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

Stem definition	Drug id	CAS RN
sulpiride derivatives	3502	179474-81-8

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

motegrity
prucalopride succinate
resolor
prucalopride
R093877

a 5-HT4 agonist enterokinetic compound

Molecular weight: 367.87
Formula: C18H26ClN3O3
CLOGP: 1.53
LIPINSKI: 0
HAC: 6
HDO: 2
TPSA: 76.82
ALOGS: -3.46
ROTB: 6

Status: ONP

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

Drug dosage:

Dose	Unit	Route
2	mg	O

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	8.73 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	4.55 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.70 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	22.50 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Oct. 15, 2009	EMA
Dec. 14, 2018	FDA	SHIRE DEV LLC

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
Pituitary tumour benign	132.50	34.68	27	2078	1754	50601265
Hyperprolactinaemia	94.61	34.68	23	2082	3342	50599677
Secondary adrenocortical insufficiency	77.21	34.68	16	2089	1127	50601892
Head banging	73.17	34.68	13	2092	402	50602617
Screaming	57.13	34.68	15	2090	2963	50600056
Psychiatric symptom	50.77	34.68	15	2090	4555	50598464
Arthropod bite	46.63	34.68	15	2090	6030	50596989
Headache	45.95	34.68	78	2027	506457	50096562
Anger	40.92	34.68	16	2089	11317	50591702
Wrist fracture	40.71	34.68	16	2089	11471	50591548
Feeling jittery	37.65	34.68	15	2090	11145	50591874
Crying	34.85	34.68	17	2088	20399	50582620

FDA Adverse Event Reporting System (Male)

None

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
Pituitary tumour benign	132.84	31.52	27	2031	2266	64494408
Hyperprolactinaemia	96.35	31.52	23	2035	4042	64492632
Secondary adrenocortical insufficiency	69.98	31.52	16	2042	2329	64494345
Head banging	67.24	31.52	12	2046	500	64496174
Screaming	58.55	31.52	15	2043	3514	64493160
Headache	51.51	31.52	73	1985	529394	63967280
Psychiatric symptom	45.72	31.52	14	2044	6259	64490415
Arthropod bite	44.76	31.52	14	2044	6707	64489967
Wrist fracture	43.13	31.52	15	2043	9986	64486688
Feeling jittery	38.46	31.52	14	2044	10621	64486053
Anger	33.13	31.52	14	2044	15727	64480947

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	A06AX05	ALIMENTARY TRACT AND METABOLISM DRUGS FOR CONSTIPATION DRUGS FOR CONSTIPATION Other drugs for constipation
MeSH PA	D005765	Gastrointestinal Agents
MeSH PA	D054368	Laxatives
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D058828	Serotonin 5-HT4 Receptor Agonists
MeSH PA	D018490	Serotonin Agents
MeSH PA	D017366	Serotonin Receptor Agonists
FDA MoA	N0000193870	Serotonin 4 Receptor Agonists
FDA EPC	N0000193871	Serotonin-4 Receptor Agonist

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

Disease	Relation	SNOMED_ID	DOID
Constipation	indication	14760008	DOID:2089
Perforation of intestine	contraindication	56905009	DOID:2074
Ulcerative colitis	contraindication	64766004	DOID:8577

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.83	acidic
pKa2	8.57	Basic
pKa3	1.07	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 1MG BASE	MOTEGRITY	TAKEDA PHARMS USA	N210166	Dec. 14, 2018	RX	TABLET	ORAL	Dec. 14, 2023	NEW CHEMICAL ENTITY
EQ 2MG BASE	MOTEGRITY	TAKEDA PHARMS USA	N210166	Dec. 14, 2018	RX	TABLET	ORAL	Dec. 14, 2023	NEW CHEMICAL ENTITY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
5-hydroxytryptamine receptor 4	GPCR	Q13639	5HT4R_HUMAN	AGONIST	Ki	8.60		CHEMBL	DRUG LABEL
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		Ki	5.63		PDSP
5-hydroxytryptamine receptor 3A	Ion channel	P46098	5HT3A_HUMAN		Ki	5.40		CHEMBL
5-hydroxytryptamine receptor 4	GPCR		5HT4R_RAT		EC50	7.58		CHEMBL

External reference:

ID	Source
D09205	KEGG_DRUG
179474-85-2	SECONDARY_CAS_RN
4038160	VANDF
CHEBI:135552	CHEBI
CHEMBL117287	ChEMBL_ID
CHEMBL2105748	ChEMBL_ID
C406662	MESH_SUPPLEMENTAL_RECORD_UI
243	IUPHAR_LIGAND_ID
7702	INN_ID
DB06480	DRUGBANK_ID
0A09IUW5TP	UNII
3052762	PUBCHEM_CID
2107309	RXNORM
26947	MMSL
304089	MMSL
d07541	MMSL
013402	NDDF
013403	NDDF
1149428003	SNOMEDCT_US
699273008	SNOMEDCT_US
774192009	SNOMEDCT_US
C0913506	UMLSCUI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
MOTEGRITY	HUMAN PRESCRIPTION DRUG LABEL	1	54092-546	TABLET, FILM COATED	1 mg	ORAL	NDA	29 sections
MOTEGRITY	HUMAN PRESCRIPTION DRUG LABEL	1	54092-547	TABLET, FILM COATED	2 mg	ORAL	NDA	29 sections