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

Details

Stereochemistry ABSOLUTE
Molecular Formula C34H53NO11
Molecular Weight 651.786
Optical Activity UNSPECIFIED
Defined Stereocenters 5 / 5
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of NALOXEGOL

SMILES

C=CCN1CC[C@@]23c4c5ccc(c4O[C@@]3([H])[C@]([H])(CC[C@]2([C@@]1([H])C5)O)OCCOCCOCCOCCOCCOCCOCCOC)O

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 651.786
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 5 / 5
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: 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

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

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

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P35372|||G8XRH8|||Q5TDA1|||Q9UN57
Gene ID: 4988
Gene Symbol: OPRM1
Target Organism: Homo sapiens (Human)
7.40000000000000036 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
MOVANTIK

Approved Use

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

Launch Date

1410825600000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
81.1 ng/mL
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
8 ng/mL
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
100 ng/mL
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
334.8 ng × h/mL
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
39 ng × h/mL
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
403.6 ng × h/mL
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
14.1 h
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
17.4 h
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
20.3 h
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
unknown, unknown
NALOXEGOL OXALATE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
95.8%
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:
healthy, 18 - 45 years
Health Status: healthy
Age Group: 18 - 45 years
Sex: M
Sources:
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:
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:
healthy, 59 years (range: 18 - 65 years)
Health Status: healthy
Age Group: 59 years (range: 18 - 65 years)
Sex: M+F
Sources:
Other AEs: Myalgia, Restless leg syndrome...
Other AEs:
Myalgia (33.3%)
Restless leg syndrome (16.7%)
Dizziness (50%)
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
AEs

AEs

AESignificanceDosePopulation
Dizziness 16.7%
1000 mg single, oral
Highest studied dose
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
healthy, 18 - 45 years
Health Status: healthy
Age Group: 18 - 45 years
Sex: M
Sources:
Gastrointestinal disorder (NOS) 16.7%
1000 mg single, oral
Highest studied dose
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
healthy, 18 - 45 years
Health Status: healthy
Age Group: 18 - 45 years
Sex: M
Sources:
Nausea 16.7%
1000 mg single, oral
Highest studied dose
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
healthy, 18 - 45 years
Health Status: healthy
Age Group: 18 - 45 years
Sex: M
Sources:
Somnolence 16.7%
1000 mg single, oral
Highest studied dose
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
healthy, 18 - 45 years
Health Status: healthy
Age Group: 18 - 45 years
Sex: M
Sources:
CNS disorder (NOS) 33.3%
1000 mg single, oral
Highest studied dose
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
healthy, 18 - 45 years
Health Status: healthy
Age Group: 18 - 45 years
Sex: M
Sources:
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:
healthy, 59 years (range: 18 - 65 years)
Health Status: healthy
Age Group: 59 years (range: 18 - 65 years)
Sex: M+F
Sources:
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:
healthy, 59 years (range: 18 - 65 years)
Health Status: healthy
Age Group: 59 years (range: 18 - 65 years)
Sex: M+F
Sources:
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:
healthy, 59 years (range: 18 - 65 years)
Health Status: healthy
Age Group: 59 years (range: 18 - 65 years)
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [Inhibition 100 uM]
no
no
no
no
no
no
no
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
yes
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
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
PubMed

PubMed

TitleDatePubMed
Incidence, prevalence, and management of opioid bowel dysfunction.
2001 Nov
Opioid-induced bowel dysfunction: prevalence, pathophysiology and burden.
2007 Jul
Naloxegol: First oral peripherally acting mu opioid receptor antagonists for opioid-induced constipation.
2015 Jul-Sep
Naloxegol: A Novel Therapy in the Management of Opioid-Induced Constipation.
2016 Nov
Patents

Patents

Sample Use Guides

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
Substance Class Chemical
Created
by admin
on Sat Jun 26 00:03:25 UTC 2021
Edited
by admin
on Sat Jun 26 00:03:25 UTC 2021
Record UNII
44T7335BKE
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
NALOXEGOL
DASH   INN   USAN   WHO-DD  
INN   USAN  
Official Name English
NALOXEGOL [WHO-DD]
Common Name English
NALOXEGOL [USAN]
Common Name English
AZ-13337019
Code English
NALOXEGOL [NFLIS-DRUG]
Common Name English
NKTR-118
Code 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 Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
WHO-VATC QA06AH03
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
WHO-ATC A06AH03
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
NCI_THESAURUS C681
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
Code System Code Type Description
DRUG CENTRAL
4832
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
PRIMARY
CAS
854601-70-0
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
PRIMARY
RXCUI
1551777
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
PRIMARY RxNorm
ChEMBL
CHEMBL2219418
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
PRIMARY
HSDB
8338
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
PRIMARY
MERCK INDEX
M11770
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
PRIMARY
INN
9434
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
PRIMARY
NCI_THESAURUS
C97506
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
PRIMARY
LACTMED
Naloxegol
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
PRIMARY
DRUG BANK
DB09049
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
PRIMARY
EPA CompTox
854601-70-0
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
PRIMARY
EVMPD
SUB126723
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
PRIMARY
FDA UNII
44T7335BKE
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
PRIMARY
WIKIPEDIA
NALOXEGOL
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
PRIMARY
PUBCHEM
56959087
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
PRIMARY
IUPHAR
7539
Created by admin on Sat Jun 26 00:03:25 UTC 2021 , Edited by admin on Sat Jun 26 00:03:25 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
TRANSPORTER -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
MINOR
METABOLIC ENZYME -> SUBSTRATE
MAJOR
BINDER->LIGAND
BINDING
METABOLIC ENZYME -> SUBSTRATE
MAJOR
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
EXCRETED UNCHANGED
16 % of radioactivity dose was found in urine, with 10 % as unchanged drug and 6 % as metabolites.
URINE
Related Record Type Details
METABOLITE -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC