Disease relevance of Epiroprim

• On the basis of these results, PS-15 and epiroprim combined with dapsone are candidates for use for the prevention of both pneumocystosis and toxoplasmosis [1].
• Used alone, dapsone and epiroprim, each at a dose of 50 mg/kg of body weight per day, protected 10 and 0% of the mice, respectively [2].
• In combination with dapsone epiroprim led to a complete cure of toxoplasmosis in mice [3].
• The antimicrobial effects of a new dihydrofolate reductase inhibitor, epiroprim, either singly or in combination with dapsone against Mycobacterium leprae, were evaluated in vivo using a mouse footpad model [4].

High impact information on Epiroprim

• Antibacterial activities of epiroprim, a new dihydrofolate reductase inhibitor, alone and in combination with dapsone [5].
• In a rat model of dual infection, we studied such dihydrofolate reductase (DHFR) inhibitors as PS-15 (25 mg/kg of body weight), epiroprim (100 mg/kg), and pyrimethamine (3 mg/kg) alone or in combination with various doses of dapsone (50, 25, or 5 mg/kg) for the prevention of pneumocystosis and toxoplasmosis [1].
• Epiroprim (EPM; Ro 11-8958) is a new selective inhibitor of microbial dihydrofolate reductase [5].

Chemical compound and disease context of Epiroprim

• Synergistic combinations of Ro 11-8958 and other dihydrofolate reductase inhibitors with sulfamethoxazole and dapsone for therapy of experimental pneumocystosis [6].

Biological context of Epiroprim

• The 50% inhibitory concentration (IC50) of epiroprim for T. gondii dihydrofolate reductase was 0.9 micromole, similar to that of pyrimethamine, but epiroprim was 650-fold more selective than pyrimethamine for T. gondii compared with human dihydrofolate reductase [7].

Analytical, diagnostic and therapeutic context of Epiroprim

• The favorable results achieved with Ro 11-8958 indicate that it should be considered for clinical trials [6].
• Simple HPLC determination of the concentrations of epiroprim in the serum and brains of mice [8].
• A pilot study on the efficacy of epiroprim against developmental stages of Toxoplasma gondii and Pneumocystis carinii in animal models [3].

References