Abstract

Background: Tegoprazan is a potassium channel inhibitor with an anti-acid secretion effect. It is metabolized by CYP3A4, a cytochrome enzyme the occurrence of which in the Mexican population, differs from that in some other populations. Since the efficacy and safety studies on tegoprazan have been conducted in Koreans, it is of considerable clinical importance to establish whether differences exist in CYP3A4 metabolism between the two populations.
Aims: To evaluate the oral pharmacokinetics of tegoprazan and to compare the pharmacokinetic data with those reported in the literature for Koreans.
Materials and methods: The investigation was carried out in a cohort of 20 healthy Mexican volunteers (11 women and 9 men), who were administered a dose of 50 mg after fasting for at least 10 hours. Blood samples were taken at selected time points over 24 hours, and tegoprazan plasma concentrations measured using high-performance liquid chromatography. Pharmacokinetic parameters were compared to those in Koreans reported in the literature.
Results: Tegoprazan is rapidly absorbed from the gastrointestinal tract reaching C_max at ~ 1 hour post dose (t_max) and is removed from the circulation with an average half-life of ~ 4 hours. The pharmacokinetic parameters obtained were similar to those obtained in Koreans including elimination half-life, maximum tegoprazan concentrations, and oral bioavailability.
Discussion and conclusion: Since no clinically relevant pharmacokinetic differences were observed in the pharmacokinetics of tegoprazan, a substrate for CYP3A4, between Mexicans and Koreans, it is concluded that the efficacy and safety data for tegoprazan obtained in Koreans will be valid in the Mexican population.

Author Details

Authors

• Miriam del Carmen Carrasco-Portugal¹
• Gisselle Vanessa González-Hernández²
• Pablo David López-Cartagena²
• Francisco Javier Flores-Murrieta^{1, 3}

Departments

• ¹ Laboratorio de Farmacología Clínica y Experimental, Instituto Nacional de Enfermedades Respiratorias Ismael Cosío Villegas,
• ² Productos Científicos, S.A. de C.V., and
• ³ Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina del Instituto Politécnico Nacional, Mexico

Address

Francisco Javier Flores-Murrieta, PhD, FCP
Laboratorio de Farmacología Clínica y Experimental
Instituto Nacional de Enfermedades Respiratorias Ismael Cosío
Villegas Calzada de Tlalpan 4502
Alcaldía Tlalpan, Ciudad de México. C.P. 14080, Mexico
Email: [email protected]

Citation