Naldemedine

DB11691ApprovedInvestigationalSmall moleculeOpioid Antagonists

Naldemedine is an opioid antagonist used to to treat opioid-induced constipation. It is a modified form of DB00704 to which a side chain has been added to increase molecular weight and polar surface area resulting in restricted transport across the blood brain barrier.

Mechanism: Naldemedine binds to and antagonizes mu-, delta-, and kappa-opioid receptors. The binding of opioid agonists to peripheral mu-opioid receptors slows the transit of feces through the intestine resulting in constipation. By antagonizing mu-opioid receptors, naldemedine inhibits this effect.
Curator reviewed
Primary indication: For the treatment of opioid-induced constipation.Curator reviewed · 1 structured indication
Formula / weight: C₃₂H₃₄N₄O₆ · 570.646 g/mol (avg)
First approval: United States, 2017 · European Union, 2020
Code names: S-297995
Brand names: Rizmoic
Symproic

Resolves to

Compound

UNII03KSI6WLXHCAS916072-89-4ChEMBLCHEMBL2105755PubChem54732242

Clinical / RWD

RxNorm1876597ATCA06AH05

Structure

InChIKeyAXQACEQYCPKDMV-RZAWKFBISA-NSMILES[H][C@@]12OC3=C4C(C[C@@]5([H])N(CC6CC6)CC[C@@]14[C@@]5(O)CC(C(=O)NC(C)(C)C1=NC(=NO1)C1=CC=CC=C1)=C2O)=CC=C3O

Targets

P41143OPRD1P41145OPRK1P35372OPRM1

Transporters

Q2M3G0ABCB5

What you can answer from here — as of September 13, 2026

3Protein targetsEach mapped to UniProt, with action and pharmacological action

Listed above

1TransporterSubstrate / inhibitor direction, not just membership

Listed above

784Drug interactionsStructured to mechanism, not free text

10Clinical trialsPhase, status and sponsor resolved per trial

1Structured indicationCondition, population, route and combination as fields, not prose