biostudies-literatureBurkard UBoehringer Ingelheim International GmbH87-99https://www.ebi.ac.uk/biostudies/studies/S-EPMC8901509biostudies-literatureUnknown42(1)BACKGROUND AND OBJECTIVES: BI 425809, a novel glycine transporter-1 inhibitor, may ameliorate cognitive deficits in schizophrenia. The objectives of the studies were: to assess absolute bioavailability of oral BI 425809 compared with intravenous (IV) microtracer infusion (study 1), and to determine the mass balance, distribution, metabolism, and excretion of BI 425809 (study 2).<h4>Methods</h4>These were Phase I, open-label, non-randomized, single-period, single-arm studies in healthy males. Study 1 administered a single oral dose of unlabeled BI 425809 25 mg, then an IV microtracer infusion of [¹⁴C]-BI 425809 30 µg. In study 2, participants received an oral dose of [¹⁴C]-BI 425809 25 mg containing [¹⁴C]-labeled (dose: 3.7 megabecquerel (0.41 mSv)) and unlaClinical drug investigationThe Absolute Bioavailability, Absorption, Distribution, Metabolism, and Excretion of BI 425809 Administered as an Oral Dose or an Oral Dose with an Intravenous Microtracer Dose of [¹⁴C]-BI 425809 in Healthy Males.PMC89015091346-0016Study numbers 1346-0015Desch MTeitelbaum AMShatillo YWunderlich GSchlecker CLiu PMack SRBurkard UChan TSfalseThe Absolute Bioavailability, Absorption, Distribution, Metabolism, and Excretion of BI 425809 Administered as an Oral Dose or an Oral Dose with an Intravenous Microtracer Dose of [¹⁴C]-BI 425809 in Healthy Males.BACKGROUND AND OBJECTIVES: BI 425809, a novel glycine transporter-1 inhibitor, may ameliorate cognitive deficits in schizophrenia. The objectives of the studies were: to assess absolute bioavailability of oral BI 425809 compared with intravenous (IV) microtracer infusion (study 1), and to determine the mass balance, distribution, metabolism, and excretion of BI 425809 (study 2).<h4>Methods</h4>These were Phase I, open-label, non-randomized, single-period, single-arm studies in healthy males. Study 1 administered a single oral dose of unlabeled BI 425809 25 mg, then an IV microtracer infusion of [¹⁴C]-BI 425809 30 µg. In study 2, participants received an oral dose of [¹⁴C]-BI 425809 25 mg containing [¹⁴C]-labeled (dose: 3.7 megabecquerel (0.41 mSv)) and unla2022-01-01T00:00:00Z2022 Jan2026-05-09T03:22:37.276Z2025-02-19T03:46:49.156ZS-EPMC89015093493605510.1007/s40261-021-01111-9