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May 1, 20260 citations

Assessment of the Drug-Drug Interaction Potential of Lotiglipron (PF-07081532) with Midazolam, Omeprazole, Dabigatran, Rosuvastatin, and the Oral Contraceptives Levonorgestrel and Ethinyl Estradiol.

CCCarol Cronenberger NANeeta B. AminPfizer (United States)VLVu LePfizer (United States)

Key Points

This research aims to evaluate the drug-drug interaction potential of lotiglipron with various medications.
Conducted two Phase 1 studies to assess drug interactions.
Investigated co-administration effects on liver transaminase levels.
Terminated studies early due to safety concerns regarding elevated transaminases.
31% of participants in Study 1 showed elevated liver transaminases (>3 × ULN).
19% of participants in Study 2 exhibited similar transaminase elevations.
Both studies were prematurely terminated due to safety issues associated with metabolic drug interactions.

Abstract

) following co-administration with semaglutide. Across both studies a subset of lotiglipron-treated participants (31% and 19% in Studies 1 and 2, respectively) had elevations in liver transaminases (alanine/aspartate aminotransferase >3 × ULN), which (based on PK data) were associated with reduced ability of the liver to transport/metabolize drugs cleared by multiple pathways. Based on the results of the two Phase 1 studies reported here along with the results of a Phase 2 study where transaminases elevations were also noted, both Phase 1 studies were prematurely terminated along with the clinical development of lotiglipron. ClinicalTrials.gov identifiers: NCT05671653; NCT05788328.

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