes in susceptibility to firstgeneration integrase inhibitors, but minor fold changes to inhibitors with second-generation resistance profiles. Virology 2010; 402:338-346.
35. Garrido C, Villacian J, Zahonero N, et al. Broad phenotypic cross-resistance to elvitegravir in HIV-infected patients failing on raltegravir-containing regimens. Antimicrob Agents Chemother 2012; 56:2873-2878.
36. Boyd SD, Maldarelli F, Sereti I, et al. Transmitted raltegravir resistance in an HIV-1 CRF-AG-infected patient. Antivir Ther 2011; 16:257-261.
37. Cohen CJ, Molina JM, Cahn P, et al. Efficacy and safety of rilpivirine (TMC278) versus efavirenz at 48 weeks in treatment-naive HIV-1-infected patients: pooled results from the phase 3 double-blind randomized ECHO and THRIVE Trials. J Acquir Immune Defic Syndr 2012; 60:33-42.
38. Wilkin A, Pozniak AL, Morales-Ramirez J, et al. Long-term efficacy, safety, and tolerability of rilpivirine (RPV, TMC278) in HIV type 1-infected antiretroviral-naive patients: week 192 results from a phase IIb randomized trial. AIDS Res Hum Retroviruses 2012; 28:437-446.
39. 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.
40. Jackson A, Else L, Tija J, et al., editors. Rilpivirine-LA Formulation: Pharmacokinetics in Plasma, Genital Tract in HIV- Females and Rectum in Males [abstract 35]. In: Abstracts of the 19th Conference on Retroviruses and Opportunistic Infections; 5-8 March 2012; Seattle, Washington, USA.
41. Else L, Jackson A, Tjia J, editors. Pharmacokinetics of long-acting rilpivirine in plasma, genital tract and rectum of HIV-negative females and males administered a single 600mg dose [abstract O-12]. In: Abstracts of the 13th International Workshop on Clinical Pharmacology of HIV Therapy; 16- 18 April 2012; Barcelona, Spain.
42. Edurant [package insert]. Raritan, NJ: Tibotec Therapuetics; 2011.
43. Azijn H, Tirry I, Vingerhoets J, et al. TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. Antimicrob Agents Chemother 2010; 54:718- 727.
44. Min S, DeJesus E, McCurdy L, et al., editors. Pharmacokinetics (PK) and safety in healthy and hiv-infected subjects and short-term antiviral efficacy of S/GSK1265744, a next generation once daily HIV integrase inhibitor [abstract H-1228]. In: Abstracts of the 49th Interscience Conference on Antimicrobial Agents and Chemotherapy; 12-15 September 2009; San Francisco, California, USA.
45. Spreen E, Ford SL, Chen S, et al., editors. Pharmacokinetics, safety, tolerability of the HIV intergrase inhibitor S/GSK1265744 long acting parenteral nanosuspension following single dose administration to healthy adults [abstract TUPE040]. In: Abstracts of the XIX International AIDS Conference; 22-27 July 2012; Washington, DC, USA.
46. National Institutes of Health. A Single Dose Escalation Study to Investigate the Safety, Tolerability and Pharmacokinetics of Intramuscular and Subcutaneous Long Acting GSK1265744 in Healthy Subjects. http://clinicaltrials. gov/ct2/show/NCT01215006. [Accessed 19 July 2012].
47. National Institutes of Health. Study to Investigate the safety, tolerability and pharmacokinetics of repeat dose administration of long-acting GSK1265744 and long-acting TMC278 Intramuscular and subcutaneous injections in healthy adult subjects. http://clinicaltrials.gov/ct2/show/NCT01593046. [Accessed 19 July 2012].
48. Burkly LC, Olson D, Shapiro R, et al. Inhibition of HIV infection by a novel CD4 domain 2-specific monoclonal antibody. Dissecting the basis for its inhibitory effect on HIV-induced cell fusion. J Immunol 1992; 149:1779-1787.
49. Moore JP, Sattentau QJ, Klasse PJ, Burkly LC. A monoclonal antibody to CD4 domain 2 blocks soluble CD4-induced conformational changes in the envelope glycoproteins of human immunodeficiency virus type 1 (HIV-1) and HIV-1 infection of CD4 cells. J Virol 1992; 66:4784-4793.
50. Song R, Franco D, Kao CY, et al. Epitope mapping of ibalizumab, a humanized anti-CD4 monoclonal antibody with anti-HIV-1 activity in infected patients. J Virol 2010; 84:6935-6942.
51. Kuritzkes DR, Jacobson J, Powderly WG, et al. Antiretroviral activity of the anti- CD4 monoclonal antibody TNX-355 in patients infected with HIV type 1. J Infect Dis 2004; 189:286-291.
52. Jacobson JM, Kuritzkes DR, Godofsky E, et al. Safety, pharmacokinetics, and antiretroviral activity of multiple doses of ibalizumab (formerly TNX-355), an anti-CD4 monoclonal antibody, in human immunodeficiency virus type 1- infected adults. Antimicrob Agents Chemother 2009; 53:450-457.
53. Khanlou H, Gathe J, Schrader S, et al., editors. Safety, efficacy and pharmacokinetics of ibalizumab in treatment-experienced HIV-1 infected patients: a Phase 2b study [abstract H2-794b]. In: Abstracts of the 51st Interscience Conference on Antimicrobial Agents and Chemotherapy; 17-20 September 2011; Chicago, Illinois, USA.
54. National Institutes of Health. Safety Study of Ibalizumab Subcutaneous Injection in Healthy Volunteers (TMB-108). http://www.clinicaltrials.gov/ct2/ show/NCT01292174. [Accessed 19 July 2012].