Melarsoprol

Melarsoprol, a melaminophenylarsine-type trivalent organic arsenical, is an important agent for African trypanosomiasis. Melarsoprol inhibits the growth of lymphoid leukemic cell by inducing apoptosis. Melarsoprol crosses the blood-brain barrier^[1][2][3]. In Vitro: Melarsoprol (1-100 nM; 24-96 h) causes a dose- and time-dependent inhibition of survival and growth in lymphoid leukemic cells^[2].
Melarsoprol (10-100 nM; 24 h) exhibits morphologic characteristics of apoptosis^[2].
Melarsoprol (1-100 nM; 24 h) inhibits the expression of bcl-2 mRNA and protein^[2].
In Vivo: In mice, the organic solution of Melarsoprol (0.039 mmol/kg), injected intravenously as control formulation, is found to concentrate significantly in the bone marrow (C_max = 1.64 mmol/g), though, the brain concentration is quite high (C_max = 0. 093 mmol/g) and the LD₅₀ is 0.12 mmol/kg^[3].