Drug intelligence / Profile preview

bupivacaine + meloxicam + ropivacaine

Development stage
Preclinical
Lead developer
Heron Therapeutics
Modality
Small Molecules
Administration
Topical, Transdermal, Local Instillation, Infiltration
01

Overview

This is a **combination drug** involving the local anesthetics **bupivacaine** and **ropivacaine** with the nonsteroidal anti-inflammatory drug (NSAID) **meloxicam**. *Bupivacaine* and *ropivacaine* act as sodium channel blockers that prevent the initiation and transmission of nerve impulses, providing localized anesthesia and analgesia. *Meloxicam* inhibits cyclooxygenase-2 (COX-2), decreasing the synthesis of prostaglandins and thus reducing inflammation and pain. Each agent contributes distinct, complementary mechanisms: bupivacaine and ropivacaine block nociceptive signaling at the site of administration, while meloxicam reduces inflammatory mediators that sensitize nerves post-injury. While bupivacaine + meloxicam is an FDA-approved combination (Zynrelef) for postsurgical pain, and experimental and transdermal systems exist for ropivacaine + meloxicam, there is currently no widely recognized single product that contains all three agents. However, the rationale for combining them is to provide potent, long-duration local anesthesia and anti-inflammatory effects for improved post-operative pain control[2][3][4][5].

02

Targets

NaV (Voltage-gated sodium channels)PTGER1 (Prostaglandin E Receptor 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PGHS-1 (Prostaglandin G/H Synthase 1)

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