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

Stem definition	Drug id	CAS RN
sulpiride derivatives and analogues	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

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:

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Property	Value	Reference
S (Water solubility)	97 mg/mL	Bocci G, Oprea TI, Benet LZ
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
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Bocci G, Oprea TI, Benet LZ
t_half (Half-life)	22.50 hours	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.70 %	Lombardo F, Berellini G, Obach RS

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Approvals:

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

FDA Adverse Event Reporting System (Female)

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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	132.91	28.81	28	2840	1967	63484187
Hyperprolactinaemia	94.22	28.81	24	2844	3876	63482278
Secondary adrenocortical insufficiency	83.49	28.81	18	2850	1410	63484744
Head banging	72.06	28.81	13	2855	403	63485751
Screaming	54.53	28.81	15	2853	3247	63482907
Psychiatric symptom	47.56	28.81	15	2853	5208	63480946
No adverse event	44.40	28.81	26	2842	41379	63444775
Arthropod bite	41.33	28.81	15	2853	7963	63478191
Headache	41.27	28.81	89	2779	633152	62853002
Anger	38.17	28.81	16	2852	12440	63473714

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FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

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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	133.80	31.02	28	2675	2548	79739137
Hyperprolactinaemia	96.75	31.02	24	2679	4652	79737033
Secondary adrenocortical insufficiency	75.25	31.02	18	2685	2996	79738689
Head banging	65.85	31.02	12	2691	529	79741156
Screaming	56.02	31.02	15	2688	3918	79737767
Headache	49.46	31.02	83	2620	653689	79087996
Psychiatric symptom	43.29	31.02	14	2689	7021	79734664
Arthropod bite	40.74	31.02	14	2689	8457	79733228
Wrist fracture	39.66	31.02	15	2688	11906	79729779
Therapeutic drug monitoring analysis not performed	35.37	31.02	9	2694	1927	79739758

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A06AX05	ALIMENTARY TRACT AND METABOLISM DRUGS FOR CONSTIPATION DRUGS FOR CONSTIPATION Other drugs for constipation
FDA EPC	N0000193871	Serotonin-4 Receptor Agonist
FDA MoA	N0000193870	Serotonin 4 Receptor Agonists
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

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

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

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🐶 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)

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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

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	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

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External reference:

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ID	Source
013402	NDDF
013403	NDDF
0A09IUW5TP	UNII
1149428003	SNOMEDCT_US
179474-85-2	SECONDARY_CAS_RN
2107309	RXNORM
243	IUPHAR_LIGAND_ID
26947	MMSL
304089	MMSL
3052762	PUBCHEM_CID

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Pharmaceutical products:

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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	54092-546	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
MOTEGRITY	HUMAN PRESCRIPTION DRUG LABEL	1	54092-547	TABLET, FILM COATED	2 mg	ORAL	NDA	29 sections

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