In vitro resistance development for RO-0335, a novel diphenylether nonnucleoside reverse transcriptase inhibitor

Antiviral Research

Volumn 86, Issue 2, 2010, Pages 212-219

  Javanbakht, H ^a   Ptak, R G ^b   Chow, E ^a   Yan, J M ^a   Russell, J D ^b   Mankowski, M K ^b   Hogan, P A ^b   Hogg, J H ^a   Vora, H ^e   Hang, J Q ^a   Li, Y ^a   Su, G ^c   Paul, A ^d   Cammack, N ^a   Klumpp, K ^a   Heilek, G ^a  

^a Roche Palo Alto   (United States)

^b SOUTHERN RESEARCH INSTITUTE   (United States)

^c RIGEL PHARMACEUTICALS INC   (United States)

^d Gilead   (United States)

^e Department of Environmental and Radiological Health Sciences   (United States)

Author keywords

HIV 1; Nonnucleoside reverse transcriptase inhibitor; Resistance

Indexed keywords

EFAVIRENZ; ETRAVIRINE; NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITOR; RO 0335; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ANTIVIRAL RESISTANCE; ANTIVIRAL SUSCEPTIBILITY; ARTICLE; CONTROLLED STUDY; DRUG STRUCTURE; GENOTYPE; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS 1; IC 50; NONHUMAN; PRIORITY JOURNAL; SITE DIRECTED MUTAGENESIS; VIRUS MUTATION; VIRUS REPLICATION;

AMINO ACID SUBSTITUTION; ANTI-HIV AGENTS; CELL LINE; DNA MUTATIONAL ANALYSIS; DRUG RESISTANCE, VIRAL; HIV REVERSE TRANSCRIPTASE; HIV-1; HUMANS; MOLECULAR STRUCTURE; MUTAGENESIS, SITE-DIRECTED; MUTATION, MISSENSE; REVERSE TRANSCRIPTASE INHIBITORS; SERIAL PASSAGE;

HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 77951296712     PISSN: 01663542     EISSN: 18729096     Source Type: Journal    
DOI: 10.1016/j.antiviral.2010.02.323     Document Type: Article

References (24)

1. Anastassopoulou C.G., Marozsan A.J., Matet A., Snyder A.D., Arts E.J., Kuhmann S.E., Moore J.P. Escape of HIV-1 from a small molecule CCR5 inhibitor is not associated with a fitness loss. PLoS Pathog. 2007, 3:e79.
2. Antinori A., Zaccarelli M., Cingolani A., Forbici F., Rizzo M.G., Trotta M.P., Di Giambenedetto S., Narciso P., Ammassari A., Girardi E., De Luca A., Perno C.F. Cross-resistance among nonnucleoside reverse transcriptase inhibitors limits recycling efavirenz after nevirapine failure. AIDS Res. Hum. Retroviruses 2002, 18:835-838.
3. Bacheler L., Jeffrey S., Hanna G., D'Aquila R., Wallace L., Logue K., Cordova B., Hertogs K., Larder B., Buckery R., Baker D., Gallagher K., Scarnati H., Tritch R., Rizzo C. Genotypic correlates of phenotypic resistance to efavirenz in virus isolates from patients failing nonnucleoside reverse transcriptase inhibitor therapy. J. Virol. 2001, 75:4999-5008.
4. Bacheler L.T., Anton E.D., Kudish P., Baker D., Bunville J., Krakowski K., Bolling L., Aujay M., Wang X.V., Ellis D., Becker M.F., Lasut A.L., George H.J., Spalding D.R., Hollis G., Abremski K. Human immunodeficiency virus type 1 mutations selected in patients failing efavirenz combination therapy. Antimicrob. Agents Chemother. 2000, 44:2475-2484.
5. Buckheit R.W., Swanstrom R. Characterization of an HIV-1 isolate displaying an apparent absence of virion-associated reverse transcriptase activity. AIDS Res. Hum. Retroviruses 1991, 7:295-302.
6. Charneau P., Mirambeau G., Roux P., Paulous S., Buc H., Clavel F. HIV-1 reverse transcription. A termination step at the center of the genome. J. Mol. Biol. 1994, 241:651-662.
7. De Clercq E. Non-nucleoside reverse transcriptase inhibitors (NNRTIs): past, present, and future. Chem. Biodivers. 2004, 1:44-64.
8. Delaugerre C., Rohban R., Simon A., Mouroux M., Tricot C., Agher R., Huraux J.M., Katlama C., Calvez V. Resistance profile and cross-resistance of HIV-1 among patients failing a non-nucleoside reverse transcriptase inhibitor-containing regimen. J. Med. Virol. 2001, 65:445-448.
9. Demeter L.M., Shafer R.W., Meehan P.M., Holden-Wiltse J., Fischl M.A., Freimuth W.W., Para M.F., Reichman R.C. Delavirdine susceptibilities and associated reverse transcriptase mutations in human immunodeficiency virus type 1 isolates from patients in a phase I/II trial of delavirdine monotherapy (ACTG 260). Antimicrob. Agents Chemother. 2000, 44:794-797.
10. Grant R.M., Hecht F.M., Warmerdam M., Liu L., Liegler T., Petropoulos C.J., Hellmann N.S., Chesney M., Busch M.P., Kahn J.O. Time trends in primary HIV-1 drug resistance among recently infected persons. JAMA 2002, 288:181-188.
11. Hammer S.M., Saag M.S., Schechter M., Montaner J.S., Schooley R.T., Jacobsen D.M., Thompson M.A., Carpenter C.C., Fischl M.A., Gazzard B.G., Gatell J.M., Hirsch M.S., Katzenstein D.A., Richman D.D., Vella S., Yeni P.G., Volberding P.A. Treatment for adult HIV infection: 2006 recommendations of the International AIDS Society-USA panel. JAMA 2006, 296:827-843.
12. Johnson V.A., Brun-Vézinet F., Clotet B., Günthard H.F., Kuritzkes D.R., Pillay D., Schapiro J.M., Richman D.D. Update of the drug resistance mutations in HIV-1: Spring 2008. Top. HIV Med. 2008, 16:62-68.
13. Koval C.E., Dykes C., Wang J., Demeter L.M. Relative replication fitness of efavirenz-resistant mutants of HIV-1: correlation with frequency during clinical therapy and evidence of compensation for the reduced fitness of K103N+L100I by the nucleoside resistance mutation L74V. Virology 2006, 353:184-192.
14. Marée A.F., Keulen W., Boucher C.A., De Boer R.J. Estimating relative fitness in viral competition experiments. J. Virol. 2000, 74:11067-11072.
15. Pauwels R., De Clercq E., Desmyter J., Balzarini J., Goubau P., Herdewijn P., Vanderhaeghe H., Vandeputte M. Sensitive and rapid assay on MT-4 cells for detection of antiviral compounds against the AIDS virus. J. Virol. Methods 1987, 16:171-185.
16. Quiñones-Mateu M.E., Ball S.C., Marozsan A.J., Torre V.S., Albright J.L., Vanham G., van der Groen G., Colebunders R.L., Arts E.J. A dual infection/competition assay shows a correlation between ex vivo human immunodeficiency virus type 1 fitness and disease progression. J. Virol. 2000, 74:9222-9233.
17. Richman D.D., Havlir D., Corbeil J., Looney D., Ignacio C., Spector S.A., Sullivan J., Cheeseman S., Barringer K., Pauletti D., Shih C.-K., Myers M., Griffin J. Nevirapine resistance mutations of human immunodeficiency virus type 1 selected during therapy. J. Virol. 1994, 68:1660-1666.
18. Richman D.D., Morton S.C., Wrin T., Hellmann N., Berry S., Shapiro M.F., Bozzette S.A. The prevalence of antiretroviral drug resistance in the United States. AIDS 2004, 18:1393-1401.
19. Sato A., Hammond J., Alexander T.N., Graham J.P., Binford S., Sugita K., Sugimoto H., Fujiwara T., Patick A.K. In vitro selection of mutations in human immunodeficiency virus type 1 reverse transcriptase that confer resistance to capravirine, a novel nonnucleoside reverse transcriptase inhibitor. Antiviral Res. 2006, 70:66-74.
20. Tillekeratne L.M., Sherette A., Fulmer J.A., Hupe L., Hupe D., Gabbara S., Peliska J.A., Hudson R.A. Differential inhibition of polymerase and strand-transfer activities of HIV-1 reverse transcriptase. Bioorg. Med. Chem. Lett. 2002, 12:525-528.
21. Vingerhoets J., Azijn H., Fransen E., De Baere I., Smeulders L., Jochmans D., Andries K., Pauwels R., de Béthune M.P. TMC125 displays a high genetic barrier to the development of resistance: evidence from in vitro selection experiments. J. Virol. 2005, 79:12773-12782.
22. Weinstock H.S., Zaidi I., Heneine W., Bennett D., Garcia-Lerma J.G., Douglas J.M., LaLota M., Dickinson G., Schwarcz S., Torian L., Wendell D., Paul S., Goza G.A., Ruiz J., Boyett B., Kaplan J.E. The epidemiology of antiretroviral drug resistance among drug-naive HIV-1-infected persons in 10 US cities. J. Infect. Dis. 2004, 189:2174-2180.
23. Winslow D.L., Garber S., Reid C., Scarnati H., Baker D., Rayner M.M., Anton E.D. Selection conditions affect the evolution of specific mutations in the reverse transcriptase gene associated with resistance to DMP 266. AIDS 1996, 10:1205-1209.
24. Young S.D., Britcher S.F., Tran L.O., Payne L.S., Lumma W.C., Lyle T.A., Huff J.R., Anderson P.S., Olsen D.B., Carroll S.S., Pettibone D.J., O'Brien J.A., Ball R.G., Balani S.K., Lin J.H., Chen I.-W., Schleif W.A., Sardana V.V., Long W.J., Byrnes V.W., Emini E.A. L-743, 726 (DMP-266): a novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase. Antimicrob. Agents Chemother. 1995, 39:2602-2605.