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Either single (50 mg) or multiple ( 25 mg/day •~ 4 days) dose of etretinate was administered orally into 5 healthy volunteers once a day 30 minutes after breakfast. After the administration with a single dose of 50 mg or the initial dose of 25 mg, the AUC (Area Under the 'Curve) of the blood level of unchanged etretinate was 1,305 ng •Ehr/ml with 50 mg and 267 ng •Ehr /ml with 25 mg. The approximate half-life was 2 hr with 25 mg and 3.6 hr with 50 mg. The AUC of the main metabolite, Ro 10-1670, was 2.7 times as large as that of unchanged etretinate with the first dose of 25 mg, but the AUC with 50 mg was merely 1.5 times as large as that with the first dose of 25 mg. On the 4 th day of the administration with 25 mg/day, the AUC of unchanged etretinate became 1.6 times as large as the 1 st day, but the AUC of the main metabolite was decreased on the 4 th day down to 61 % of the level on the 1st day. The amount equivalent to 49% (28.0-66. %) of the dose was excreted into feces. Fecal excretion rate was 3.3 %for the main metabolite. No changed etretinate nor its main metabolite was detected in the urine. Main adverse reactions attributable to etretinate were itching

Pharmacokinetics of Etretinate in Healthy Volunteers After Oral Administration of Single and Mutiple Doses