Sucunamostat (SCO-792) hydrochloride is an orally active, reversible inhibitor of enteropeptidase, displaying inhibition constants (IC50) of 4.6 nM for rat enteropeptidase and 5.4 nM for human enteropeptidase. In vitro, it dissociates slowly from enteropeptidase, while in vivo, it hinders protein digestion [1].

Sucunamostat hydrochloride, administered orally in single doses of 10 and 30 mg/kg, effectively and dose-dependently inhibited the elevation of plasma branched-chain amino acids (BCAA) induced by oral protein doses in rats [1]. Pharmacokinetic parameters in male Sprague-Dawley rats for Sucunamostat hydrochloride showed the following values: PO (10 mg/kg) and IV (2 mg/kg) resulted in a C max (ng/mL) of 6.60 ± 1.36 and 564 ± 58, respectively; T max (h) was 1.7 ± 0.6; AUC 0-24 (ng/mL·h) was 54.1 ± 7.5 for PO and 303 ± 23 for IV; AUC inf (ng/mL·h) was 49.8 ± 5.4 for PO and 304 ± 30 for IV; the Vd SS (mL/kg) was recorded at 1290 ± 299; CL p (mL/min/kg) at 663 ± 66; and bioavailability was calculated at 0.4% [1].