Drug intelligence / Profile preview

midazolam + PF-03716539

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Intranasal
01

Overview

Midazolam is a short-acting benzodiazepine used for sedation, anxiolysis, amnesia, and as an adjunct to anesthesia. It acts as a positive allosteric modulator at the GABA(A) receptor benzodiazepine binding site, enhancing the inhibitory effect of gamma-aminobutyric acid (GABA) in the central nervous system. It is indicated for preoperative sedation, procedural sedation, induction of anesthesia, and acute seizure management[1][2][3][4][5][7]. PF-03716539 (also known as PF 3716539) is an investigational small molecule developed by Pfizer and ViiV Healthcare. Its primary development has been for pharmacokinetic enhancement of anti-infective drugs by inhibiting CYP3A4 enzyme activity in vivo. Clinical studies have evaluated its potential to inhibit CYP3A4 and assess drug-drug interactions with antiretrovirals such as darunavir or maraviroc[6][8]. The combination "midazolam + PF-03716539" would be used primarily in clinical research settings to evaluate drug-drug interactions mediated via CYP3A4 inhibition.

Other names
midazolamPF 3716539PF3716539PF-3716539
02

Targets

CYP3A4 (Cytochrome P450 3A4)

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