Drug intelligence / Profile preview

PF-06882961 + midazolam

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

**PF-06882961 + midazolam** refers to the co-administration of two drugs: PF-06882961 (also known as danuglipron), an oral small-molecule agonist of the glucagon-like peptide-1 receptor (GLP-1R) developed to treat type 2 diabetes mellitus and obesity, and midazolam, a short-acting benzodiazepine commonly used as a sedative, anxiolytic, and as a probe drug for assessing CYP3A4 (cytochrome P450 3A4) enzyme activity. This combination is primarily investigated in pharmacokinetic interaction studies to assess the impact of PF-06882961 on the metabolism of midazolam, a CYP3A4 substrate. PF-06882961 exerts its action by activating the GLP-1 receptor, mimicking the action of endogenous GLP-1, enhancing insulin secretion, suppressing glucagon secretion, and reducing appetite[1][2][4][5]. Midazolam works as a positive allosteric modulator at GABA-A receptors, resulting in sedative and anxiolytic effects.

02

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