Send to

Choose Destination
Expert Opin Drug Metab Toxicol. 2015 Jan;11(1):7-14. doi: 10.1517/17425255.2015.982531. Epub 2014 Nov 26.

Evaluation of pharmacokinetic and pharmacodynamic interactions of canagliflozin and teneligliptin in Japanese healthy male volunteers.

Author information

Department of Clinical Pharmacology, Development Division, Mitsubishi Tanabe Pharma Corporation , 17-10 Nihonbashi-Koamicho, Chuo-ku, Tokyo 103-8405 , Japan +81 3 6748 7763 ; +81 3 3663 6449 ;



To investigate the pharmacokinetic/pharmacodynamic interactions of the antidiabetic agents canagliflozin (a sodium-glucose cotransporter-2 inhibitor) and teneligliptin (a dipeptidyl peptidase-4 inhibitor) in Japanese healthy adult men.


Open-label, one-way crossover study used canagliflozin (200 mg/day p.o.) and teneligliptin (40mg/day p.o). A single dose of object drug (either canagliflozin or teneligliptin) was administered on day 1 followed by washout and continuous administration of precipitant drug (days 1 - 9). Both drugs were concomitantly administered on day 7.


No changes in AUC0 - 72h and Cmax were observed for canagliflozin+teneligliptin versus monotherapy; geometric mean ratios for AUC0 - 72h and Cmax were 0.982 and 0.982 for the plasma concentration of canagliflozin and 0.983 and 0.976 for the plasma concentration of teneligliptin, respectively. Plasma concentrations of active and total glucagon-like peptide-1 (GLP-1) increased with canagliflozin+teneligliptin versus teneligliptin alone. Mean AUC0.5 - 4h increased post-meal, on combination therapy, from 9.6 to 12.5 pmol·h/l (active GLP-1) and from 21.5 to 32.3 pmol·h/l (total GLP-1). Adverse events developed in four subjects; all were mild and resolved but one subject withdrew due to generalized erythema.


GLP-1 levels increased with the canagliflozin+teneligliptin combination, and no PK interaction was observed. This combination may show favorable antidiabetic effects without increasing systemic exposure.


DPP-4 inhibitor; SGLT2 inhibitor; canagliflozin; drug-drug interaction; teneligliptin

[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Taylor & Francis
Loading ...
Support Center