Absorption and excretion of a new antidepressive (SQ 10,996) in humans

A single oral dose of 10 mg of SQ 10,996-14C was absorbed slowly by 3 normal male volunteers, with peak plasma concentrations achieved 6 hr after ingestion; the plasma half-life was about 38.5 hr. On average, 82.3 +/- 3.5% of the radioactivity present in the 2 hr plasma sample was bound to plasma proteins. These volunteers excreted an average of 31 and 52% of the dose in the urine and feces, respectively. All subjects excreted minor amounts of 14CO2 in the expired air. No unchanged SQ 10,996-14C was found in the urine. Three unidentified metabolites were excreted in urine. SQ 10,996-14C was excreted in the feces only as unchanged drug, suggesting that the drug is incompletely absorbed. The volunteers tolerated the drug well and experienced no adverse effects.