Drug intelligence / Profile preview

bupivacaine + calcitonin + fentanyl

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Peptides, Small Molecules, Recombinant Proteins and Enzymes
Administration
Intrathecal, Epidural
01

Overview

This is a combination of three drugs—bupivacaine, calcitonin, and fentanyl—used for analgesia. Bupivacaine is an amide-type local anesthetic that blocks voltage-gated sodium channels in neuronal membranes, inhibiting nerve impulse conduction and providing regional anesthesia or analgesia. Fentanyl is a potent synthetic opioid agonist primarily targeting the mu opioid receptor to produce strong analgesic effects by inhibiting pain signal transmission in the central nervous system. Calcitonin is a peptide hormone that inhibits osteoclastic bone resorption and has been explored for its potential analgesic properties, possibly through modulation of inflammatory mediators and direct action on central pain pathways. The combination aims to provide synergistic or additive pain relief by targeting different mechanisms involved in nociception and inflammation[1][2][6][9].

02

Targets

KOR (Kappa opioid receptor)CALCR (Calcitonin receptor)NaV (Voltage-gated sodium channels)MOR (Mu opioid receptor)DOR (Opioid Receptor Delta 1)

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