Drug intelligence / Profile preview

VX-150

Development stage
Phase 2
Lead developer
Vertex
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

VX-150 is an orally bioavailable pro-drug developed for the treatment of pain. It rapidly converts in the body to its active form, which is a highly selective inhibitor of the voltage-gated sodium channel NaV1.8, with over 400-fold selectivity compared to other sodium channel subtypes[1][3][4][5]. By inhibiting NaV1.8, VX-150 reduces neuronal excitability and repetitive firing associated with nociceptor hyperexcitability and central sensitization—key mechanisms underlying both acute and chronic pain[3][6]. Clinical studies have shown that VX-150 provides significant analgesic effects in various experimental pain models as well as in patients undergoing bunionectomy surgery or suffering from neuropathic pain[2][3][6]. The drug has demonstrated good safety and tolerability profiles in clinical trials.

Other names
VRT-1207355 (active moiety)VRT-1268114 (study code)
02

Targets

SCN10A (Sodium channel protein type X alpha subunit)

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