Chemical Compound Review:
Daraprim 5-(4-chlorophenyl)-6-ethyl- pyrimidine-2,4...
Synonyms:
Daraclor, Malocide, Chloridin, Tindurine, pyrimethamine, ...
- Toxoplasmic encephalitis in patients with the acquired immunodeficiency syndrome. Members of the ACTG 077p/ANRS 009 Study Team. Luft, B.J., Hafner, R., Korzun, A.H., Leport, C., Antoniskis, D., Bosler, E.M., Bourland, D.D., Uttamchandani, R., Fuhrer, J., Jacobson, J. N. Engl. J. Med. (1993)
- Falciparum malaria despite pyrimethamine/suifadoxine in five tourists to East Africa. Eichenlaub, D., Rogler, G., Hoffmann, H.G., Weise, H.J. Lancet (1982)
- Stevens-Johnson syndrome due to pyrimethamine/sulfadoxine during presumptive self-therapy of malaria. Phillips-Howard, P.A., Behrens, R.H., Dunlop, J. Lancet (1989)
- NIH conference. Recent advances in the management of AIDS-related opportunistic infections. Lane, H.C., Laughon, B.E., Falloon, J., Kovacs, J.A., Davey, R.T., Polis, M.A., Masur, H. Ann. Intern. Med. (1994)
- Twice-weekly maintenance therapy with sulfadiazine-pyrimethamine to prevent recurrent toxoplasmic encephalitis in patients with AIDS. Spanish Toxoplasmosis Study Group. Podzamczer, D., Miró, J.M., Bolao, F., Gatell, J.M., Cosín, J., Sirera, G., Domingo, P., Laguna, F., Santamaría, J., Verdejo, J. Ann. Intern. Med. (1995)
- The critical period of pyrimethamine teratogenesis in the rat. Izumi, H., Kokue, E., Hayama, T. Nippon Juigaku Zasshi (1984)
- Transfection of the primate malaria parasite Plasmodium knowlesi using entirely heterologous constructs. van der Wel, A.M., Tomás, A.M., Kocken, C.H., Malhotra, P., Janse, C.J., Waters, A.P., Thomas, A.W. J. Exp. Med. (1997)
- Decreased sensitivity of artesunate and chloroquine of Plasmodium falciparum infecting hemoglobin H and/or hemoglobin constant spring erythrocytes. Yuthavong, Y., Butthep, P., Bunyaratvej, A., Fucharoen, S. J. Clin. Invest. (1989)
- Sulfadoxine/pyrimethamine alone or with amodiaquine or artesunate for treatment of uncomplicated malaria: a longitudinal randomised trial. Dorsey, G., Njama, D., Kamya, M.R., Cattamanchi, A., Kyabayinze, D., Staedke, S.G., Gasasira, A., Rosenthal, P.J. Lancet (2002)
- Amodiaquine, sulfadoxine/pyrimethamine, and combination therapy for treatment of uncomplicated falciparum malaria in Kampala, Uganda: a randomised trial. Staedke, S.G., Kamya, M.R., Dorsey, G., Gasasira, A., Ndeezi, G., Charlebois, E.D., Rosenthal, P.J. Lancet (2001)
- Failure of dapsone/pyrimethamine plus chloroquine against falciparum malaria in Papua New Guinea. Edstein, M.D., Veenendaal, J.R., Rieckmann, K.H., O'Donoghue, M. Lancet (1988)
- Molecular basis of differential resistance to cycloguanil and pyrimethamine in Plasmodium falciparum malaria. Peterson, D.S., Milhous, W.K., Wellems, T.E. Proc. Natl. Acad. Sci. U.S.A. (1990)
- Alteration of mitochondrial gene expression and disruption of respiratory function by the lipophilic antifolate pyrimethamine in mammalian cells. Sprecher, H., Barr, H.M., Slotky, J.I., Tzukerman, M., Eytan, G.D., Assaraf, Y.G. J. Biol. Chem. (1995)
- Primary prophylaxis for Pneumocystis carinii pneumonia: a randomized trial comparing cotrimoxazole, aerosolized pentamidine and dapsone plus pyrimethamine. Mallolas, J., Zamora, L., Gatell, J.M., Miró, J.M., Vernet, E., Valls, M.E., Soriano, E., SanMiguel, J.G. AIDS (1993)
- Point mutations may account for pyrimethamine resistance. Ash, C. Trends Pharmacol. Sci. (1989)
- Amino acid changes linked to pyrimethamine resistance in the dihydrofolate reductase-thymidylate synthase gene of Plasmodium falciparum. Cowman, A.F., Morry, M.J., Biggs, B.A., Cross, G.A., Foote, S.J. Proc. Natl. Acad. Sci. U.S.A. (1988)
- Stable molecular transformation of Toxoplasma gondii: a selectable dihydrofolate reductase-thymidylate synthase marker based on drug-resistance mutations in malaria. Donald, R.G., Roos, D.S. Proc. Natl. Acad. Sci. U.S.A. (1993)
- Evidence that a point mutation in dihydrofolate reductase-thymidylate synthase confers resistance to pyrimethamine in falciparum malaria. Peterson, D.S., Walliker, D., Wellems, T.E. Proc. Natl. Acad. Sci. U.S.A. (1988)
- Role of clindamycin in the treatment of central nervous system toxoplasmosis. Rolston, K.V., Hoy, J. Am. J. Med. (1987)
- Competitive inhibition of folate absorption by dihydrofolate reductase inhibitors, trimethoprim and pyrimethamine. Zimmerman, J., Selhub, J., Rosenberg, I.H. Am. J. Clin. Nutr. (1987)
- In vitro activities of novel antifolate drug combinations against Plasmodium falciparum and human granulocyte CFUs. Winstanley, P.A., Mberu, E.K., Szwandt, I.S., Breckenridge, A.M., Watkins, W.M. Antimicrob. Agents Chemother. (1995)
- Sulfadoxine specific lymphocyte transformation in a patient with eosinophilic pneumonia induced by sulfadoxine-pyrimethamine (Fansidar). Daniel, P.T., Holzschuh, J., Berg, P.A. Thorax (1989)
- Efficacy of artesunate plus pyrimethamine-sulphadoxine for uncomplicated malaria in Gambian children: a double-blind, randomised, controlled trial. von Seidlein, L., Milligan, P., Pinder, M., Bojang, K., Anyalebechi, C., Gosling, R., Coleman, R., Ude, J.I., Sadiq, A., Duraisingh, M., Warhurst, D., Alloueche, A., Targett, G., McAdam, K., Greenwood, B., Walraven, G., Olliaro, P., Doherty, T. Lancet (2000)
- Plasmodium falciparum cross-resistance between trimethoprim and pyrimethamine. Iyer, J.K., Milhous, W.K., Cortese, J.F., Kublin, J.G., Plowe, C.V. Lancet (2001)
- Use of pyrimethamine-sulfadoxine (Fansidar) in prophylaxis against chloroquine-resistant Plasmodium falciparum and Pneumocystis carinii. Pearson, R.D., Hewlett, E.L. Ann. Intern. Med. (1987)
- Crystal structure of dihydrofolate reductase from Plasmodium vivax: pyrimethamine displacement linked with mutation-induced resistance. Kongsaeree, P., Khongsuk, P., Leartsakulpanich, U., Chitnumsub, P., Tarnchompoo, B., Walkinshaw, M.D., Yuthavong, Y. Proc. Natl. Acad. Sci. U.S.A. (2005)
- Bifunctional thymidylate synthase-dihydrofolate reductase in protozoa. Ivanetich, K.M., Santi, D.V. FASEB J. (1990)
- Translational up-regulation of antifolate drug targets in the human malaria parasite Plasmodium falciparum upon challenge with inhibitors. Nirmalan, N., Sims, P.F., Hyde, J.E. Mol. Biochem. Parasitol. (2004)
- Toxoplasma gondii induces the secretion of monocyte chemotactic protein-1 in human fibroblasts, in vitro. Brenier-Pinchart, M.P., Pelloux, H., Simon, J., Ricard, J., Bosson, J.L., Ambroise-Thomas, P. Mol. Cell. Biochem. (2000)
- Antifolate resistance associated with loss of MRP1 expression and function in Chinese hamster ovary cells with markedly impaired export of folate and cholate. Stark, M., Rothem, L., Jansen, G., Scheffer, G.L., Goldman, I.D., Assaraf, Y.G. Mol. Pharmacol. (2003)
- DHFR and DHPS genotypes of Plasmodium falciparum isolates from Gabon correlate with in vitro activity of pyrimethamine and cycloguanil, but not with sulfadoxine-pyrimethamine treatment efficacy. Aubouy, A., Jafari, S., Huart, V., Migot-Nabias, F., Mayombo, J., Durand, R., Bakary, M., Le Bras, J., Deloron, P. J. Antimicrob. Chemother. (2003)
- Stable transfection of malaria parasite blood stages. van Dijk, M.R., Waters, A.P., Janse, C.J. Science (1995)
- Kinetic and molecular properties of the dihydrofolate reductase from pyrimethamine-sensitive and pyrimethamine-resistant clones of the human malaria parasite Plasmodium falciparum. Chen, G.X., Mueller, C., Wendlinger, M., Zolg, J.W. Mol. Pharmacol. (1987)
- Disposition of intravenous pyrimethamine in healthy volunteers. Almond, D.S., Szwandt, I.S., Edwards, G., Lee, M.G., Winstanley, P.A. Antimicrob. Agents Chemother. (2000)
- Isocratic reversed-phase HPLC method to measure pyrimethamine extracted from plasma of infants treated for toxoplasmosis. Zytkovicz, T.H., Salter, J., Hennigan, L., Timperi, R., Maguire, J., Hoff, R. Clin. Chem. (1991)