Drug intelligence / Profile preview

articaine

Development stage
Approved
Lead developer
Hoechst
Modality
Small Molecules
Administration
Dental, Infiltration, Epidural, Intrathecal
01

Overview

Articaine is a **small-molecule amide local anesthetic** used primarily for local and regional anesthesia, especially in dentistry, and is also being developed in a topical ophthalmic formulation. Pharmacologically, it blocks **voltage-gated sodium channels** in peripheral nerves, preventing initiation and propagation of action potentials and thereby producing reversible loss of sensation. Unlike many other amide anesthetics, articaine contains a thiophene ring and an additional ester group, which contributes to rapid tissue penetration and hydrolysis. Publicly verifiable development activity includes American Genomics' **AG-920**, an articaine sterile topical ophthalmic solution studied in Phase 1 and Phase 3 trials for ocular surface anesthesia, while marketed dental products include articaine hydrochloride formulations, commonly combined with epinephrine for infiltration or nerve block anesthesia.

Brand names
OrablocSeptanestUbistesinUltracain
Other names
articaine hydrochloride阿替卡因
02

Targets

SCN4A (Voltage-gated sodium channel protein type 4 subunit alpha)SCN10A (Sodium channel protein type X alpha subunit)SCN9A (Sodium channel protein type 9 subunit alpha)

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