Disease relevance of Melarsomine

• A 36-kDa protein was isolated by affinity chromatography using Cymelarsan, an arsenical drug currently used in African trypanosomiasis treatment, as ligand [1].
• A dose of 0.25 mg/kg body weight of Cymelarsan given i/m is recommended [2].

High impact information on Melarsomine

• We also show that a laboratory line of Trypanosoma brucei gambiense, adapted to high levels of resistance for the melaminophenyl arsenical drug melarsamine hydrochloride (Cymelarsan), had similarly lost TbAT1 and HAPT1 activity while retaining LAPT1 activity [3].
• MS was used to identify residues of glycerol-3-phosphate dehydrogenase bound by Cymelarsan; they are not conserved in the mammalian enzyme [1].
• Trypanosoma brucei: lack of cross-resistance to melarsoprol in vitro by cymelarsan-resistant parasites [4].
• Alteration to one of three adenosine transporters is associated with resistance to cymelarsan in Trypanosoma evansi [5].
• A population of Trypanosoma brucei brucei with reduced sensitivity to melarsenoxide cysteamine (Mel Cy) was produced in immunosuppresed mice using subcurative drug treatment [6].

Biological context of Melarsomine

• Our data also raise the possibility that conventional treatment regimens should be reevaluated and support the presence of at least two drug-resistance mechanisms in T. evansi and T. equiperdum, single drug resistance (berenil), and cross-resistance (berenil and cymelarsan) [7].

Analytical, diagnostic and therapeutic context of Melarsomine

• Cymelarsan (Mel Cy) at 0.25 mg/kg to 3.0 mg/kg by intramuscular injection [8].
• Evaluation of the efficacy of melarsenoxyde cysteamine (Cymelarsan) in treatment of camels experimentally infected with Trypanosoma evansi using antigen trapping enzyme-linked immunosorbent assay [9].

References