Drug intelligence / Profile preview

VX-708 + midazolam

Development stage
Unknown
Lead developer
Vertex
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination of **VX-708**, a small molecule voltage-gated sodium channel inhibitor developed by Vertex Pharmaceuticals for acute pain, and **midazolam**, a benzodiazepine commonly used as an anesthetic, sedative, and for drug-drug interaction studies. VX-708 acts by blocking voltage-gated sodium channels to reduce neuronal excitability associated with pain transmission. Midazolam is mainly used for its central nervous system depressant actions, acting as a positive allosteric modulator at the gamma-aminobutyric acid type A (GABA-A) receptor. In the context of combination studies, midazolam is frequently administered to evaluate the potential of investigational drugs to affect CYP3A enzyme activity, because midazolam is a sensitive CYP3A substrate. Trials have used this combination to assess the pharmacokinetics, pharmacodynamics, and safety of VX-708, especially for the evaluation of drug-drug interactions affecting hepatic metabolism.

02

Targets

NaV (Voltage-gated sodium channels)

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