• PPB(plasma protein-binding):3 concentrations (including effective concentrations),N=3, focusing on concentration dependence and species differences.
• Metabolic stability/MetID (in vitro metabolism): Metabolic stability/ METID (in vitro metabolism): Focuses on species differences to provide a reference for PK/PD/Tox species selection in vivo
• CYP inhibition (P450p system): IC50 or Ki, 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4
• CYP induction (P450 induction): human hepatocytes from 3 donors, mRNA expression and/or enzyme activity changes:1A2, 2B6, 3A4 (refer to FDA Guidances: DD2006 Draft and 2020 In vitro DDI for data analysis)
• Reaction phenotyping: Identification of CYP/Non-CYP metabolic pathways
• Caco-2: In vitro absorption model
• Transporter substrate assessment & inhibition (Transporter study):
(1) P-gp, BCRP
(2) Liver transporters (OATP1B1, OATP1B3)
(3) Kidney transporters (OAT1, POAT3, OCT2, MATE1, MATE2-K)
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