Naloxegol

Summary

Naloxegol (CHEMBL2219418) is an approved small-molecule μ-opioid receptor antagonist (ATC A06AH03); indicated across 5 conditions including constipation disorder and ileus.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A06AH03
• Indications: 5 conditions
• Clinical trials: 34
• Chemistry: 651.8 Da · C34H53NO11

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2219418
Name	Naloxegol
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	56959087
ChEBI	CHEBI:82975
ATC	A06AH03
Molecular formula	C34H53NO11
Molecular weight	651.8
InChIKey	XNKCCCKFOQNXKV-ZRSCBOBOSA-N

SMILES: COCCOCCOCCOCCOCCOCCOCCO[C@H]1CC[C@]2([C@H]3CC4=C5[C@]2([C@H]1OC5=C(C=C4)O)CCN3CC=C)O

IUPAC name: (4R,4aS,7S,7aR,12bS)-7-[2-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]-3-prop-2-enyl-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-4a,9-diol

ChEBI definition: An organic heteropentacyclic compound that is naloxone in which the keto group is replaced by a PEG moiety. Used for treatment of opioid-induced constipation.

Pharmacological roles (ChEBI): μ-opioid receptor antagonist, cathartic.

Also known as: AZ-13337019, Moventig, Naloxegol, NKTR-118, NALOXEGOL, naloxegol, Naloxegol (oxalate)

Parent form; salt/anhydrous children: CHEMBL2219416

Patent coverage: 157 distinct patent families (372 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Mu-type opioid receptor, Delta-type opioid receptor.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
OPRM1	6.4	IC50	398.1	nM	CHEMBL_ACT_29322747
OPRD1	6.2	IC50	631	nM	CHEMBL_ACT_29322843

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

1 approved indication. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

Indication	Phase	MONDO	EFO
constipation disorder	4	MONDO:0002203	HP:0002019

4 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
ileus	3	MONDO:0004567	MONDO:0004567
brain injury	3	MONDO:0043510	MONDO:0043510
opiate dependence	2	MONDO:0005530	EFO:0005611
non-small cell lung carcinoma	2	MONDO:0005233	EFO:0003060

Clinical trials

Total trials: 34.

Phase distribution

Phase	Trials
PHASE1	10
PHASE3	8
Not specified	7
PHASE4	4
PHASE2	4
PHASE2/PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02839889	PHASE4	TERMINATED	Tolerability, Safety, and Feasibility of Naloxegol in Patients With Cancer and OIC (Opioid Induced Constipation)
NCT02977286	PHASE4	TERMINATED	Naloxegol to Prevent Lower Gastrointestinal Paralysis in Critically Ill Adults Administered Opioids
NCT03235739	PHASE4	COMPLETED	Ancillary Effects of Oral Naloxegol (Movantik)
NCT05770960	PHASE4	COMPLETED	Colonic Motor Patterns in Healthy Volunteers
NCT05008926	PHASE3	RECRUITING	The NIPA Study Naloxegol Administration to Prevent Opioids Induced Gastrointestinal Motility Disturbance in Brain Injured PAtients
NCT01309841	PHASE3	COMPLETED	Assessment of Efficacy and Safety in Patients With Non-cancer-related Pain and Opioid-induced Constipation
NCT01323790	PHASE3	COMPLETED	Assessment of Efficacy and Safety in Patients With Non-cancer-related Pain and Opioid-induced Constipation
NCT01336205	PHASE3	COMPLETED	Assessment of Long-term Safety in Patients With Non-cancer-related Pain and Opioid-induced Constipation
NCT01384292	PHASE3	TERMINATED	Assessment of Efficacy and Safety in Relieving Opioid-induced Constipation in Patients With Cancer-related Pain
NCT01395524	PHASE3	COMPLETED	A 12-week Extension of the Phase III Study (D3820C00004) to Assess the Effect and Safety of NKTR-118 in Patients With Non-cancer-related Pain and Opioid-induced Constipation
NCT02705378	PHASE3	WITHDRAWN	The Effect of Naloxegol on Refractory Constipation in the Intensive Care Unit
NCT03316859	PHASE2/PHASE3	UNKNOWN	Naloxegol and Opioid-induced Constipation
NCT04433390	PHASE3	COMPLETED	Effect of Naloxegol on Postoperative Ileus in Patients Undergoing Cardiac Surgery
NCT00600119	PHASE2	COMPLETED	A Phase 2, Double-Blind, Multiple-Dose Escalation Study to Evaluate NKTR-118 (Oral PEG-Naloxol) in Patients With Opioid-Induced Constipation (OIC)
NCT02745353	PHASE2	TERMINATED	Naloxegol in Cancer Opioid-Induced Constipation
NCT02998606	PHASE2	TERMINATED	Movantik for Opioid-Related Esophageal Disorders
NCT03087708	PHASE2	TERMINATED	Naloxegol in Treating Patients With Stage IIIB-IV Non-small Cell Lung Cancer
NCT01318655	PHASE1	COMPLETED	Single and Multiple Ascending Dose Study for NKTR-118 and Cross-over Study to Investigate the Effect of Food for NKTR-118 in Japanese Healthy Subjects
NCT01325415	PHASE1	COMPLETED	A Placebo-controlled Four Way Crossover Study to Asses the Effect of a Single Oral Dose of NKTR-118 on QTc Interval in Healthy Male Subjects
NCT01348724	PHASE1	COMPLETED	Absorption, Distribution, Metabolism and Excretion (ADME) Study With Single Oral Administration of [14C] NKTR-118
NCT01392807	PHASE1	COMPLETED	Open-label Study to Assess the Pharmacokinetics of NKTR-118 in Patients With Impaired Hepatic Function
NCT01520896	PHASE1	COMPLETED	Study in Healthy Volunteers to Investigate the Effects of Ketoconazole on the Pharmacokinetics of NKTR-118
NCT01533870	PHASE1	COMPLETED	Study in Healthy Volunteers to Investigate the Effects of Rifampin on the Pharmacokinetics of NKTR-118
NCT01594619	PHASE1	COMPLETED	Study in Healthy Volunteers to Investigate the Effects of Diltiazem on the Pharmacokinetics of Naloxegol
NCT01623609	PHASE1	COMPLETED	Open Label, Healthy Volunteers, Bioequivalence Study With Naloxegol
NCT02099591	PHASE1	COMPLETED	Phase I Pharmacokinetics and Safety Study of Naloxegol in Paediatric OIC Patients
NCT02737059	PHASE1	COMPLETED	Effect of Naloxegol on Gastric, Small Bowel, and Colonic Transit in Healthy Subjects
NCT03720613	Not specified	RECRUITING	Risk of Major Adverse Cardiovascular Events for Naldemedine & Other Medications for Opioid Induced Constipation
NCT02813148	Not specified	COMPLETED	Naloxegol Drug Utilization Post Authorisation Safety Study
NCT02813356	Not specified	UNKNOWN	Naloxegol US PMR CV Safety.
NCT02813369	Not specified	TERMINATED	Naloxegol Health Outcome Post Authorisation Safety Study
NCT03638440	Not specified	COMPLETED	Real World Observational Study of Naloxegol for Patients With Cancer Pain Diagnosed With OIC.
NCT04173858	Not specified	COMPLETED	Evaluation of the Quality of Life of Patients With Opioid-induced Constipation Under Treatment With Naloxegol
NCT04294550	Not specified	COMPLETED	Study on Quality of Life in Advanced Cancer Patients With Opioid-induced Constipation Treated With Naloxegol

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).