Drug intelligence / Profile preview

Exparel (Pacira BioSciences, 27f347)

Development stage
Unknown
Lead developer
Pacira BioSciences
Modality
Small Molecules, Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Local Infiltration, Perineural
01

Overview

Exparel is a long-acting, liposomal formulation of the local anesthetic bupivacaine, developed by Pacira BioSciences. It utilizes the proprietary DepoFoam delivery system, which consists of a multivesicular liposomal platform (a honeycomb-like structure of phospholipids, cholesterol, and triglycerides) that encapsulates the active drug. This technology allows for the sustained release of bupivacaine over an extended period, typically providing postsurgical analgesia for up to 72 hours. The drug functions by binding to and blocking voltage-gated sodium channels on the internal surface of nerve cell membranes, preventing the influx of sodium ions and thereby inhibiting the generation and conduction of nerve impulses. Exparel is FDA-approved for single-dose infiltration into the surgical site to produce postsurgical local analgesia and as an interscalene brachial plexus nerve block for postsurgical regional analgesia. The University of Missouri-Columbia is currently conducting a Phase 4 trial to evaluate its efficacy specifically in reducing opioid utilization following lumbar spine surgeries.

Brand names
Exparel
Other names
liposomal bupivacainebupivacaine liposome injectable suspensionbupivacaine liposomal
02

Targets

NaV (Voltage-gated sodium channels)

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