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prucalopride 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| sulpiride derivatives and analogues | 3502 | 179474-81-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a 5-HT4 agonist enterokinetic compound
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 |
| 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 |
| BA (Bioavailability) | 70 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.855 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 4.667 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 7.551 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.932 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 74.780 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 82.050 | % | High | 1 |
| herg | hERG pIC50 | 5.003 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 0.979 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.090 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 72.870 | % | High | 1 |
| kinase-safety-class | ACVR2B,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAP3K7,MAPK10,MAPK7,MET,NTRK2,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1 | 31 | |||
| kinase-selectivity-class | AXL,BRAF,EIF2AK3,EPHB4,SIK2,STK33 | 6 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 6.471 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 5.358 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 75.120 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 24.774 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 81.190 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 2.679 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 87.650 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 71.530 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 924.698 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 14, 2018 | FDA | SHIRE DEV LLC | |
| Oct. 15, 2009 | EMA |
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 | 132.69 | 24.41 | 28 | 3829 | 2104 | 90622486 |
| Hyperprolactinaemia | 92.39 | 24.41 | 25 | 3832 | 5408 | 90619182 |
| Secondary adrenocortical insufficiency | 81.10 | 24.41 | 19 | 3838 | 2299 | 90622291 |
| Head banging | 72.34 | 24.41 | 13 | 3844 | 419 | 90624171 |
| Insurance issue | 63.31 | 24.41 | 22 | 3835 | 10936 | 90613654 |
| Inability to afford medication | 63.14 | 24.41 | 17 | 3840 | 3605 | 90620985 |
| No adverse event | 57.80 | 24.41 | 36 | 3821 | 67946 | 90556644 |
| Screaming | 53.34 | 24.41 | 15 | 3842 | 3735 | 90620855 |
| Headache | 49.24 | 24.41 | 111 | 3746 | 862635 | 89761955 |
| Psychiatric symptom | 47.80 | 24.41 | 16 | 3841 | 7102 | 90617488 |
| Anger | 44.33 | 24.41 | 18 | 3839 | 13702 | 90610888 |
| Serum amyloid A protein increased | 42.22 | 24.41 | 9 | 3848 | 708 | 90623882 |
| Arthropod bite | 40.81 | 24.41 | 15 | 3842 | 8752 | 90615838 |
| Crying | 39.30 | 24.41 | 20 | 3837 | 25625 | 90598965 |
| Heliotrope rash | 38.58 | 24.41 | 7 | 3850 | 238 | 90624352 |
| Poikiloderma | 36.76 | 24.41 | 7 | 3850 | 311 | 90624279 |
| Therapeutic drug monitoring analysis not performed | 36.69 | 24.41 | 9 | 3848 | 1320 | 90623270 |
| Wrist fracture | 35.59 | 24.41 | 16 | 3841 | 15608 | 90608982 |
| Transferrin decreased | 35.19 | 24.41 | 7 | 3850 | 391 | 90624199 |
| Mental disorder | 34.96 | 24.41 | 20 | 3837 | 32298 | 90592292 |
| Iron binding capacity total decreased | 34.09 | 24.41 | 7 | 3850 | 459 | 90624131 |
| Inappropriate schedule of product administration | 32.78 | 24.41 | 36 | 3821 | 149897 | 90474693 |
| Feeling jittery | 32.67 | 24.41 | 15 | 3842 | 15356 | 90609234 |
| Suicidal ideation | 32.15 | 24.41 | 26 | 3831 | 73829 | 90550761 |
| Depressed mood | 31.48 | 24.41 | 22 | 3835 | 50200 | 90574390 |
| Abdominal pain | 29.55 | 24.41 | 57 | 3800 | 395664 | 90228926 |
| Hypoacusis | 29.49 | 24.41 | 17 | 3840 | 27833 | 90596757 |
| Pollakiuria | 29.35 | 24.41 | 18 | 3839 | 32987 | 90591603 |
| Nervousness | 28.83 | 24.41 | 18 | 3839 | 34038 | 90590552 |
| Impaired gastric emptying | 28.80 | 24.41 | 13 | 3844 | 12796 | 90611794 |
| Product availability issue | 28.41 | 24.41 | 11 | 3846 | 7393 | 90617197 |
| Laryngectomy | 28.34 | 24.41 | 4 | 3853 | 25 | 90624565 |
| Emotional distress | 27.62 | 24.41 | 18 | 3839 | 36644 | 90587946 |
| Vasculitis | 27.13 | 24.41 | 15 | 3842 | 22678 | 90601912 |
| Lip pruritus | 26.63 | 24.41 | 7 | 3850 | 1353 | 90623237 |
| Adrenal insufficiency | 25.80 | 24.41 | 16 | 3841 | 29905 | 90594685 |
| Product monitoring error | 25.77 | 24.41 | 9 | 3848 | 4535 | 90620055 |
| Nausea | 25.72 | 24.41 | 104 | 3753 | 1110212 | 89514378 |
| Mitochondrial myopathy | 25.51 | 24.41 | 5 | 3852 | 259 | 90624331 |
| Rib fracture | 25.00 | 24.41 | 15 | 3842 | 26420 | 90598170 |
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 |
|---|---|---|---|---|---|---|
| Duplicate therapy error | 51.38 | 35.79 | 8 | 685 | 288 | 42620354 |
| Delirium tremens | 45.32 | 35.79 | 8 | 685 | 624 | 42620018 |
| Serum amyloid A protein increased | 44.61 | 35.79 | 7 | 686 | 265 | 42620377 |
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 | 130.63 | 25.62 | 28 | 3767 | 2819 | 110582685 |
| Hyperprolactinaemia | 93 | 25.62 | 25 | 3770 | 6550 | 110578954 |
| Serum amyloid A protein increased | 83.34 | 25.62 | 16 | 3779 | 926 | 110584578 |
| Secondary adrenocortical insufficiency | 72.92 | 25.62 | 19 | 3776 | 4415 | 110581089 |
| Head banging | 65.11 | 25.62 | 12 | 3783 | 556 | 110584948 |
| Headache | 54.08 | 25.62 | 103 | 3692 | 882274 | 109703230 |
| Screaming | 52.62 | 25.62 | 15 | 3780 | 4866 | 110580638 |
| Psychiatric symptom | 43.24 | 25.62 | 15 | 3780 | 9198 | 110576306 |
| Duplicate therapy error | 42.22 | 25.62 | 8 | 3787 | 431 | 110585073 |
| Arthropod bite | 38.75 | 25.62 | 14 | 3781 | 9657 | 110575847 |
| Delirium tremens | 37.94 | 25.62 | 8 | 3787 | 743 | 110584761 |
| Wrist fracture | 36.70 | 25.62 | 15 | 3780 | 14402 | 110571102 |
| Feeling jittery | 36.40 | 25.62 | 15 | 3780 | 14707 | 110570797 |
| Therapeutic drug monitoring analysis not performed | 35.28 | 25.62 | 9 | 3786 | 1922 | 110583582 |
| Impaired gastric emptying | 34.43 | 25.62 | 14 | 3781 | 13261 | 110572243 |
| Crying | 34.26 | 25.62 | 17 | 3778 | 25611 | 110559893 |
| Heliotrope rash | 33.46 | 25.62 | 6 | 3789 | 238 | 110585266 |
| Suicidal ideation | 31.57 | 25.62 | 26 | 3769 | 93911 | 110491593 |
| Mental disorder | 30.25 | 25.62 | 18 | 3777 | 38773 | 110546731 |
| Vision blurred | 30.01 | 25.62 | 29 | 3766 | 128993 | 110456511 |
| Anger | 29.61 | 25.62 | 14 | 3781 | 18993 | 110566511 |
| Poikiloderma | 29.26 | 25.62 | 6 | 3789 | 486 | 110585018 |
| Transferrin decreased | 28.62 | 25.62 | 6 | 3789 | 542 | 110584962 |
| Laryngectomy | 28.45 | 25.62 | 4 | 3791 | 31 | 110585473 |
| Iron binding capacity total decreased | 28.41 | 25.62 | 6 | 3789 | 561 | 110584943 |
| Mast cell activation syndrome | 27.32 | 25.62 | 7 | 3788 | 1521 | 110583983 |
| Abdominal pain | 26.61 | 25.62 | 56 | 3739 | 512933 | 110072571 |
| Hypoacusis | 26.58 | 25.62 | 16 | 3779 | 35175 | 110550329 |
| Nervousness | 25.90 | 25.62 | 16 | 3779 | 36835 | 110548669 |
| Pollakiuria | 25.63 | 25.62 | 17 | 3778 | 44178 | 110541326 |
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 | D017366 | Serotonin Receptor Agonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018490 | Serotonin Agents |
| MeSH PA | D054368 | Laxatives |
| MeSH PA | D058828 | Serotonin 5-HT4 Receptor Agonists |
| FDA MoA | N0000193870 | Serotonin 4 Receptor Agonists |
| FDA EPC | N0000193871 | Serotonin-4 Receptor Agonist |
| CHEBI has role | CHEBI:35469 | antidepressant |
| CHEBI has role | CHEBI:50503 | laxative |
| CHEBI has role | CHEBI:53784 | antispasmodic drug |
| CHEBI has role | CHEBI:55324 | gastrointestinal drug |
Related Drugs by ATC class:
A06AX Other drugs for constipation 7 drugs
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 | July 10, 2028 | ADDITIONAL CLINICAL TRIAL INFORMATION ADDED TO PEDIATRIC USE SUBSECTION |
| EQ 2MG BASE | MOTEGRITY | TAKEDA PHARMS USA | N210166 | Dec. 14, 2018 | RX | TABLET | ORAL | July 10, 2028 | ADDITIONAL CLINICAL TRIAL INFORMATION ADDED TO PEDIATRIC USE SUBSECTION |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| 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 |
| DB06480 | DRUGBANK_ID |
| 0A09IUW5TP | UNII |
| 2107309 | RXNORM |
| 26947 | MMSL |
| 304089 | MMSL |
| 346516 | MMSL |
| d07541 | MMSL |
| 013402 | NDDF |
| 013403 | NDDF |
| 1149428003 | SNOMEDCT_US |
| 699273008 | SNOMEDCT_US |
| 774192009 | SNOMEDCT_US |
| C0913506 | UMLSCUI |
| 7702 | INN_ID |
| 3052762 | PUBCHEM_CID |
| 0A09IUW5TP | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Prucalopride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0749 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 26 sections |
| Prucalopride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0750 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 26 sections |
| Prucalopride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0406-6301 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 28 sections |
| Prucalopride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0406-6302 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 28 sections |
| PRUCALOPRIDE | Human Prescription Drug Label | 1 | 0781-8158 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 26 sections |
| PRUCALOPRIDE | Human Prescription Drug Label | 1 | 0781-8159 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 26 sections |
| Prucalopride | Human Prescription Drug Label | 1 | 27241-294 | TABLET | 1 mg | ORAL | ANDA | 26 sections |
| Prucalopride | Human Prescription Drug Label | 1 | 27241-295 | TABLET | 2 mg | ORAL | ANDA | 26 sections |
| PRUCALOPRIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-391 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 26 sections |
| PRUCALOPRIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-392 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 26 sections |
| MOTEGRITY | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54092-546 | TABLET, FILM COATED | 1 mg | ORAL | NDA | 28 sections |
| MOTEGRITY | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54092-547 | TABLET, FILM COATED | 2 mg | ORAL | NDA | 28 sections |
| Prucalopride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-4806 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 26 sections |
| Prucalopride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-4807 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 26 sections |
| Prucalopride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69097-218 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 17 sections |
| Prucalopride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69097-219 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 17 sections |
| Prucalopride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-2698 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 27 sections |
| Prucalopride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-2699 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 27 sections |
| Prucalopride succinate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70069-821 | TABLET | 1 mg | ORAL | ANDA | 25 sections |
| Prucalopride succinate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70069-822 | TABLET | 2 mg | ORAL | ANDA | 25 sections |
| Prucalopride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70748-389 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 24 sections |
| Prucalopride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70748-390 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 24 sections |
| prucalopride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70771-1899 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 1 sections |
| prucalopride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70771-1900 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 1 sections |
| Prucalopride | Human Prescription Drug Label | 1 | 70954-596 | TABLET | 1 mg | ORAL | ANDA | 26 sections |
| Prucalopride | Human Prescription Drug Label | 1 | 70954-597 | TABLET | 2 mg | ORAL | ANDA | 26 sections |
| PRUCALOPRIDE | Human Prescription Drug Label | 1 | 72205-218 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 24 sections |
| PRUCALOPRIDE | Human Prescription Drug Label | 1 | 72205-218 | TABLET, FILM COATED | 1 mg | ORAL | ANDA | 24 sections |
| PRUCALOPRIDE | Human Prescription Drug Label | 1 | 72205-219 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 24 sections |
| PRUCALOPRIDE | Human Prescription Drug Label | 1 | 72205-219 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 24 sections |