Drug intelligence / Profile preview

bupivacaine + meloxicam

Development stage
Approved
Lead developer
Heron Therapeutics
Modality
Small Molecules
Administration
Instillation
01

Overview

Zynrelef (bupivacaine and meloxicam) is an extended-release, fixed-dose combination of the amide local anesthetic bupivacaine and the nonsteroidal anti-inflammatory drug (NSAID) meloxicam. Developed by Heron Therapeutics, it is specifically formulated for needle-free instillation into the surgical site to provide analgesia for up to 72 hours post-surgery. The mechanism of action is synergistic: bupivacaine blocks voltage-gated sodium channels to prevent the generation and conduction of nerve impulses, while meloxicam inhibits cyclooxygenase-2 (COX-2) to reduce prostaglandin synthesis and local inflammation. This reduction in inflammation helps maintain a higher local pH, which enhances the efficacy of bupivacaine. The Allegheny Singer Research Institute has conducted prospective cohort studies evaluating its use in robot-assisted total knee arthroplasty (RATKA) to assess its impact on postoperative pain and opioid consumption.

Brand names
Zynrelef
Other names
bupivacaine/meloxicam extended-releaseHTX-011HTX011HTX 011
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)NaV (Voltage-gated sodium channels)

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