Phase I study of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine maleate (MN-1695), a new anti-ulcer agent.

A phase I study of 2,4-diamino-6-(2,5-dichlorophenyl)-s-triazine (MN-1695), which is expected to have an anti-ulcer effect, was performed in 14 healthy male subjects. The safety and pharmacokinetics were examined in single-dose oral administration of 1, 2, 4, 8 and 16 mg/body and multiple-dose administration of 2 mg/body/day, once daily, for 28 consecutive days. As for the subjective symptoms, only light headache, general malaise and heart burn were observed in two out of 4 subjects in the 16-mg group. No abnormalities were found in blood pressure, pulse rate, respiratory rate, body temperature, body weight and ECG both in single- and multiple-dose studies. No abnormal changes attributed to this drug appeared in hematological and biochemical examinations and urinalysis. Times for reaching the maximum plasma concentration in the single-dose study were 3.5, 8 and 3.3 h in 4-, 8- and 16-mg groups, respectively. The elimination half-lives from the plasma were 152, 145 and 148 h for the 3 groups, respectively. The plasma concentration curves in the multiple-dose study were similar to those simulated with the pharmacokinetic parameters obtained in the single-dose study. The plasma concentration increased until the 14th day, as the administration continued, and reached steady state thereafter; there seemed to be no abnormal cumulation. The elimination patterns after multiple-dose administration were almost the same as those in the single-dose study; the half-life was about 170 h.(ABSTRACT TRUNCATED AT 250 WORDS)