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Trulicity ® (dulaglutid) injektion
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The use of DPP-4 inhibitors, such as sitagliptin, in combination with dulagutide, was not evaluated in the clinical studies assessing dulaglutide.
Coadministration of Dulaglutide With Sitagliptin
An open-label, 2-period, crossover, clinical pharmacology study was done in 29 patients with T2DM that evaluated the mutual effects on the PK of both dulaglutide 1.5 mg and sitagliptin 100 mg.1
Potential for Dulaglutide to Influence the Pharmacokinetics of Sitagliptin
Dulaglutide delays gastric emptying and has the potential to impact the rate of absorption of concomitantly administered oral medicinal products.2
Sitagliptin exposure was unaffected when coadministered with a single dose of dulaglutide. Following coadministration with 2 consecutive doses of dulaglutide, resulted in a decrease of the sitagliptin
AUC(0-τ) and by approximately 7.4 %
Cmax by approximately 23.1 %,.
Sitagliptin tmax increased approximately 0.5 hours following coadministration with dulaglutide compared to sitagliptin alone.2
Based on the analysis, no clinically significant effect on the PK of sitagliptin was seen and no dose adjustment was recommended for sitagliptin when coadministered with dulaglutide (Figure 1).1
Figure 1. Impact of Dulaglutide on the Pharmacokinetics of Coadministered Dipeptidyl Peptidase-4 Inhibitor, Sitagliptin1
Abbreviations:
AUC = area under the time-concentration curve; Cmax = maximum
concentration; PK = pharmacokinetic.
Note: Reference group is
coadministered medication given alone.
Potential for Coadministered Sitagliptin to Influence the Pharmacokinetics of Dulaglutide
Sitagliptin can produce up to 80 % inhibition of DPP‑4 over a 24‑hour period.2
Compared to dulaglutide being taken alone, the coadministration of a single dose of dulaglutide 1.5 mg with steady-state sitagliptin 100 mg resulted in dulaglutide's increase in
the area under the AUC by approximately 38%
Cmax by approximately 27%, and
Therefore, dulaglutide does have a high degree of protection against DPP‑4 inactivation. The increased exposure may enhance the effects of dulaglutide on blood glucose levels.2
1. Geiser J, de la Peña A, Cui X, et al. No dose adjustment is needed when coadministering dulaglutide with once-daily sitagliptin. Poster presented at: American Society for Clinical Pharmacology and Therapeutics (ASCPT) Annual Meeting: March 15-18, 2017; Washington, D.C.
2. Trulicity [summary of product characteristics]. Eli Lilly Nederland B.V., The Netherlands.
Glossary
AUC = area under the curve
Cmax = maximum plasma concentration
DPP-4 = dipeptidyl peptidase-4
GLP-1 RA = glucagon-like peptide-1 receptor agonist
PK = pharmacokinetic
T2DM = type 2 diabetes mellitus
Tmax = time to maximum concentration
Datum fӧr senaste ӧversyn 2020 M01 08