Stavudine:pharmacology,clinical use and future role

Bibliography

• MOYLE GJ: Use of viral resistance patterns to antire troviral drugs in optimising selection of drug combinationsand sequences. Drugs (1996) 52:168–185.
   Google Scholar
• Definitive resistance review.
   Google Scholar
• CHENG N, MERRILL BM, PAINTER GR, FRICK LW, FURMAN PA: Identification of the nucleotide binding site of HIV-1 reverse transcriptase using dTTP as a photoaffinity label. Biochemistry (1993) 32:7630–7634.
   PubMed Web of Science ®Google Scholar
• AUGUST EM, BIRKS EM, PRUSOFF WH: 3'-De-oxythymidin-2'-ene permeation of human lymphocyte 119 cells by nonfacilitated diffusion. Mol. Pharmacol (1991) 39:264–269.
   Google Scholar
• MANSURI MM, STARRETT JE, GHAZZOULI I et al: 142,3-dideoxy-3-D-glycyro-p ent-2-enofuronosy0thymine. A highly potent and selective anti-HIV agent. J. Med. Chem. (1989) 32:461–466.
   Google Scholar
• MANSURI MM, HITCHCOCK MJM, BUROKER RA et al: Comparison of biological properties in vitro and toxic-ity in vivo of three thymidine analogues (d4T, FddT, and AZT) active against HIV. Antimicrob. Agents Chemother. (1990) 34:637–641.
   PubMedGoogle Scholar
• NORTH TW, CRONN RC, REMINGTON KM, TANDBERG RT:Direct comparisons of inhibitor sensitivities of reverse transcriptase from feline and human immunodefi-ciency viruses. Antimicrob. Agents Chemother. (1990) 34:1505–1507.
   PubMed Web of Science ®Google Scholar
• ONO K, NAKANE H, HERDEWIJN P, BALZARINI J, DECLERCQ E: Differential inhibitory effects of several dideoxynucleoside 5'-triphosphates on the activities of reverse transcriptase and various cellular DNA polym-erases. Mol Pharmacol (1989) 35:578–583.
   PubMed Web of Science ®Google Scholar
• LEWIS W, GONZALEZ B, CHOMYN A, PAPOIAN T: Zi-dovudine induces molecular, biochemical and ultras-tructural changes in rat skeletal muscle mitochondria. Clin. Invest. (1992) 89:1354–1360.
   Google Scholar
• CHEN CH, CHENG YC: Delayed cytotoxicity and selective loss of mitochondrial DNA in cells treated with the anti-human immunodeficiency virus compound 2',3'-dideoxycytidine. J. Biol. Chem. (1989) 264:11934–11937.
   PubMed Web of Science ®Google Scholar
• HO H-T, HITCHCOCK MJM: Cellular pharmacology of 2',3'-dideoxy-2',3'-didehydrothymidine, a nucleoside analog active against human immunodeficiency virus. Antimicrob. Aunts Chemother. (1989) 33:844–849.
   PubMed Web of Science ®Google Scholar
• BALZARINI J, HERDEWIJN P, DE CLERCQ E: Differential patterns of intracellular metabolism of 2',3'-didehydro-2',3'- di deoxy thymidine and 3'-azido-2',3'-dide- oxythy midi ne,twopotentanti-humanimmunodeficiency virus compounds. 1 Biol. Chem. (1989) 262:6127–6133.
   Google Scholar
• MARTIN JC, HITCHCOCK MJM, FRIDLAND A et al: Com-parative studies of 2',3'-didehydro-2',3'-dideoxythymid-ine (d4T) with other pyrimidine nucleoside analogues. Ann. NY Acad. Sci. (1990) 616:22–28.
   PubMed Web of Science ®Google Scholar
• ZHU Z, HO H-T, HITCHCOCK MJM, SOMMADOSI J-P: Cellular pharmacology of 2',3'-didehydro-2',3'- dideoxy thymidine (d41) in peripheral blood mononuclear cells. Biochem. Pharmacol (1990) 39:R15–R19.
   PubMed Web of Science ®Google Scholar
• STRETCHER BN, PESCE J, FRAME PT, GREENBERG KA, STEIN DS: Correlates of zidovudine phosphorylAion with markers of HIV disease progression and drug toxicity. AIDS (1994) 8:763–769.
   PubMed Web of Science ®Google Scholar
• YOKOTA T, MOCHIZUKI S, KONNO K eta].: Inhibitory effects of selected antiviral compounds on human hepatitis B virus DNA synthesis. Antimicrob. Agents Chemother. (1991) 35:394–397.
   Google Scholar
• BABA M, PAUWELS R, HEDEWIJN P eta].: Both 2',3'-dide-oxythymidine and its 2',3'-unsaturated derivative (2',3'-dideoxythymidene) are potent and selective inhibitors of human immunodeficiency virus in vitro. Biochem. Biophys. Res. Commun. (1987) 142:128–134.
   Google Scholar
• HAMAMOTO Y, NAKASHIMA H, MATSUI T et al: Inhibi-tory effect of 2',3'-didehydro-2',3'-dideoxynucleosides on infectivity, cytopathic effects, and replication of human immunodeficiency virus. Antimicrob. Agnts Chemother. (1987) 31:907–910.
   PubMed Web of Science ®Google Scholar
• GOGU SR, BECKMAN BS, AGRAWAL KC: Anti-HIV drugs: comparative toxicities in murine fetal liver and bone marrow erythroid progenitor cells. Life Sci. (1989) 31:907–910.
   Google Scholar
• GAO WY, AGBARIA R, DRISCOLL JS, MITSUYA H: Divergent anti-human immunodeficiency virus activity and anabolic phosphorylation of 2',3'-dideoxynucleoside analogs in resting and activated human cells. J. Biol. Chem. (1994) 269:12633–12638.
   Google Scholar
• Potential rationale for combining nucleoside analogues.
   Google Scholar
• MERRILL DP, MOONIS M, CHOU T-C, HIRSCH MS: Lami-vudine or stavudine in two- and three-drug combina-tions against human immunodeficiency virus type 1 replication in vitro. J. Infect. Dis. (1996) 173:355–364.
   PubMed Web of Science ®Google Scholar
• LACEY SF, LARDER BA: Novel mutation (V751) in human immunodeficiency virus type 1 reverse transcriptase confers resistance to 2',3' didehydro-2',3-dide-oxythymidine in cell culture. Antimicrob. Agents Chemother. (1994) 38:1428–1432.
   PubMed Web of Science ®Google Scholar
• GU Z, GAO Q, FANG H et al.: Identification of novel mutations that confer drug resistance in the human immunodeficiency virus polymerase gene. Leukemia (1994) 8\(Suppl. 0:5166–5169.
   Google Scholar
• UN P-F, SAMANTA H, ROSE RE et al.: Genotypic and phenotypic analysis of human immunodeficiency virustype 1 isolates from patients on prolonged stavudine therapy. J. Infect. Dis. (1994) 170:1157–1164.
   Google Scholar
• Only published clinical study of stavudine resistance.
   Google Scholar
• SHEPP D, ASHRAF A, MILLAN C, PERGOLIZZI R: Pheno-typic and genotypic characterisation of HIV isolates during stavudine (d4T) therapy. 2nd National Conference on Human Retroviruses and Related Infections. Washington DC (29 January - 2 February 1995). Abstract 453.
   Google Scholar
• COAKLEY E, GILLIS J, PENDEAULT L, DUNKLE L, HAMMER S: Susceptibilities of HIV-1 isolates derived from pa-tients treated with didanosine (ddI) andstavudine (d4T) in combination. 4th Conference on Retroviruses and Oppor-tunisitic Infections. Washington DC (22–26 January 1997). Abstract 575.
   Google Scholar
• SHIRASAKA T, KAVLICK MF, VENO T et al: Emergence of human immunodeficiency virus type 1 variants with resistance to multiple dideoxynucleosides in patients receiving therapy with dideoxynucleosides. Proc. Natl Acad. Sci. USA (1995) 92:2398–2402.
   Google Scholar
• Report of multi-nucleoside-resistant HIV.
   Google Scholar
• HITCHCOCK MJM: 2',3'-didehydro-2',3'-dideoxy thymid-ine (d41), an anti-HIV agent. Antiviral Chem. Chemother. (1991) 2:125–132.
   Google Scholar
• SCHILLING BE, NELSON DR, PROCTOR JE et aL: The nonclinical toxicologic profile of stavudine. Curr. Ther. Res. (1995) 56:201–218.
   Web of Science ®Google Scholar
• DUDLEY MN, GRAHAM la, KAUL S eta].: Pharmacokinet-ics of stavudine in patients with AIDS or AIDS-related complex. J. Infect. Dis. (1992) 166:480–485.
   Google Scholar
• HORTON CM, DUDLEY MN, KAUL S et al.: Population pharmacokinetics of stavudine (d41) in patients with AIDS or advanced AIDS-related complex. Antimicrob. Agents Chemother. (1995) 39:2309–2315.
   PubMed Web of Science ®Google Scholar
• GRASELA D, CHRISTOFALO B, RAYMOND R, STOLTZ R, STEWART M: Safety and pharmacokinetics (PK) of sta-vudine (d41) in subjects with mild, moderate or severe renal impairment. 2nd National Conference on Human Retroviruses and Related Infections. Washington DC (29 January - 2 February 1995). Abstract 490.
   Google Scholar
• PETTY B, GRASELA D, SCHAAD H, CHRISTAFALO B, STE-WART M: Safety and pharmacokinetics of lavudine (d4T) in hepatic impairment. 2nd National Conference on Human Refroviruses and Related Infections. Washington DC (29 January - 2 February 1995). Abstract 491.
   Google Scholar
• MACLEOD CM, BARTLEY EA, PAUL SK, STEWART MB: Effect of food on oral absorption of stavudine (d4T). 23rd Annual Meeting of the American College of Clinical Pharmacology. Orlando (6–8 October 1994). Abstract 69.
   Google Scholar
• CRETTON EM, ZHOU Z, KIDD LB eta].: In vitro and in vivo disposition and metabolism of 3'-deoxy-2',3'-dide-hydrothymidine. Antimicrob. Agents Chemother. (1993) 37:1916–1925.
   Google Scholar
• KLINE MW, DUNKLE LM, CHURCH JA et al.: A Phase I/11evaluation of stavudine (d4T) in children with human immunodeficiency virus infection. Paediatrics (1995) 96:247–252.
   PubMed Web of Science ®Google Scholar
• BAWDON RE, KAUL S, SOBHI S: The ex vivo transfer of the anti-HIV nucleoside compound d4T in the human placenta. Gynecol Obstet Invest. (1994) 38:1–4.
   PubMed Web of Science ®Google Scholar
• SIEFERT RD, STEWART MB, SRAMEK JJ et al: Pharma co-kinetics of co-administered didanosine and stavudine in HIV-seropositive male patients. Br. J. Clin. Pharmacol (1994) 38:405–410.
   PubMed Web of Science ®Google Scholar
• BROWNE MJ, MAYER KH, CHAFEE SBD et al: 2',3'-didehydro-2',3'-dideoxythymidine (d4T) in patients with AIDSor AIDS-related complex: a Phase I trial. J. Infect. Dis. (1993) 167:21–29.
   Google Scholar
• First clinical activity data.
   Google Scholar
• MURRAY HW, SQUIRES KE, WEISS W et al: Stavudine in patients with AIDS or AIDS-related complex: AIDS Clini-cal Trials Group 089.1 Infect. Dis. (1995) 171\(Suppl. 2):5123–130.
   Google Scholar
• SKOWRON G: Biologic effects and safety of stavudine: overview of Phase I and II clinical trials. J. Infect. Dis.(1995) 171 (Suppl. 2):5113–117.
   Google Scholar
• The Phase I/II studies.
   Google Scholar
• PETERSEN EA, RAMIREZ-RONDA CH, HARDY WD et al.: Dose-related activity of stavudine in patients infected with the human immunodeficiency virus. J. Infect. Dis. (1995) 171 (Suppl. 2):5131–139.
   Google Scholar
• CALVEZ V, FAUVEAU V, FERCHAL F et al.: Virological efficacy of stavudine vs. placebo in early HIV infection. 3rd Conference on Refroviruses and Opportunistic Infections. Washington (28 January - 1 February 1996). Abstract 142.
   Google Scholar
• HAMMER SM, KATZENSTEIN DA, HUGHES MD eta].: A trial comparing nucleoside monotherapy with combination therapy in HIV-infected adults with CD4 cell counts from 200–500 per cubic millimeter. New Engl. J. Med. (1996) 335:1081–1090.
   Google Scholar
• GOTTLIEB M, PETERSON D, ADLER M eta].: Comparison of safety and efficacy of two doses of stavudine (Zerit, d41) in a large simple trial in the US parallel track program. 35th Interscience Conference on Antimicrobial Agents and Chemotherapy. San Francisco (17–20 September 1995). Abstract 1171.
   Google Scholar
• PAVIA AT, GATHE J, THE BMS-019 STUDY GROUP et al:
   Google Scholar
• ••Clinical efficacy of stavudine (d4T, Zerifi compared tozidovudine (ZDV, Retrovir) in ZDV-pre-treated HIV positive patients. 35th Intel-science Conference on Antimi-crobial Agents and Chemotherapy. San Francisco (17–20 September 1995). Abstract 1169.
   Google Scholar
• The clinical end-point study.
   Google Scholar
• DELTA CO-ORDINATING COMMITTEE: DELTA: a random-ised double-blind controlled trial comparing combina-tions of zidovudine plus didanosine or zalcitabine or zidovudine alone in HIV infected individuals. Lancet (1996) 348:283–288.
   PubMed Web of Science ®Google Scholar
• POLLARD R, PETERSON D, HARDY D et al.: Antiviral effect and safety of stavudine (d4T) and didanosine (ddl) combination therapy in HIV-infected subjects in an ongoing pilot randomized double-blinded bial. 3rd Conference on Retroviruses and Opportunistic Infections. Washington DC (28 January - 1 February 1996). Abstract 197.
   Google Scholar
• Stavudine's potential as combination drug.
   Google Scholar
• PENDEAULT L, ELTON R, ADLER M et al: Stavudine (d4T), didanosine (ddl) and nelfinavir combination therapy in HIV-infected subjects: antiviral effect and safety in an ongoing pilot study. 4th Conference on Retroviruses and Opportunistic Infections. Washington DC (22–26 January 1997). Abstract 241.
   Google Scholar
• SAIMOT AG, LANDMAN R, DAMOND F et al: Ritonavir, stavudine (d4T), didanosine (ddl) as a triple combina-tion treatment in antiretrovir al-naive patients. 4th Con-ference on Retroviruses and Opportunistic Infections. Washington DC (22–26 January 1997). Abstract 246.
   Google Scholar
• MARS ME, GENSOLLEN S, RAVAUX L et al: Association between AZT and d4T in HIV infected patients: a pilot study (comparison with d4T, AZT, and AZT/ddl). 35th Intel-science Conference on Antimicrobial Agents and Che-motherapy San Francisco (17–20 September 1995). Abstract 1118.
   Google Scholar
• KATLAMA C, VALANTIN MA, CALVEZ V eta].: ALTIS: a pilot open study of d4T/3TC in antiretroviral-naive and -ex-perienced patients. 4th Conference on Retroviruses and Opportunistic Infections. Washington DC (22–26 January 1997). Abstract LB4.
   Google Scholar
• FOUDRAINE N, DE WOLF F, HOETELMANS R et al.: CSF and serum HIV RNA levels during AZT/3TC and d4T/3TC treatment. 4th Conference on Retroviruses and Opportunis-tic Infections. Washington DC (22–26 January 1997). Abstract LB5.
   Google Scholar
• NOVAK RM, COLOMBO J, LINARES-DIAZ M, MORIERA L: Comparison of AZT/3TC vs. d4T/3TC for the treatment of HIV in persons with CD4 counts 300 and prior AZT experience. Xlth International Conference on AIDS. Van-couver (7–12 July 1996). Abstract Tu.B. 2132.
   Google Scholar
• DE TRUCHIS P, ZUCHMAN D, DUPONT C et al: Combina-tion therapy with d4T + 3TC + indinavir (IDV) in nucleoside-experienced HIV-infected patients: an open label study. 4th Conference on Retroviruses and Opportun-istic Infections. Washington DC (22–26 January 1997). Ab-stract 247.
   Google Scholar
• GATHE J, Jr., BURKHARDT B, HAWLEY P et al: A random-ized Phase II study of Viracept, a novel HIV protease inhibitor used in combination with stavudine (d4T) vs. stavudine (d4T) alone. Xlth International Conference on AIDS. Vancouver (7–12 July 1996). Abstract Mo.B. 413.
   Google Scholar
• RUTSCHMANN OT, KAISER L, FATHI M, PERRIN L: Adding saquinavir to d4T in advanced HIV infected patients. 3rd International Congress on Drug Therapy in HIV Infection. Birmingham (3–7 November 1996). Abstract p41.
   Google Scholar
• MOYLE GJ, NELSON MR, HAWKINS D, GAZZARD BG: The use and toxicity of didanosine (ddl) in HIV antibody positive individuals intolerant to zidovudine (AZT). Quart J. Med. (1993) 86:155–163.
   PubMedGoogle Scholar
• MOYLE GJ, GOLL A, SNAPE S et al.: Safety and tolerability of zalcitabine (ddC) in patients with AIDS or advanced AIDS-related complex inthe European expanded access programme. Int. J. Antimicrob. Agents (1996) 7:41–48.
   PubMed Web of Science ®Google Scholar
• PORTEGIES P: AIDS dementia complex: a review. J. Acquk. Immune Defic. Syndr. (1994) 7\(Suppl. 2):538–S49.
   Google Scholar
• MOYLE G: Activity and role of lamivudine in the treat-ment of adults with human immunodeficiency virus type 1 infection: a review. Exp. Opin. Invest Drugs (1996) 5:913–924.
   Google Scholar