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Tapentadol Prolonged Release

Grünenthal GmbH · FDA-approved active Small molecule

Tapentadol is a mu-opioid receptor agonist and noradrenaline reuptake inhibitor that provides analgesia through dual mechanisms.

Tapentadol prolonged release, developed by Grünenthal GmbH, is an opioid analgesic for moderate to severe chronic pain. It has completed several Phase 3 and 4 trials, demonstrating efficacy and safety in various pain conditions, including osteoarthritis and low back pain. The drug lacks an FDA label but has been studied extensively in Europe.

At a glance

Generic nameTapentadol Prolonged Release
Also known as- Nucynta, - Palexia, Nucynta, Palexia, Nucynta®
SponsorGrünenthal GmbH
Drug classMu-opioid receptor agonist and noradrenaline reuptake inhibitor
TargetMu-opioid receptor; noradrenaline transporter (NET)
ModalitySmall molecule
Therapeutic areaPain Management
PhaseFDA-approved

Mechanism of action

Tapentadol binds to mu-opioid receptors to produce opioid-mediated pain relief while simultaneously inhibiting the reuptake of noradrenaline, enhancing descending pain inhibitory pathways. The prolonged-release formulation provides sustained analgesia over 24 hours, allowing for twice-daily dosing. This dual mechanism may offer improved tolerability compared to pure mu-opioid agonists.

Approved indications

Common side effects

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