Active Ingredient History

  • Now
Naldemedine (Symproic) is an opioid antagonist indicated for the treatment of opioid-induced constipation (OIC) in adult patients with chronic non-cancer pain. Naldemedine is an opioid antagonist with binding affinities for mu-, delta-, and kappa-opioid receptors. Naldemedine functions as a peripherally-acting mu-opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids. Naldemedine is a derivative of naltrexone to which a side chain has been added that increases the molecular weight and the polar surface area, thereby reducing its ability to cross the blood-brain barrier (BBB). Naldemedine is also a substrate of the P-glycoprotein (P-gp) efflux transporter. Based on these properties, the CNS penetration of naldemedine is expected to be negligible at the recommended dose levels, limiting the potential for interference with centrally-mediated opioid analgesia. Naldemedine was approved in 2017 in both the US and Japan for the treatment of Opioid-induced Constipation.   NCATS

  • SMILES: CC(C)(NC(=O)C1=C(O)[C@@H]2Oc3c(O)ccc4C[C@H]5N(CC6CC6)CC[C@@]2(c34)[C@@]5(O)C1)c7onc(n7)c8ccccc8
  • Mol. Mass: 570.65
  • ALogP: 3.48
  • ChEMBL Molecules:
More Chemistry
  • Mechanism of Action:
  • Multi-specific: Missing data
  • Black Box: No
  • Availability: Prescription Only
  • Delivery Methods: Oral
  • Pro Drug: No

Drug Pricing (per unit)

United States

$5.8283 - $12.6630
More Pricing Detail

Note: This drug pricing data is preliminary, incomplete, and may contain errors.

naldemedine | naldemedine tosylate | s-297995 | symproic


Data collection and curation is an ongoing process for CDEK - if you notice any information here to be missing or incorrect, please let us know! When possible, please include a source URL (we verify all data prior to inclusion).

Report issue