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CG 5503;tapentadol

Johnson & Johnson Pharmaceutical Research & Development, L.L.C. · Phase 3 active Small molecule

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

Tapentadol is a mu-opioid receptor agonist and norepinephrine reuptake inhibitor that provides analgesia through dual mechanisms. Used for Moderate to severe acute pain, Moderate to severe chronic pain.

At a glance

Generic nameCG 5503;tapentadol
SponsorJohnson & Johnson Pharmaceutical Research & Development, L.L.C.
Drug classOpioid analgesic with norepinephrine reuptake inhibition
TargetMu-opioid receptor; norepinephrine transporter
ModalitySmall molecule
Therapeutic areaPain Management
PhasePhase 3

Mechanism of action

Tapentadol binds to mu-opioid receptors in the central nervous system to produce opioid-mediated pain relief, while simultaneously inhibiting the reuptake of norepinephrine, which enhances descending pain inhibitory pathways. This dual mechanism allows for effective analgesia at lower doses compared to pure opioid agonists, potentially reducing opioid-related side effects.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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