naldemedine (symproic) Report issue

Small molecule Approved FDA
AACT ChEMBL DrugBank Drugs@FDA PubChem

Active Ingredient History

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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

Chemistry

  • 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
  • InChIKey: AXQACEQYCPKDMV-RZAWKFBISA-N
  • Mol. Mass: 570.65
  • ALogP: 3.48
  • ChEMBL Molecules:
    naldemedine  
    naldemedine tosylate  
More Chemistry

Pharmacology

  • 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.

Alternative names

naldemedine | naldemedine tosylate | s-297995 | symproic

Organizations (6)

Research & Development (5)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (2)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (4)

Approved Indications (1)


 

Constipation

Experimental Indications - Clinical Trial Phases 1-4 (3)


 

Intestinal Neoplasms (Phase 2)

Opioid-Induced Constipation (Phase 3)

Pancreatitis (Phase 2/Phase 3)

Overview

  • Highest Phase: Phase 3
  • # of Trials: 8
  • # of Trial Organizations: 5

Trials by Phase

Trial Phase Start Date Organizations Indications

Feedback

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