The antitumor activity of 2-[bis-(2-chloroethyl)-amino]
ethanesulfonic acid (also referred to here as "
taurine mustard" or "
taumustine") was evaluated in the murine P388 and L1210
lymphocytic leukemias and in the pigmented and nonpigmented
B16 melanoma systems. Treatment with a single ip dose of
taumustine (40 mg/kg) resulted in
a 130% increase in life-span for mice bearing P388 (intraperitoneal), a 93% increase for mice bearing L1210 (intraperitoneal), and an approximately 80% increase for mice bearing
B16 melanoma (intraperitoneal). Repeated low doses (10 mg/kg) of
taumustine promoted a 250% increase in life-span for mice bearing P388 (intraperitoneal), the absence of ascitic fluid from day 4 onward, and the presence of pulmonary emboli from day 5 onward. The inclusion of
taurine (5 mM) in the culture medium of P388 cells in primary culture for 45 hours did not alter the cytotoxicity of
taumustine, and pretreatment of the
tumor-bearing host with
taurine (250 mg/kg) in daily treatments with
taumustine for up to 8 days did not interfere with antitumor activity (140-160% increased life-span). However, treatment of
tumor-bearing mice with
taurine abrogated neurotoxicity, intestinal
necrosis, pulmonary emboli formation, and tail vein
necrosis due to the administration of
taumustine. The modulation by
taurine of
taumustine activity suggests that the combination of these agents offers an advantage of selectivity and host protection during
chemotherapy.