메뉴 건너뛰기




Volumn 40, Issue 8, 2014, Pages 1101-1111

Preformulation studies of EFdA, a novel nucleoside reverse transcriptase inhibitor for HIV prevention

Author keywords

Caco 2 cells; EFdA; Permeability; Preformulation; Solubility; Transport

Indexed keywords

4' ETHYNYL 2 FLUORO 2 DEOXYADENOSINE; OCTANOL; RNA DIRECTED DNA POLYMERASE INHIBITOR; UNCLASSIFIED DRUG; WATER; 4'-ETHYNYL-2-FLUORO-2'-DEOXYADENOSINE; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; DEOXYADENOSINE DERIVATIVE;

EID: 84905450163     PISSN: 03639045     EISSN: 15205762     Source Type: Journal    
DOI: 10.3109/03639045.2013.809535     Document Type: Article
Times cited : (12)

References (30)
  • 1
    • 84905463539 scopus 로고    scopus 로고
    • UNAIDS, Global Report: UNAIDS world AIDS day report 2011
    • UNAIDS, Global Report: UNAIDS world AIDS day report 2011.
  • 2
    • 44349159423 scopus 로고    scopus 로고
    • Setting the stage: Host invasion by HIV
    • Hladik F, McElrath MJ. Setting the stage: host invasion by HIV. Nat Rev Immunol 2008;8:447-57.
    • (2008) Nat Rev Immunol , vol.8 , pp. 447-457
    • Hladik, F.1    McElrath, M.J.2
  • 3
    • 77949532283 scopus 로고    scopus 로고
    • In vitro and ex vivo testing of tenofovir shows it is effective as an HIV-1 microbicide
    • Rohan LC, Moncla BJ, Ayudhya RP, et al. In vitro and ex vivo testing of tenofovir shows it is effective as an HIV-1 microbicide. PLoS One 2010;5:e9310.
    • (2010) PLoS One , vol.5
    • Rohan, L.C.1    Moncla, B.J.2    Ayudhya, R.P.3
  • 4
    • 84857131210 scopus 로고    scopus 로고
    • Development and characterization of a vaginal film containing dapivirine, a non-nucleoside reverse transcriptase inhibitor (NNRTI), for prevention of HIV-1 sexual transmission
    • Akil A, Parniak MA, Dezzutti CS, et al. Development and characterization of a vaginal film containing dapivirine, a non-nucleoside reverse transcriptase inhibitor (NNRTI), for prevention of HIV-1 sexual transmission. Drug Deliv Transl Res 2011;1:511-17.
    • (2011) Drug Deliv Transl Res , vol.1 , pp. 511-517
    • Akil, A.1    Parniak, M.A.2    Dezzutti, C.S.3
  • 5
    • 79955528232 scopus 로고    scopus 로고
    • Formulation development of retrocyclin 1 ananlog RC-101 as an anti-HIV vaginal microbicide product
    • Sassi AB, Cost MR, Cole AL, et al. Formulation development of retrocyclin 1 ananlog RC-101 as an anti-HIV vaginal microbicide product. Antimicrob Agents Chemother 2011;55:2282-9.
    • (2011) Antimicrob Agents Chemother , vol.55 , pp. 2282-2289
    • Sassi, A.B.1    Cost, M.R.2    Cole, A.L.3
  • 6
    • 84862782043 scopus 로고    scopus 로고
    • Vaginal film drug delivery of the pyrimidinedione IQP-0528 for the prevention of HIV infection
    • Ham AS, Rohan LC, Boczar A, et al. Vaginal film drug delivery of the pyrimidinedione IQP-0528 for the prevention of HIV infection. Pharm Res 2012;29:1897-907.
    • (2012) Pharm Res , vol.29 , pp. 1897-1907
    • Ham, A.S.1    Rohan, L.C.2    Boczar, A.3
  • 7
    • 77955103248 scopus 로고    scopus 로고
    • Compartmental transport model of microbicide delivery by an intravaginal ring
    • Geonnotti AR, Katz DF. Compartmental transport model of microbicide delivery by an intravaginal ring. J Pharm Sci 2010;99: 3514-21.
    • (2010) J Pharm Sci , vol.99 , pp. 3514-3521
    • Geonnotti, A.R.1    Katz, D.F.2
  • 8
    • 79951889468 scopus 로고    scopus 로고
    • In vivo evaluation of the release of zidovudine and polystyrene sulfonate from a dual intravaginal bioadhesive polymeric device in the pig model
    • Ndesendo VM, Pillay V, Choonara YE, et al. In vivo evaluation of the release of zidovudine and polystyrene sulfonate from a dual intravaginal bioadhesive polymeric device in the pig model. J Pharm Sci 2011;100:1416-35.
    • (2011) J Pharm Sci , vol.100 , pp. 1416-1435
    • Ndesendo, V.M.1    Pillay, V.2    Choonara, Y.E.3
  • 9
    • 84868035130 scopus 로고    scopus 로고
    • Safety and pharmacokinetics of intravaginal rings delivering tenofovir in pig-tailed macaques
    • Moss JA, Malone AM, Smith TJ, et al. Safety and pharmacokinetics of intravaginal rings delivering tenofovir in pig-tailed macaques. Antimicrob Agents Chemother 2012;56:5952-60.
    • (2012) Antimicrob Agents Chemother , vol.56 , pp. 5952-5960
    • Moss, J.A.1    Malone, A.M.2    Smith, T.J.3
  • 10
    • 84865986541 scopus 로고    scopus 로고
    • An intravaginal ring that releases the NNRTI MIV-150 reduces SHIV transmission in macaques
    • Singer R, Mawson P, Derby N, et al. An intravaginal ring that releases the NNRTI MIV-150 reduces SHIV transmission in macaques. Sci Transl Med 2012;4:150ra123.
    • (2012) Sci Transl Med , vol.4
    • Singer, R.1    Mawson, P.2    Derby, N.3
  • 11
    • 33847390394 scopus 로고    scopus 로고
    • Microbicide drug candidates to prevent HIV infection
    • Balzarini J, Van Damme L. Microbicide drug candidates to prevent HIV infection. Lancet 2007;369:787-97.
    • (2007) Lancet , vol.369 , pp. 787-797
    • Balzarini, J.1    Van Damme, L.2
  • 12
    • 34547620353 scopus 로고    scopus 로고
    • Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 40-ethynyl-2-fluoro-20- deoxyadenosine
    • Nakata H, Amano M, Koh Y, et al. Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 40-ethynyl-2-fluoro-20- deoxyadenosine. Antimicrob Agents Chemother 2007;51:2701-8.
    • (2007) Antimicrob Agents Chemother , vol.51 , pp. 2701-2708
    • Nakata, H.1    Amano, M.2    Koh, Y.3
  • 13
    • 48349089930 scopus 로고    scopus 로고
    • 20-Deoxy-40-Cethynyl- 2-halo-adenosines active against drug-resistant human immunodeficiency virus type 1 variants
    • Kawamoto A, Kodama E, Sarafianos SG, et al. 20-Deoxy-40-Cethynyl- 2-halo-adenosines active against drug-resistant human immunodeficiency virus type 1 variants. Int J Biochem Cell Biol 2008;40:2410-20.
    • (2008) Int J Biochem Cell Biol , vol.40 , pp. 2410-2420
    • Kawamoto, A.1    Kodama, E.2    Sarafianos, S.G.3
  • 14
    • 72149100464 scopus 로고    scopus 로고
    • Mechanism of inhibition of HIV-1 reverse transcriptase by 40-ethynyl-2-fluoro-20- deoxyadenosine triphosphate, a translocation defective reverse transcriptase inhibitor
    • Michailidis E, Marchand B, Kodama EN, et al. Mechanism of inhibition of HIV-1 reverse transcriptase by 40-ethynyl-2-fluoro-20- deoxyadenosine triphosphate, a translocation defective reverse transcriptase inhibitor. J Biol Chem 2009;284:35681-91.
    • (2009) J Biol Chem , vol.284 , pp. 35681-35691
    • Michailidis, E.1    Marchand, B.2    Kodama, E.N.3
  • 15
    • 70349088181 scopus 로고    scopus 로고
    • Potent activity of a nucleoside reverse transcriptase inhibitor, 40-ethynyl-2-fluoro-20-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted Nod/SCID janus kinase 3 knockout mice
    • Hattori S, Ide K, Nakata H, et al. Potent activity of a nucleoside reverse transcriptase inhibitor, 40-ethynyl-2-fluoro-20-deoxyadenosine, against human immunodeficiency virus type 1 infection in a model using human peripheral blood mononuclear cell-transplanted Nod/SCID janus kinase 3 knockout mice. Antimicrob Agents Chemother 2009;53:3887-93.
    • (2009) Antimicrob Agents Chemother , vol.53 , pp. 3887-3893
    • Hattori, S.1    Ide, K.2    Nakata, H.3
  • 16
    • 85006536441 scopus 로고    scopus 로고
    • Response of simian immunodeficiency virus to the novel nucleoside reverse transcriptase inhibitor 40-ethynyl-2-fluoro-20-deoxyadenosine in vitro and in vivo
    • Murphey-Corb M, Rajakumar P, Michael H, et al. Response of simian immunodeficiency virus to the novel nucleoside reverse transcriptase inhibitor 40-ethynyl-2-fluoro-20-deoxyadenosine in vitro and in vivo. Antimicrob Agents Chemother 2009;53: 3887-93.
    • (2009) Antimicrob Agents Chemother , vol.53 , pp. 3887-3893
    • Murphey-Corb, M.1    Rajakumar, P.2    Michael, H.3
  • 17
    • 1442324407 scopus 로고    scopus 로고
    • Transport characteristics of 9-nitrocamptothecin in the human intestinal cell line Caco-2 and everted gut sacs
    • Sha XY, Fang XL. Transport characteristics of 9-nitrocamptothecin in the human intestinal cell line Caco-2 and everted gut sacs. Int J Pharm 2004;272:161-71.
    • (2004) Int J Pharm , vol.272 , pp. 161-171
    • Sha, X.Y.1    Fang, X.L.2
  • 18
    • 78649921807 scopus 로고    scopus 로고
    • A three-dimensional coculture of enterocytes, monocytes and dendritic cells to model inflamed intestinal mucosa in vitro
    • Leonard F, Collnot EM, Lehr CM. A three-dimensional coculture of enterocytes, monocytes and dendritic cells to model inflamed intestinal mucosa in vitro. Mol Pharm 2010;7:2103-19.
    • (2010) Mol Pharm , vol.7 , pp. 2103-2119
    • Leonard, F.1    Collnot, E.M.2    Lehr, C.M.3
  • 19
    • 38449084547 scopus 로고    scopus 로고
    • Determination of drug permeability and prediction of drug absorption in Caco-2 monolayers
    • Hubatsch I, Ragnarsson EG, Artursson P. Determination of drug permeability and prediction of drug absorption in Caco-2 monolayers. Nat Protoc 2007;2:2111-19.
    • (2007) Nat Protoc , vol.2 , pp. 2111-2119
    • Hubatsch, I.1    Ragnarsson, E.G.2    Artursson, P.3
  • 20
    • 0035286778 scopus 로고    scopus 로고
    • Caco-2 monolayers in experimental and theoretical predictions of drug transport
    • Artursson P, Palm K, Luthman K. Caco-2 monolayers in experimental and theoretical predictions of drug transport. Adr Drug Deliv Rev 2001;46:27-43.
    • (2001) Adr Drug Deliv Rev , vol.46 , pp. 27-43
    • Artursson, P.1    Palm, K.2    Luthman, K.3
  • 21
    • 78649640372 scopus 로고    scopus 로고
    • In vitro evaluation of viability, integrity, and inflammation in genital epithelia upon exposure to pharmaceutical excipients and candidate microbicides
    • Gali Y, Delezay O, Brouwers J, et al. In vitro evaluation of viability, integrity, and inflammation in genital epithelia upon exposure to pharmaceutical excipients and candidate microbicides. Antimicrob Agents Chemother 2010;54:5105-14.
    • (2010) Antimicrob Agents Chemother , vol.54 , pp. 5105-5114
    • Gali, Y.1    Delezay, O.2    Brouwers, J.3
  • 22
    • 0035984827 scopus 로고    scopus 로고
    • Comparative in vitro sensitivities of human immune cell lines, vaginal and cervical epithelial cell lines, and primary cells to candidate microbicides nonoxynol 9, C31G, and sodium dodecyl sulfate
    • Krebs FC, Miller SR, Catalone BJ, et al. Comparative in vitro sensitivities of human immune cell lines, vaginal and cervical epithelial cell lines, and primary cells to candidate microbicides nonoxynol 9, C31G, and sodium dodecyl sulfate. Antimicrob Agents Chemother 2002;46:2292-8.
    • (2002) Antimicrob Agents Chemother , vol.46 , pp. 2292-2298
    • Krebs, F.C.1    Miller, S.R.2    Catalone, B.J.3
  • 23
    • 0035180107 scopus 로고    scopus 로고
    • Papillomavirus microbicidal activities of high-molecular-weight cellulose sulfate, dextran sulfate, and polystyrene sulfonate
    • Christensen ND, Reed CA, Culp TD, et al. Papillomavirus microbicidal activities of high-molecular-weight cellulose sulfate, dextran sulfate, and polystyrene sulfonate. Antimicrob Agents Chemother 2001;45:3427-32.
    • (2001) Antimicrob Agents Chemother , vol.45 , pp. 3427-3432
    • Christensen, N.D.1    Reed, C.A.2    Culp, T.D.3
  • 24
    • 0025311288 scopus 로고
    • Epithelial transport of drugs in cell culture I: A model for studying the passive diffusion of drugs over intestinal absorptive (Caco-2) cells
    • Artursson P. Epithelial transport of drugs in cell culture. I: A model for studying the passive diffusion of drugs over intestinal absorptive (Caco-2) cells. J Pharm Sci 1990;79:476-82.
    • (1990) J Pharm Sci , vol.79 , pp. 476-482
    • Artursson, P.1
  • 25
    • 0025804183 scopus 로고
    • Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells
    • Artursson P, Karlsson J. Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells. Biochem Biophys Res Comm 1991;175:880-5.
    • (1991) Biochem Biophys Res Comm , vol.175 , pp. 880-885
    • Artursson, P.1    Karlsson, J.2
  • 26
    • 0043127396 scopus 로고    scopus 로고
    • PH-dependent bidirectional transport of weakly basic drugs across Caco-2 monolayers: Implications for drug-drug interactions
    • Neuhoff S, Ungell AL, Zamora I, Artursson P. pH-dependent bidirectional transport of weakly basic drugs across Caco-2 monolayers: implications for drug-drug interactions. Pharm Res 2003;20: 1141-8.
    • (2003) Pharm Res , vol.20 , pp. 1141-1148
    • Neuhoff, S.1    Ungell, A.L.2    Zamora, I.3    Artursson, P.4
  • 27
    • 19444382806 scopus 로고    scopus 로고
    • PH-dependent passive and active transport of acidic drugs across Caco-2 cell monolayers
    • Neuhoff S, Ungell AL, Zamora I, Artursson P. pH-dependent passive and active transport of acidic drugs across Caco-2 cell monolayers. Eur J Pharm Sci 2005;25:211-20.
    • (2005) Eur J Pharm Sci , vol.25 , pp. 211-220
    • Neuhoff, S.1    Ungell, A.L.2    Zamora, I.3    Artursson, P.4
  • 28
    • 3843134182 scopus 로고    scopus 로고
    • Permeability of tritiated water through human cervical and vaginal tissue
    • Sassi AB, Mccullough KD, Cost MR, et al. Permeability of tritiated water through human cervical and vaginal tissue. J Pharm Sci 2004; 93:2009-16.
    • (2004) J Pharm Sci , vol.93 , pp. 2009-2016
    • Sassi, A.B.1    McCullough, K.D.2    Cost, M.R.3
  • 29
    • 0031958251 scopus 로고    scopus 로고
    • Species differences in size discrimination in the paracellular pathway reflected by oral bioavailability of poly (ethylene glycol) and D-peptides
    • He YL, Murby S, Warhurst G, et al. Species differences in size discrimination in the paracellular pathway reflected by oral bioavailability of poly (ethylene glycol) and D-peptides. J Pharm Sci 1998;87:626-33.
    • (1998) J Pharm Sci , vol.87 , pp. 626-633
    • He, Y.L.1    Murby, S.2    Warhurst, G.3
  • 30
    • 0030751673 scopus 로고    scopus 로고
    • The thiocarboxanilide nonnucleoside UC781 is a tight-binding inhibitor of HIV-1 reverse transcriptase
    • Barnard J, Borkow G, Parniak MA. The thiocarboxanilide nonnucleoside UC781 is a tight-binding inhibitor of HIV-1 reverse transcriptase. Biochemistry 1997;36:7786-92.
    • (1997) Biochemistry , vol.36 , pp. 7786-7792
    • Barnard, J.1    Borkow, G.2    Parniak, M.A.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.