Ocular Pharmacology and Toxicology of TRPV1 Antagonist SAF312 (Libvatrep).

ABSTRACT:

Purpose

To evaluate the pharmacology and toxicology of SAF312, a transient receptor potential vanilloid 1 (TRPV1) antagonist.

Methods

TRPV1 expression in human ocular tissues was evaluated with immunohistochemistry. Inhibition of calcium influx in Chinese hamster ovary (CHO) cells expressing human TRPV1 (hTRPV1) and selectivity of SAF312 were assessed by a fluorescent imaging plate reader assay. Ocular tissue and plasma pharmacokinetics (PK) were assessed following a single topical ocular dose of SAF312 (0.5%, 1.0%, 1.5%, 2.5%) in rabbits. Safety and tolerability of SAF312 were evaluated in rabbits and dogs. Effects of SAF312 on corneal wound healing after photorefractive keratectomy (PRK) surgery were assessed in rabbits.

Results

TRPV1 expression was noted in human c

SUBMITTER: Mogi M 

PROVIDER: S-EPMC10484039 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature