U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C34H53NO11
Molecular Weight 651.7847
Optical Activity UNSPECIFIED
Defined Stereocenters 5 / 5
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of NALOXEGOL

SMILES

COCCOCCOCCOCCOCCOCCOCCO[C@H]1CC[C@@]2(O)[C@H]3CC4=C5C(O[C@@H]1[C@@]25CCN3CC=C)=C(O)C=C4

InChI

InChIKey=XNKCCCKFOQNXKV-ZRSCBOBOSA-N
InChI=1S/C34H53NO11/c1-3-9-35-10-8-33-30-26-4-5-27(36)31(30)46-32(33)28(6-7-34(33,37)29(35)25-26)45-24-23-44-22-21-43-20-19-42-18-17-41-16-15-40-14-13-39-12-11-38-2/h3-5,28-29,32,36-37H,1,6-25H2,2H3/t28-,29+,32-,33-,34+/m0/s1

HIDE SMILES / InChI
Molecular Formula C34H53NO11
Molecular Weight 651.7847
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 5 / 5
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/24896818; http://www.nektar.com/product_pipeline/cns_pain_oral_naloxegol_nktr118.html

MOVANTIK (naloxegol) is a peripherally-acting mu-opioid receptor antagonist indicated for the treatment of opioid-induced constipation (OIC) in adult patients with chronic noncancer pain. It is being investigated for the treatment of constipation as a side effect of prescription opioid pain medicines.

CNS Activity

CNS Non-penetrant
1040
Curator's Comment: Naloxegol at high doses in animals has considerable CNS effects. These exposures were in excess of what can be expected in humans at the labeled recommended doses.

Originator

Nektar Therapeutics
2
Curator's Comment: Naloxegol was developed using Nektar's oral small molecule polymer conjugate technology.In September 2009, AstraZeneca and Nektar Therapeutics entered into a worldwide agreement for naloxegol. Under Nektar's agreement with AstraZeneca, AstraZeneca is responsible for development and commercialization. MOVANTIK is a trademark and MOVENTIG is a registered trademark of the AstraZeneca group of companies.

Approval Year

2014
503
Targets

Targets

Primary TargetPharmacologyConditionPotency
Mu-type opioid receptor
61
Target ID: P35372|||G8XRH8|||Q5TDA1|||Q9UN57
Gene ID: 4988.0
Gene Symbol: OPRM1
Target Organism: Homo sapiens (Human)
Antagonist
2849
 7.4 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
Approved
8583
MOVANTIK

Approved Use

Indicated for the treatment of opioid-induced constipation (OIC) in adult patients with chronic non-cancer pain.

Launch Date

2014
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
8 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/23726675
5 mg 1 times / day multiple, oral
dose: 5 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
NALOXEGOL OXALATE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
81.1 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/23726675
25 mg 1 times / day multiple, oral
dose: 25 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
NALOXEGOL OXALATE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
100 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/23726675
50 mg 1 times / day multiple, oral
dose: 50 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
NALOXEGOL OXALATE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
39 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/23726675
5 mg 1 times / day multiple, oral
dose: 5 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
NALOXEGOL OXALATE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
334.8 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/23726675
25 mg 1 times / day multiple, oral
dose: 25 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
NALOXEGOL OXALATE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
403.6 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/23726675
50 mg 1 times / day multiple, oral
dose: 50 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
NALOXEGOL OXALATE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
17.4 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/23726675
5 mg 1 times / day multiple, oral
dose: 5 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
NALOXEGOL OXALATE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
14.1 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/23726675
25 mg 1 times / day multiple, oral
dose: 25 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
NALOXEGOL OXALATE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
20.3 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/23726675
50 mg 1 times / day multiple, oral
dose: 50 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
NALOXEGOL OXALATE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
6 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204760s009lbl.pdf
unknown, unknown
 NALOXEGOL OXALATE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
95.8%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204760s009lbl.pdf
unknown, unknown
 NALOXEGOL OXALATE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
1000 mg single, oral
Highest studied dose
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137715
healthy, 18 - 45 years
Health Status: healthy
Age Group: 18 - 45 years
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137715
Other AEs: Gastrointestinal disorder (NOS), Nausea...
Other AEs:
Gastrointestinal disorder (NOS) (16.7%)
Nausea (16.7%)
CNS disorder (NOS) (33.3%)
Somnolence (16.7%)
Dizziness (16.7%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137715
250 mg 2 times / day steady, oral
Highest studied dose
Dose: 250 mg, 2 times / day
Route: oral
Route: steady
Dose: 250 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137716
healthy, 59 years (range: 18 - 65 years)
Health Status: healthy
Age Group: 59 years (range: 18 - 65 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137716
Other AEs: Myalgia, Restless leg syndrome...
Other AEs:
Myalgia (33.3%)
Restless leg syndrome (16.7%)
Dizziness (50%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137716
25 mg 1 times / day steady, oral
Recommended
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Disc. AE: Diarrhea, Abdominal pain...
AEs leading to
discontinuation/dose reduction:
Diarrhea (3.1%)
Abdominal pain (2.9%)
Nausea (1.1%)
Vomiting (0.9%)
Depression (0.2%)
Hypotension (0.2%)
Influenza like illness (0.2%)
Chills (0.2%)
Abdominal pain upper (1.1%)
Hyperhidrosis (0.9%)
Back pain (0.4%)
Myalgia (0.4%)
Liver function test abnormal (0.4%)
Headache (0.4%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
12.5 mg 1 times / day steady, oral
Dose: 12.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Disc. AE: Diarrhea, Abdominal pain...
AEs leading to
discontinuation/dose reduction:
Diarrhea (0.9%)
Abdominal pain (0.9%)
Nausea (1.1%)
Vomiting (0.5%)
Depression (0.2%)
Hypotension (0.2%)
Dizziness (0.5%)
Abdominal discomfort (0.2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
AEs

AEs

AESignificanceDosePopulation
Dizziness 16.7%
1000 mg single, oral
Highest studied dose
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137715
healthy, 18 - 45 years
Health Status: healthy
Age Group: 18 - 45 years
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137715
Gastrointestinal disorder (NOS) 16.7%
1000 mg single, oral
Highest studied dose
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137715
healthy, 18 - 45 years
Health Status: healthy
Age Group: 18 - 45 years
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137715
Nausea 16.7%
1000 mg single, oral
Highest studied dose
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137715
healthy, 18 - 45 years
Health Status: healthy
Age Group: 18 - 45 years
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137715
Somnolence 16.7%
1000 mg single, oral
Highest studied dose
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137715
healthy, 18 - 45 years
Health Status: healthy
Age Group: 18 - 45 years
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137715
CNS disorder (NOS) 33.3%
1000 mg single, oral
Highest studied dose
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137715
healthy, 18 - 45 years
Health Status: healthy
Age Group: 18 - 45 years
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137715
Restless leg syndrome 16.7%
250 mg 2 times / day steady, oral
Highest studied dose
Dose: 250 mg, 2 times / day
Route: oral
Route: steady
Dose: 250 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137716
healthy, 59 years (range: 18 - 65 years)
Health Status: healthy
Age Group: 59 years (range: 18 - 65 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137716
Myalgia 33.3%
250 mg 2 times / day steady, oral
Highest studied dose
Dose: 250 mg, 2 times / day
Route: oral
Route: steady
Dose: 250 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137716
healthy, 59 years (range: 18 - 65 years)
Health Status: healthy
Age Group: 59 years (range: 18 - 65 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137716
Dizziness 50%
250 mg 2 times / day steady, oral
Highest studied dose
Dose: 250 mg, 2 times / day
Route: oral
Route: steady
Dose: 250 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137716
healthy, 59 years (range: 18 - 65 years)
Health Status: healthy
Age Group: 59 years (range: 18 - 65 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/27137716
Chills 0.2%
Disc. AE
25 mg 1 times / day steady, oral
Recommended
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Depression 0.2%
Disc. AE
25 mg 1 times / day steady, oral
Recommended
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Hypotension 0.2%
Disc. AE
25 mg 1 times / day steady, oral
Recommended
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Influenza like illness 0.2%
Disc. AE
25 mg 1 times / day steady, oral
Recommended
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Back pain 0.4%
Disc. AE
25 mg 1 times / day steady, oral
Recommended
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Headache 0.4%
Disc. AE
25 mg 1 times / day steady, oral
Recommended
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Liver function test abnormal 0.4%
Disc. AE
25 mg 1 times / day steady, oral
Recommended
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Myalgia 0.4%
Disc. AE
25 mg 1 times / day steady, oral
Recommended
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Hyperhidrosis 0.9%
Disc. AE
25 mg 1 times / day steady, oral
Recommended
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Vomiting 0.9%
Disc. AE
25 mg 1 times / day steady, oral
Recommended
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Abdominal pain upper 1.1%
Disc. AE
25 mg 1 times / day steady, oral
Recommended
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Nausea 1.1%
Disc. AE
25 mg 1 times / day steady, oral
Recommended
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Abdominal pain 2.9%
Disc. AE
25 mg 1 times / day steady, oral
Recommended
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Diarrhea 3.1%
Disc. AE
25 mg 1 times / day steady, oral
Recommended
Dose: 25 mg, 1 times / day
Route: oral
Route: steady
Dose: 25 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Abdominal discomfort 0.2%
Disc. AE
12.5 mg 1 times / day steady, oral
Dose: 12.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Depression 0.2%
Disc. AE
12.5 mg 1 times / day steady, oral
Dose: 12.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Hypotension 0.2%
Disc. AE
12.5 mg 1 times / day steady, oral
Dose: 12.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Dizziness 0.5%
Disc. AE
12.5 mg 1 times / day steady, oral
Dose: 12.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Vomiting 0.5%
Disc. AE
12.5 mg 1 times / day steady, oral
Dose: 12.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Abdominal pain 0.9%
Disc. AE
12.5 mg 1 times / day steady, oral
Dose: 12.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Diarrhea 0.9%
Disc. AE
12.5 mg 1 times / day steady, oral
Dose: 12.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Nausea 1.1%
Disc. AE
12.5 mg 1 times / day steady, oral
Dose: 12.5 mg, 1 times / day
Route: oral
Route: steady
Dose: 12.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204760Orig1s000MedR.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
2252

inducer
1087

substrate
1946
inhibitor
2438
inhibitor
2507

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
2153

CYP2C19
2057

P-gp
1741

BCRP
910

OAT1
725

OAT3
747

OCT2
779

OATP1B1
1079

OATP1B3
961
CYP3A
220

P-gp
2052

OATP1B1
503

BCRP
697
CYP1A2
832

CYP2B6
669
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
BCRP
985
 no [IC50 >100 uM]
OAT1
730
 no [IC50 >100 uM]
OAT3
749
 no [IC50 >100 uM]
OATP1B1
1095
 no [IC50 >100 uM]
OATP1B3
970
 no [IC50 >100 uM]
OCT2
782
 no [IC50 >100 uM]
P-gp
1932
 no [IC50 >100 uM]
CYP3A4
2633
 no [Inhibition 100 uM]
CYP1A2
2333
 no
CYP1A2
2333
 no
CYP2B6
1160
 no
CYP2C19
2141
 no
CYP2C9
2497
 no
CYP2D6
2546
 no
CYP3A4
2633
 no
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
BCRP
697
 no
OATP1B1
503
 no
CYP3A
220
 yes
CYP3A4
1946
 yes
yes (co-administration study)
Comment: Co-administration with ketoconazole, a strong CYP3A4/P-gp inhibitor, resulted in 11-fold and ~ 12.85-fold increases in Cmax and AUC of naloxegol. Therefore dosing with such drugs is contraindicated.
Page: 24.0
P-gp
2052
 yes
yes (co-administration study)
Comment: Co-administration with ketoconazole, a strong CYP3A4/P-gp inhibitor, resulted in 11-fold and ~ 12.85-fold increases in Cmax and AUC of naloxegol. Therefore dosing with such drugs is contraindicated.
Page: 9.0
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:82975
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:82975
ChemicalBook
CB32614743
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB32614743
ZINC
ZINC000095564694
http://zinc15.docking.org/substances/ZINC000095564694
PubMed

PubMed

TitleDatePubMed
Naloxegol: A Novel Therapy in the Management of Opioid-Induced Constipation.
2016-11
Naloxegol: treatment for opioid-induced constipation in chronic non-cancer pain.
2015-03
Naloxegol: First oral peripherally acting mu opioid receptor antagonists for opioid-induced constipation.
2014-09-25
A phase 2, double-blind, randomized, placebo-controlled, dose-escalation study to evaluate the efficacy, safety, and tolerability of naloxegol in patients with opioid-induced constipation.
2013-09
New approaches to the treatment of opioid-induced constipation.
2008-08
Opioid-induced bowel dysfunction: prevalence, pathophysiology and burden.
2007-07
Incidence, prevalence, and management of opioid bowel dysfunction.
2001-11
Patents

Patents

US6323236
11

Sample Use Guides

In Vivo Use Guide
The recommended MOVANTIK dosage is 25 mg once daily in the morning. If patients are not able to tolerate MOVANTIK, reduce the dosage to 12.5 mg once daily.
Route of Administration: Oral
In Vitro Use Guide
Unknown
Substance Class Chemical
Created
by admin
on Mon Mar 31 21:02:50 GMT 2025
Edited
by admin
on Mon Mar 31 21:02:50 GMT 2025
Record UNII
44T7335BKE
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
NKTR-118
Preferred Name English
NALOXEGOL
DASH   INN   USAN   WHO-DD  
INN   USAN  
Official Name English
NALOXEGOL [USAN]
Common Name English
AZ-13337019
Code English
NALOXEGOL [NFLIS-DRUG]
Common Name English
Naloxegol [WHO-DD]
Common Name English
MORPHINAN-3,14-DIOL, 4,5-EPOXY-6-(3,6,9,12,15,18,21-HEPTAOXADOCOS-1-YLOXY)-17-(2-PROPEN-1-YL)-, (5.ALPHA.,6.ALPHA.)-
Systematic Name English
4,5.ALPHA.-EPOXY-6.ALPHA.-((3,6,7,12,15,18,21-HEPTAOXADOCOSYL)OXY)-17-(PROP-2-ENYL)MORPHINAN-3,14-DIOL
Systematic Name English
NALOXEGOL [MI]
Common Name English
naloxegol [INN]
Common Name English
Classification Tree Code System Code
NDF-RT N0000175691
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
WHO-VATC QA06AH03
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
WHO-ATC A06AH03
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
NCI_THESAURUS C681
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
Code System Code Type Description
DRUG CENTRAL
4832
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
EPA CompTox
DTXSID80234684
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
CAS
854601-70-0
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
SMS_ID
100000152160
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
RXCUI
1551777
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY RxNorm
CHEBI
82975
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
ChEMBL
CHEMBL2219418
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
HSDB
8338
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
MERCK INDEX
m11770
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
INN
9434
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
DAILYMED
44T7335BKE
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
USAN
ZZ-128
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
NCI_THESAURUS
C97506
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
LACTMED
Naloxegol
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
DRUG BANK
DB09049
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
EVMPD
SUB126723
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
FDA UNII
44T7335BKE
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
WIKIPEDIA
NALOXEGOL
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
PUBCHEM
56959087
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
IUPHAR
7539
Created by admin on Mon Mar 31 21:02:50 GMT 2025 , Edited by admin on Mon Mar 31 21:02:50 GMT 2025
PRIMARY
Related Record Type Details
MU-TYPE OPIOID RECEPTOR
TARGET -> INHIBITOR
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> SUBSTRATE
CYTOCHROME P450 2D6
METABOLIC ENZYME -> SUBSTRATE
MINOR
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
MAJOR
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
CYTOCHROME P450 3A5
METABOLIC ENZYME -> SUBSTRATE
MAJOR
Structure of NALOXEGOL
EXCRETED UNCHANGED
In feces, ~ 68 % of radioactivity dose was found; 58 % of fecal radioactivity was characterized, with 16 % noted to be unchanged drug and remaining as metabolites.
FECAL
Structure of NALOXEGOL
EXCRETED UNCHANGED
16 % of radioactivity dose was found in urine, with 10 % as unchanged drug and 6 % as metabolites.
URINE
Related Record Type Details
Structure of CARBOXYMETHYL-PEG6-NALOXOL
METABOLITE -> PARENT
Structure of HO-PEG5-NALOXOL
METABOLITE -> PARENT
PLASMA; URINE
Structure of 3,6,9,12-TETRAOXATETRADECANOIC ACID, 14-(((5.ALPHA.,6.ALPHA.)-4,5-EPOXY-3,14-DIHYDROXY-17-(2-PROPEN-1-YL)MORPHINAN-6-YL)OXY)-
METABOLITE -> PARENT
FECAL; PLASMA; URINE
Structure of ACETIC ACID, 2-(2-(2-(2-(((5.ALPHA.,6.ALPHA.)-4,5-EPOXY-3,14-DIHYDROXY-17-(2-PROPEN-1-YL)MORPHINAN-6-YL)OXY)ETHOXY)ETHOXY)ETHOXY)-
METABOLITE -> PARENT
FECAL; URINE
Related Record Type Details
Structure of NALOXEGOL
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
NIH
NCATS
PRIVACY NOTICE
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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