Drug intelligence / Profile preview

tapentadol + pregabalin

Development stage
Phase 4
Lead developer
Grünenthal
Modality
Small Molecules
Administration
Oral
01

Overview

Tapentadol + pregabalin is a combination therapy of two centrally acting analgesic agents used to manage chronic pain, particularly in conditions with a neuropathic component such as osteoarthritis and chronic low back pain. Tapentadol acts as both a mu-opioid receptor agonist and norepinephrine reuptake inhibitor, restoring descending noradrenergic inhibitory tone and inhibiting nociceptive transmission at the spinal cord level. Pregabalin binds to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system, modulating the release of excitatory neurotransmitters and reducing neuronal hyperexcitability. When administered together, these drugs target different mechanisms involved in centrally driven chronic pain, providing superior analgesia by restoring inhibitory control while also reducing spinal neuronal hyperexcitability[1][2][4][5].

02

Targets

MOR (Mu opioid receptor)NET (Norepinephrine Transporter)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)

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