Naldemedine

CHEMBL2105755 Phase 4 Approved Small molecule

Half-Life

—

Bioavailability

—

Protein Binding

—

Molecular Weight

570.6 g/mol

LogP

3.2

Phase

4

Used to relieve constipation caused by opioid pain medications, this drug blocks opioid receptors specifically in the gut without affecting pain relief in the brain. It helps restore normal bowel function in people taking opioids for chronic pain.

Molecular Weight

570.6000 g/mol

LogP

3.20

TPSA

141.00 Å²

Lipinski RO5

Pass

Therapeutic Areas

Bladder Cancer Breast Cancer Colorectal Cancer Non-Small Cell Lung Cancer Ovarian Cancer Pancreatic Cancer Prostate Cancer Thyroid Cancer

Mechanism of Action

Binds to mu (μ), kappa (κ), and/or delta (δ) opioid receptors in the central and peripheral nervous system, mimicking endogenous endorphins. Activation of these G-protein-coupled receptors inhibits pain signal transmission and modulates the emotional response to pain.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Mechanism

Binds to mu (μ), kappa (κ), and/or delta (δ) opioid receptors in the central and peripheral nervous system, mimicking endogenous endorphins. Activation of these G-protein-coupled receptors inhibits pain signal transmission …

2D Structure

SVG PNG

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SMILES

CC(C)(NC(=O)C1=C(O)[C@@H]2Oc3c(O)ccc4c3[C@@]23CCN(CC2CC2)[C@H](C4)[C@]3(O)C1)c1nc(-c2ccccc2)no1

InChI

InChI=1S/C32H34N4O6/c1-30(2,29-33-27(35-42-29)18-6-4-3-5-7-18)34-28(39)20-15-32(40)22-14-19-10-11-21(37)25-23(19)31(32,26(41-25)24(20)38)12-13-36(22)16-17-8-9-17/h3-7,10-11,17,22,26,37-38,40H,8-9,12-16H2,1-2H3,(H,34,39)/t22-,26+,31+,32-/m1/s1

Molecular Formula

C32H34N4O6

HBD / HBA

4 / 9

Rotatable Bonds

6

Heavy Atoms

42

No targets recorded

Target interaction data is not yet available for this drug.

No interactions recorded

Drug interaction data is not yet available for this compound.

No side effects recorded

Side effect data is not yet available for this drug.

Frequently Asked Questions

Used to relieve constipation caused by opioid pain medications, this drug blocks opioid receptors specifically in the gut without affecting pain relief in the brain. It helps restore normal bowel function in people taking opioids for chronic pain.

Binds to mu (μ), kappa (κ), and/or delta (δ) opioid receptors in the central and peripheral nervous system, mimicking endogenous endorphins. Activation of these G-protein-coupled receptors inhibits pain signal transmission and modulates the emotional response to pain.

Yes, Naldemedine is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.

{# References & Data Sources section for drug detail pages. Renders standard pharmacological database links plus the drug's data_sources field. #}

References & Data Sources

ChEMBL — European Bioinformatics Institute (EBI). CHEMBL2105755. Open-access bioactivity database.
PubChem — National Center for Biotechnology Information (NCBI). CID 54732242. Chemical information database.

Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.

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Structure

Quick Data

Formula: C32H34N4O6
Synonyms: 1

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Medical Disclaimer

This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.

Data sources: ChEMBL, PubChem, DailyMed.