Pharmacokinetic–pharmacodynamic (dipeptidyl peptidase‐4 inhibition) model to support dose rationale in diabetes patients, including those with renal impairment, for once‐weekly administered omarigliptin

• Published in: British journal of clinical pharmacology Vol. 85; no. 12; pp. 2759 - 2771
• Main Authors: Jain, Lokesh, Chain, Anne S.Y., Tatosian, Daniel A., Hing, Jeremy, Passarell, Julie A., Kauh, Eunkyung A., Lai, Eseng
• Format: Journal Article
• Language: English
• Published: England John Wiley and Sons Inc 01.12.2019
• Subjects: Blood Glucose - analysis; Clinical Trials as Topic; Diabetes Mellitus, Type 2 - blood; Diabetes Mellitus, Type 2 - complications; Diabetes Mellitus, Type 2 - drug therapy; Dipeptidyl Peptidase 4 - blood; dipeptidyl peptidase‐4 inhibitor; Dipeptidyl-Peptidase IV Inhibitors - administration & dosage; Dipeptidyl-Peptidase IV Inhibitors - blood; Dipeptidyl-Peptidase IV Inhibitors - therapeutic use; Dose-Response Relationship, Drug; Drug Administration Schedule; Heterocyclic Compounds, 2-Ring - administration & dosage; Heterocyclic Compounds, 2-Ring - blood; Heterocyclic Compounds, 2-Ring - therapeutic use; Humans; Hypoglycemic Agents - administration & dosage; Hypoglycemic Agents - blood; Hypoglycemic Agents - therapeutic use; Kidney Failure, Chronic - blood; Kidney Failure, Chronic - complications; Kidney Failure, Chronic - drug therapy; Models, Biological; omarigliptin; Original; population pharmacodynamics; population pharmacokinetics; Pyrans - administration & dosage; Pyrans - blood; Pyrans - therapeutic use; Renal Insufficiency - blood; Renal Insufficiency - complications; Renal Insufficiency - drug therapy; type 2 diabetes mellitus; type 2 diabetes mellitus; dipeptidyl peptidase-4 inhibitor; population pharmacodynamics; omarigliptin; population pharmacokinetics
• ISSN: 0306-5251; 1365-2125; 1365-2125
• DOI: 10.1111/bcp.14103

Aims To characterize the population pharmacokinetics (PK) and pharmacodynamics (PD) of the once‐weekly dipeptidyl peptidase‐4 (DPP‐4) inhibitor omarigliptin in healthy subjects and patients with type 2 diabetes mellitus, and use these models to support the dosing recommendation for patient labelling...