In Vitro ADME and Preclinical Pharmacokinetics of Ulotaront, a TAAR1/5-HT 1A Receptor Agonist for the Treatment of Schizophrenia

• Published in: Pharmaceutical research Vol. 39; no. 5; p. 837
• Main Authors: Xiao, Guangqing, Chen, Yu-Luan, Dedic, Nina, Xie, Linghong, Koblan, Kenneth S, Galluppi, Gerald R
• Format: Journal Article
• Language: English
• Published: United States 01.05.2022
• Subjects: drug-drug interactions; blood–brain barrier; CYP2D6; TAAR1; phenotyping; ulotaront

Ulotaront (SEP-363856) is a TAAR1 agonist with 5-HT agonist activity currently in clinical development for the treatment of schizophrenia. The objectives of the current study were to characterize the in vitro ADME properties, preclinical PK, and to evaluate the DDI potential of ulotaront and its maj...