Drug intelligence / Profile preview

tapentadol

Development stage
Approved
Lead developer
Grünenthal
Modality
Small Molecules
Administration
Oral
01

Overview

Tapentadol is a centrally acting synthetic opioid analgesic used to treat moderate to severe pain, including neuropathic pain associated with diabetic peripheral neuropathy. It is available in both immediate-release and extended-release formulations (Nucynta, Nucynta ER). Tapentadol has a dual mechanism of action as both a mu-opioid receptor agonist and a norepinephrine reuptake inhibitor. This unique profile allows it to address both nociceptive and neuropathic pain. Unlike tramadol, tapentadol does not significantly affect serotonin reuptake. Tapentadol was first approved by the FDA in 2008 for the management of severe pain when alternative treatments are inadequate[1][3][5][7].

Brand names
NucyntaNucynta ER
Other names
R331333R-331333R 331333
02

Targets

MOR (Mu opioid receptor)NET (Norepinephrine Transporter)

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