naloxegol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
opioid receptor antagonists/agonists related to normorphine	4832	854601-70-0

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

moventig
naloxegol oxalate
movantik
naloxegol
NKTR-118

A peripherally acting opioid receptor antagonist specific for mu-opioid receptors. Used to decrease the constipating effects of opioids.

Molecular weight: 651.79
Formula: C34H53NO11
CLOGP: -0.18
LIPINSKI: 2
HAC: 12
HDO: 2
TPSA: 126.77
ALOGS: -4.06
ROTB: 24

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
25	mg	O

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Sept. 25, 2014	EMA
Sept. 16, 2014	FDA	ASTRAZENECA PHARMS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug withdrawal syndrome	196.80	24.24	62	2231	27132	63459597
Withdrawal syndrome	97.93	24.24	34	2259	19963	63466766
Abdominal pain	79.33	24.24	73	2220	293383	63193346
Hyperhidrosis	64.50	24.24	43	2250	107793	63378936
Drug screen positive	51.57	24.24	14	2279	3615	63483114
Diarrhoea	39.24	24.24	82	2211	715284	62771445
Chills	38.06	24.24	32	2261	113346	63373383
Nausea	29.58	24.24	82	2211	854389	62632340
Intentional product misuse	28.65	24.24	21	2272	60896	63425833
Pain	26.50	24.24	72	2221	740556	62746173
Vomiting	24.75	24.24	59	2234	559558	62927171

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug withdrawal syndrome	85.31	29.11	31	1298	19803	34935799
Withdrawal syndrome	51.75	29.11	19	1310	12436	34943166
Abdominal pain	44.92	29.11	42	1287	163576	34792026
Hyperhidrosis	43.48	29.11	30	1299	75662	34879940
Pain	38.76	29.11	43	1286	204632	34750970
Agranulocytosis	36.83	29.11	18	1311	23803	34931799

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug withdrawal syndrome	140.21	23.17	50	2592	34668	79707078
Withdrawal syndrome	69.60	23.17	28	2614	26826	79714920
Abdominal pain	61.88	23.17	70	2572	389499	79352247
Hyperhidrosis	52.51	23.17	42	2600	151450	79590296
Nausea	36.25	23.17	90	2552	957106	78784640
Diarrhoea	34.59	23.17	84	2558	880405	78861341
Pain	32.95	23.17	72	2570	703730	79038016
Vomiting	28.76	23.17	66	2576	665762	79075984
Agranulocytosis	28.37	23.17	18	2624	45012	79696734

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	A06AH03	ALIMENTARY TRACT AND METABOLISM DRUGS FOR CONSTIPATION DRUGS FOR CONSTIPATION Peripheral opioid receptor antagonists
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D009292	Narcotic Antagonists
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018689	Sensory System Agents
FDA MoA	N0000000154	Opioid Antagonists
CHEBI has role	CHEBI:35488	central nervous system depressants
CHEBI has role	CHEBI:50137	mu-opioid receptor antagonists
CHEBI has role	CHEBI:90755	antidote to opioid overdose
FDA EPC	N0000175691	Opioid Antagonist
CHEBI has role	CHEBI:75325	cathartics

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Therapeutic opioid induced constipation	indication	136801000119102

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.69	acidic
pKa2	8.06	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 12.5MG BASE	MOVANTIK	VALINOR	N204760	Sept. 16, 2014	RX	TABLET	ORAL	7056500	June 29, 2024	TREATMENT OF OPIOID-INDUCED CONSTIPATION
EQ 25MG BASE	MOVANTIK	VALINOR	N204760	Sept. 16, 2014	RX	TABLET	ORAL	7056500	June 29, 2024	TREATMENT OF OPIOID-INDUCED CONSTIPATION
EQ 12.5MG BASE	MOVANTIK	VALINOR	N204760	Sept. 16, 2014	RX	TABLET	ORAL	8067431	Dec. 16, 2024	TREATMENT OF OPIOID-INDUCED CONSTIPATION
EQ 25MG BASE	MOVANTIK	VALINOR	N204760	Sept. 16, 2014	RX	TABLET	ORAL	8067431	Dec. 16, 2024	TREATMENT OF OPIOID-INDUCED CONSTIPATION

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN	ANTAGONIST				DRUG LABEL	DRUG LABEL

External reference:

ID	Source
44T7335BKE	UNII
D10375	KEGG_DRUG
1354744-91-4	SECONDARY_CAS_RN
4019852	VANDF
4034135	VANDF
C3700399	UMLSCUI
CHEBI:82975	CHEBI
CHEBI:7459	CHEBI
CHEMBL2219418	ChEMBL_ID
56959087	PUBCHEM_CID
DB09049	DRUGBANK_ID
CHEMBL2219416	ChEMBL_ID
9434	INN_ID
C000589308	MESH_SUPPLEMENTAL_RECORD_UI
7539	IUPHAR_LIGAND_ID
1551777	RXNORM
228769	MMSL
27364	MMSL
30568	MMSL
31169	MMSL
d00311	MMSL
d08289	MMSL
004661	NDDF
015863	NDDF
015864	NDDF
372890007	SNOMEDCT_US
719411008	SNOMEDCT_US
719412001	SNOMEDCT_US
763564001	SNOMEDCT_US
89018006	SNOMEDCT_US
C0027358	UMLSCUI
DB01183	DRUGBANK_ID
1526	INN_ID
D009270	MESH_DESCRIPTOR_UI
5284596	PUBCHEM_CID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
MOVANTIK	HUMAN PRESCRIPTION DRUG LABEL	1	0310-1969	TABLET, FILM COATED	12.50 mg	ORAL	NDA	26 sections
MOVANTIK	HUMAN PRESCRIPTION DRUG LABEL	1	0310-1970	TABLET, FILM COATED	25 mg	ORAL	NDA	26 sections
MOVANTIK	HUMAN PRESCRIPTION DRUG LABEL	1	55700-383	TABLET, FILM COATED	25 mg	ORAL	NDA	27 sections
MOVANTIK	HUMAN PRESCRIPTION DRUG LABEL	1	55700-988	TABLET, FILM COATED	25 mg	ORAL	NDA	26 sections
MOVANTIK	HUMAN PRESCRIPTION DRUG LABEL	1	57841-1300	TABLET, FILM COATED	12.50 mg	ORAL	NDA	26 sections
MOVANTIK	HUMAN PRESCRIPTION DRUG LABEL	1	57841-1300	TABLET, FILM COATED	12.50 mg	ORAL	NDA	26 sections
MOVANTIK	HUMAN PRESCRIPTION DRUG LABEL	1	57841-1301	TABLET, FILM COATED	25 mg	ORAL	NDA	26 sections
MOVANTIK	HUMAN PRESCRIPTION DRUG LABEL	1	57841-1301	TABLET, FILM COATED	25 mg	ORAL	NDA	26 sections
MOVANTIK	HUMAN PRESCRIPTION DRUG LABEL	1	82625-8801	TABLET, FILM COATED	12.50 mg	ORAL	NDA	26 sections
MOVANTIK	HUMAN PRESCRIPTION DRUG LABEL	1	82625-8802	TABLET, FILM COATED	25 mg	ORAL	NDA	26 sections