Drug intelligence / Profile preview

polmacoxib + tramadol

Development stage
Preclinical
Lead developer
Crystal Genomics
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Polmacoxib + tramadol is a fixed-dose combination drug composed of two active pharmaceutical ingredients: polmacoxib, a selective cyclooxygenase-2 (COX-2) inhibitor with additional high-affinity binding to carbonic anhydrase, and tramadol, an opioid analgesic. This combination is designed for the treatment of acute and chronic pain. Polmacoxib provides anti-inflammatory and analgesic effects primarily through COX-2 inhibition, reducing prostaglandin synthesis involved in pain and inflammation. Tramadol acts as a centrally acting opioid agonist at the mu-opioid receptor and also inhibits reuptake of norepinephrine and serotonin, contributing to its analgesic properties. The rationale for combining these agents is to achieve synergistic pain relief with potentially reduced side effects compared to higher doses of either agent alone[1][2][3][4][6].

02

Targets

SERT (Sodium-dependent serotonin transporter)CA1 (Carbonic anhydrase 1)MOR (Mu opioid receptor)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)CA2 (Carbonic Anhydrase 2)NET (Norepinephrine Transporter)

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