Drug intelligence / Profile preview

bupivacaine + celecoxib

Development stage
Preclinical
Lead developer
Heron Therapeutics
Modality
Implantable Devices → Device-based Delivery → Drug Delivery Systems, Small Molecules, Transdermal Patches → Device-based Delivery → Drug Delivery Systems, Inhalation Devices → Device-based Delivery → Drug Delivery Systems
Administration
Injection (local/peripheral/nerve Block), Topical/local Application At Surgical Site[2]
01

Overview

This is a combination drug consisting of bupivacaine, an amide-type local anesthetic, and celecoxib, a selective nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase-2 (COX-2). Bupivacaine acts by reversibly blocking voltage-gated sodium channels in neuronal membranes, thereby inhibiting nerve impulse transmission and providing local or regional anesthesia. Celecoxib selectively inhibits COX-2 to reduce the synthesis of prostaglandins involved in inflammation and pain signaling. The combination is designed for enhanced pain control—bupivacaine provides immediate local anesthesia while celecoxib offers sustained anti-inflammatory and analgesic effects. This type of formulation may be used for perioperative or postoperative pain management, potentially as a long-acting depot or slow-release system administered locally at the surgical site[2][7][5].

Other names
盐酸布比卡因 + 塞来昔布
02

Targets

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

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