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

Stem definitionDrug idCAS RN
sulpiride derivatives and analogues 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: 1.53
  • 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:

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
S (Water solubility) 97 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Bocci G, Oprea TI, Benet LZ

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 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
Crying 37.05 28.81 19 2849 23324 63462830
Wrist fracture 36.83 28.81 16 2852 13571 63472583
Therapeutic drug monitoring analysis not performed 36.01 28.81 9 2859 1343 63484811
Depressed mood 34.77 28.81 22 2846 40169 63445985
Feeling jittery 33.79 28.81 15 2853 13388 63472766
Heliotrope rash 33.41 28.81 6 2862 181 63485973
Adrenal insufficiency 32.60 28.81 16 2852 17899 63468255
Suicidal ideation 32.46 28.81 25 2843 62396 63423758
Poikiloderma 32.20 28.81 6 2862 223 63485931
Transferrin decreased 31.77 28.81 6 2862 240 63485914
Inability to afford medication 31.09 28.81 9 2859 2338 63483816
Hypoacusis 30.82 28.81 17 2851 24134 63462020
Inappropriate schedule of product administration 30.44 28.81 30 2838 103935 63382219
Iron binding capacity total decreased 29.86 28.81 6 2862 332 63485822
Insurance issue 29.81 28.81 11 2857 6110 63480044
Mental disorder 29.70 28.81 17 2851 25902 63460252
Vasculitis 29.41 28.81 15 2853 18194 63467960

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

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 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
Feeling jittery 35.06 31.02 14 2689 12827 79728858
Heliotrope rash 34.67 31.02 6 2697 196 79741489
Crying 33.14 31.02 16 2687 23027 79718658
Anger 31.15 31.02 14 2689 17148 79724537

FDA Adverse Event Reporting System (Pediatric)

None

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
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|

DiseaseRelationSNOMED_IDDOID
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 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 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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
5-hydroxytryptamine receptor 4 GPCR AGONIST Ki 8.60 CHEMBL DRUG LABEL
D(4) dopamine receptor GPCR Ki 5.63 PDSP
5-hydroxytryptamine receptor 3A Ion channel Ki 5.40 CHEMBL
5-hydroxytryptamine receptor 4 GPCR EC50 7.58 CHEMBL

External reference:

IDSource
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
2107309 RXNORM
26947 MMSL
304089 MMSL
d07541 MMSL
013402 NDDF
013403 NDDF
1149428003 SNOMEDCT_US
699273008 SNOMEDCT_US
774192009 SNOMEDCT_US
C0913506 UMLSCUI
3052762 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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