Selection of diverse and clinically relevant integrase inhibitor-resistant human immunodeficiency virus type 1 mutants

Antiviral Research

Volumn 80, Issue 2, 2008, Pages 213-222

  Kobayashi, Masanori ^a   Nakahara, Koichiro ^a   Seki, Takahiro ^a   Miki, Shigeru ^a   Kawauchi, Shinobu ^a   Suyama, Akemi ^a   Wakasa Morimoto, Chiaki ^a   Kodama, Makoto ^a   Endoh, Takeshi ^a   Oosugi, Eiichi ^a   Matsushita, Yoshihiro ^a   Murai, Hitoshi ^a   Fujishita, Toshio ^a   Yoshinaga, Tomokazu ^a   Garvey, Edward ^b   Foster, Scott ^b   Underwood, Mark ^b   Johns, Brian ^b   Sato, Akihiko ^a   Fujiwara, Tamio ^a  

^a SHIONOGI AND CO LTD   (Japan)

^b GLAXOSMITHKLINE   (United States)

Author keywords

HIV; Integrase inhibitor; Resistance; S 1360; S GSK 364735

Indexed keywords

1 [5 (4 FLUOROBENZYL) 2 FURYL] 3 (1,2,4 TRIAZOL 3 YL) 1,3 PROPANEDIONE; 4 [1 (4 FLUOROBENZYL) 2 PYRROLYL] 2,4 DIOXOBUTYRIC ACID; CAPRAVIRINE; EFAVIRENZ; ELVITEGRAVIR; GSK 364735; INTEGRASE INHIBITOR; LAMIVUDINE; N (4 FLUOROBENZYL) 8 HYDROXY 5 (TETRAHYDRO 2H 1,2 THIAZIN 2 YL) 1,6 NAPHTHYRIDINE 7 CARBOXAMIDE S,S DIOXIDE; NEVIRAPINE; RALTEGRAVIR; UNCLASSIFIED DRUG;

ANTIVIRAL ACTIVITY; ARTICLE; CONCENTRATION RESPONSE; DRUG STRUCTURE; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; NONHUMAN; PRIORITY JOURNAL; VIRUS INHIBITION; VIRUS MUTATION;

CELL LINE; DRUG EVALUATION, PRECLINICAL; DRUG RESISTANCE, VIRAL; HELA CELLS; HIV INFECTIONS; HIV INTEGRASE; HIV INTEGRASE INHIBITORS; HIV-1; HUMANS; MUTATION; T-LYMPHOCYTES;

HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 53249087908     PISSN: 01663542     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.antiviral.2008.06.012     Document Type: Article

References (23)

1. Adachi A., Gendelman H.E., Koenig S., Folks T., Willey R., Rabson A., and Martin M.A. Production of acquired immunodeficiency syndrome-associated retrovirus in human and non-human cells transfected with an infectious molecular clone. J. Virol. 59 (1986) 284-291
2. Billich A. S-1360 Shionogi-GlaxoSmithKline. Curr. Opin. Investig. Drugs 4 (2003) 206-209
3. DeJesus E., Berger D., Markowitz M., Cohen C., Hawkins T., Ruane P., Elion R., Farthing C., Zhong L., Cheng A.K., McColl D., and Kearney B.P. Antiviral activity, pharmacokinetics, and dose response of the HIV-1 integrase inhibitor GS-9137 (JTK-303) in treatment-naïve and treatment-experienced patients. J. Acquir. Immune Defic. Syndr. 43 (2006) 1-5
4. Egbertson M.S., Moritz H.M., Melamed J.Y., Han W., Perlow D.S., Kuo M.S., Embrey M., Vacca J.P., Zrada M.M., Cortes A.R., Wallace A., Leonard Y., Hazuda D.J., Miller M.D., Felock P.J., Stillmock K.A., Witmer M.V., Schleif W., Gabryelski L.J., Moyer G., Ellis J.D., Jin L., Xu W., Braun M.P., Kassahun K., Tsou N.N., and Young S.D. A potent and orally active HIV-1 integrase inhibitor. Bioorg. Med. Chem. Lett. 17 (2006) 1392-1398
5. Fikkert V., Hombrouck A., Van Remoortel B., De Maeyer M., Pannecouque C., De Clercq E., Debyser Z., and Witvrouw M. Multiple mutations in human immunodeficiency virus-1 integrase confer resistance to the clinical trial drug S-1360. AIDS 18 (2004) 2019-2028
6. Fikkert V., Van Maele B., Vercammen J., Hantson A., Van Remoortel B., Michiels M., Gurnari C., Pannecouque C., De Maeyer M., Engelborghs Y., De Clercq E., Debyser Z., and Witvrouw M. Development of resistance against diketo derivatives of human immunodeficiency virus type 1 by progressive accumulation of integrase mutations. J. Virol. 77 (2003) 11459-11470
7. Fujiwara T., Sato A., El-Farrash M., Miki S., Abe K., Isaka Y., Kodama M., Wu Y., Chen L.B., Harada H., Sugimoto H., Hatanaka M., and Hinuma Y. S-1153 inhibits replication of known drug-resistant strains of human immunodeficiency virus type 1. Antimicrob. Agents Chemother. 42 (1998) 1340-1345
8. Garvey E.P., Johns B.A., Gartland M.J., Foster S.A., Miller W.H., Ferris R.G., Hazen R.J., Underwood M.R., Boros E.E., Thompson J.B., Weatherhead J.G., Koble C.S., Allen S.H., Schaller L.T., Sherrill R.G., Yoshinaga T., Kobayashi M., Wakasa-Morimoto C., Miki S., Nakahara K., Noshi T., Sato A., and Fujiwara T. The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral. Antimicrob. Agents Chemother. 52 (2008) 901-908
9. Harada S., Koyanagi Y., and Yamamoto N. Infection of HTLV-III/LAV in HTLV-I-carrying cells MT-2 and MT-4 and application in a plaque assay. Science 229 (1985) 563-566
10. Hazuda D.J., Felock P., Witmer M., Wolfe A., Stillmock K.J., Grobler A., Espeseth A., Gabryelski L., Schleif W., Blau C., and Miller M.D. Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells. Science 287 (2000) 646-650
11. Hazuda D.J., Anthony N.J., Gomez R.P., Jolly S.M., Wai J.S., Zhuang L., Fisher T.E., Embrey M., Guare Jr. J.P., Egbertson M.S., Vacca J.P., Huff J.R., Felock P.J., Witmer M.V., Stillmock K.A., Danovich R., Grobler FJ., Miller M.D., Espeseth A.S., Jin L., Chen I., Lin J.H., Kassahun K., Ellis J.D., Wong B.K., Xu W., Pearson P.G., Schleif W.A., Cortese R., Emini E., Summa V., Holloway M.K., and Young S.D. A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase. Proc. Natl. Acad. Sci. U.S.A. 101 (2004) 11233-11238
12. Hazuda, D.J., Miller, M.D., Nguyen, B.Y., Zhao, J., 2007. Resistance to the HIV-integrase inhibitor raltegravir: analysis of protocol 005, a phase 2 study in patients with triple-class resistant HIV-1 infection. XVI International Drug Resistance Workshop, Antiviral Therapy 2007, 12, S10.
13. Isaka Y., Sato A., Miki S., Kawauchi S., Sakaida H., Hori T., Uchiyama T., Adachi A., Hayami M., Fujiwara T., and Yoshie O. Small amino acid changes in the V3 loop of human immunodeficiency virus type 2 determines the coreceptor usage for CXCR4 and CCR5. Virology 264 (1999) 237-243
14. Lataillade M., Chiarella J., and Kozal M.J. Natural polymorphism of the HIV-1 integrase gene and mutations associated with integrase inhibitor resistance. Antivir. Ther. 12 (2007) 563-570
15. Markowitz M., Morales-Ramirez J.O., Nguyen B.-Y., Kovacs C.M., Steigbigel R.T., Cooper D.A., Liporace R., Schwartz R., Isaacs R., Gilde L.R., Wenning L., Zhao J., and Teppler H. The protocol 004 study team, Antiretroviral activity, pharmacokinetics, and tolerability of MK-0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment-naïve HIV-1-infected individuals. J. Acquir. Immune Defic. Syndr. 43 (2006) 509-515
16. Markowitz M., Nguyen B.-Y., Gotuzzo E., Mendo F., Ratanasuwan W., Kovacs C., Wan H., Gilde L., Isaacs R., Teppler H., and The Protocol 004 Part II Study Team. Rapid onset and durable antiretroviral effect of raltegravir (MK-0518), a novel HIV-1 integrase inhibitor, as part of combination ART in treatment HIV-1 infected patients: 48-week data. Fourth IAS Conference on HIV Pathogenesis. Treatment and Prevention, Sydney, Australia (2007) Abstract #TUPAB104
17. McColl D.J., Fransen S., Gupta S., Parkin N., Margot N., Ledford R., Chen J., Chuck S., Cheng A.K., and Miller M.D. Resistance and cross-resistance to first generation integrase inhibitors: insights from a phase 2 study of elvitegravir (GS-9137). XVI International Drug Resistance Workshop, Antiviral Therapy, vol. 12 (2007) S11
18. Nakajima N., Lu R., and Engelman A. Human immunodeficiency virus type 1 replication in the absence of integrase-mediated DNA recombination: definition of permissive and nonpermissive T-cell lines. J. Virol. 75 (2001) 7944-7955
19. Pauwels R., Balzarini J., Baba M., Snoeck R., Schols D., Herdewijn P., Desmyter J., and De Clercq E. Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds. J. Virol. Methods 20 (1988) 309-321
20. Sato A., Hammond J., Alexander T.N., Graham J.P., Binford S., Sugita K., Sugimoto H., Fujiwara T., and 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. Antivir. Res. 70 (2006) 66-74
21. Shimura K., Kodama E., Sakagami Y., Matsuzaki Y., Watanabe W., Yamataka K., Watanabe Y., Ohata Y., Doi S., Sato M., Kano M., Ikeda S., and Matsuoka M. Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137). J. Virol. 82 (2008) 764-774
22. 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., and Emini E.A. L-743,726 (DMP-206): a novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase. Antimicrob. Agents Chemother. 39 (1995) 2602-2605
23. Zolopa A.R., Mullen M., Berger D., Ruane P., and Hawkins T. The HIV integrase inhibitor GS-9137 demonstrates potent antiretroviral activity in treatment-experienced patients. 14th Conference on Retroviruses and Opportunistic Infections. Los Angeles (2007) Abstract #143LB