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

Stem definitionDrug idCAS RN
sulpiride derivatives 3502 179474-81-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • motegrity
  • prucalopride succinate
  • resolor
  • prucalopride
  • R093877
a 5-HT4 agonist enterokinetic compound
  • Molecular weight: 367.87
  • Formula: C18H26ClN3O3
  • CLOGP: 1.41
  • 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:

DoseUnitRoute
2 mg O

ADMET properties:

PropertyValueReference
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:

DateAgencyCompanyOrphan
Oct. 15, 2009 EMA
Dec. 14, 2018 FDA SHIRE DEV LLC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Pituitary tumour benign 52.41 40.51 7 72 320 2357686
Hyperprolactinaemia 46.87 40.51 7 72 715 2357291
Nausea 44.72 40.51 17 62 112172 2245834

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event

Pharmacologic Action:

SourceCodeDescription
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

Drug Use (View source of the data)

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

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 1MG BASE MOTEGRITY SHIRE DEV LLC N210166 Dec. 14, 2018 RX TABLET ORAL Dec. 14, 2023 NEW CHEMICAL ENTITY
EQ 2MG BASE MOTEGRITY SHIRE DEV LLC N210166 Dec. 14, 2018 RX TABLET ORAL Dec. 14, 2023 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
5-hydroxytryptamine receptor 4 GPCR AGONIST Ki 8.60 CHEMBL DRUG LABEL
5-hydroxytryptamine receptor 3A Ion channel Ki 5.40 CHEMBL
D(4) dopamine receptor GPCR Ki 5.63 PDSP

External reference:

IDSource
D09205 KEGG_DRUG
0A09IUW5TP UNII
7702 INN_ID
179474-85-2 SECONDARY_CAS_RN
2107310 RXNORM
d07541 MMSL
774192009 SNOMEDCT_US
4038160 VANDF
013402 NDDF
699273008 SNOMEDCT_US
CHEMBL117287 ChEMBL_ID
DB06480 DRUGBANK_ID
CHEBI:135552 CHEBI
CHEMBL2105748 ChEMBL_ID
3052762 PUBCHEM_CID
243 IUPHAR_LIGAND_ID
C406662 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
MOTEGRITY HUMAN PRESCRIPTION DRUG LABEL 1 54092-546 TABLET, FILM COATED 1 mg ORAL NDA 17 sections
MOTEGRITY HUMAN PRESCRIPTION DRUG LABEL 1 54092-547 TABLET, FILM COATED 2 mg ORAL NDA 17 sections