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lubiprostone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| prostaglandins | 4123 | 333963-40-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Member of a bicyclic fatty acid class of compounds derived from PROSTAGLANDIN E1 involved in chloride channel gating.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 0 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,IKBKB,ITK,JAK3,MAP2K6,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CG,PIM2,PRKDC,STK33,SYK,TEK,TGFBR1,ZAP70 | 36 | |||
| kinase-selectivity-class | AXL,EIF2AK3,GRK2,MAP2K6 | 4 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 31, 2006 | FDA | SUCAMPO PHARMA 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 |
|---|---|---|---|---|---|---|
| Dyspnoea | 85.49 | 14.61 | 253 | 9872 | 880702 | 89737620 |
| Chest discomfort | 68.83 | 14.61 | 81 | 10044 | 138284 | 90480038 |
| Urine chloride decreased | 45.01 | 14.61 | 8 | 10117 | 87 | 90618235 |
| Constipation | 44.18 | 14.61 | 97 | 10028 | 280298 | 90338024 |
| Urine sodium decreased | 40.37 | 14.61 | 8 | 10117 | 162 | 90618160 |
| Nausea | 28.84 | 14.61 | 217 | 9908 | 1110099 | 89508223 |
| Infusion related reaction | 28.35 | 14.61 | 6 | 10119 | 416774 | 90201548 |
| Drug intolerance | 25.65 | 14.61 | 9 | 10116 | 447582 | 90170740 |
| Glossodynia | 25.55 | 14.61 | 3 | 10122 | 321776 | 90296546 |
| Ileus | 24.83 | 14.61 | 18 | 10107 | 16528 | 90601794 |
| Rheumatoid arthritis | 23.11 | 14.61 | 6 | 10119 | 362608 | 90255714 |
| Impaired gastric emptying | 21.69 | 14.61 | 15 | 10110 | 12794 | 90605528 |
| Wound | 21.35 | 14.61 | 4 | 10121 | 302976 | 90315346 |
| Insurance issue | 21.35 | 14.61 | 14 | 10111 | 10944 | 90607378 |
| Systemic lupus erythematosus | 21.21 | 14.61 | 7 | 10118 | 361889 | 90256433 |
| Feeling abnormal | 21.00 | 14.61 | 53 | 10072 | 167182 | 90451140 |
| Contraindicated product administered | 20.98 | 14.61 | 5 | 10120 | 320134 | 90298188 |
| Syncope | 20.97 | 14.61 | 46 | 10079 | 132617 | 90485705 |
| Stoma site discharge | 20.89 | 14.61 | 8 | 10117 | 1981 | 90616341 |
| Abdominal distension | 20.32 | 14.61 | 45 | 10080 | 130556 | 90487766 |
| Metabolic alkalosis | 19.50 | 14.61 | 9 | 10116 | 3540 | 90614782 |
| Marasmus | 19.16 | 14.61 | 6 | 10119 | 817 | 90617505 |
| Hypokalaemia | 19.09 | 14.61 | 44 | 10081 | 131072 | 90487250 |
| Subacute hepatic failure | 18.43 | 14.61 | 4 | 10121 | 128 | 90618194 |
| Altered state of consciousness | 18.27 | 14.61 | 20 | 10105 | 31512 | 90586810 |
| Loss of consciousness | 18.19 | 14.61 | 45 | 10080 | 140193 | 90478129 |
| Cholecystitis chronic | 17.80 | 14.61 | 12 | 10113 | 9814 | 90608508 |
| Maternal exposure during pregnancy | 17.80 | 14.61 | 9 | 10116 | 360054 | 90258268 |
| Colitis ischaemic | 17.55 | 14.61 | 13 | 10112 | 12333 | 90605989 |
| Tremor | 16.64 | 14.61 | 46 | 10079 | 153127 | 90465195 |
| Fall | 16.50 | 14.61 | 101 | 10024 | 481709 | 90136613 |
| Hepatic enzyme increased | 16.41 | 14.61 | 10 | 10115 | 360726 | 90257596 |
| Pachymeningitis | 15.69 | 14.61 | 4 | 10121 | 259 | 90618063 |
| Dizziness | 15.67 | 14.61 | 116 | 10009 | 589168 | 90029154 |
| Arthropathy | 15.51 | 14.61 | 11 | 10114 | 366231 | 90252091 |
| Anxiety | 15.42 | 14.61 | 72 | 10053 | 309700 | 90308622 |
| Hepatobiliary scan abnormal | 15.42 | 14.61 | 3 | 10122 | 55 | 90618267 |
| Gastrointestinal oedema | 15.31 | 14.61 | 6 | 10119 | 1580 | 90616742 |
| Depression | 15.06 | 14.61 | 70 | 10055 | 300531 | 90317791 |
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 |
|---|---|---|---|---|---|---|
| Hepatic function abnormal | 50.24 | 18.32 | 43 | 4606 | 51524 | 42565162 |
| Toxic optic neuropathy | 44.07 | 18.32 | 12 | 4637 | 1028 | 42615658 |
| Pneumonia aspiration | 43.25 | 18.32 | 39 | 4610 | 50039 | 42566647 |
| Decreased appetite | 41.62 | 18.32 | 75 | 4574 | 193062 | 42423624 |
| Ileus | 39.22 | 18.32 | 25 | 4624 | 19114 | 42597572 |
| Interstitial lung disease | 31.91 | 18.32 | 41 | 4608 | 78421 | 42538265 |
| Constipation | 26.35 | 18.32 | 56 | 4593 | 162235 | 42454451 |
| Immobilisation syndrome | 22.56 | 18.32 | 6 | 4643 | 470 | 42616216 |
| Gastric cancer | 21.99 | 18.32 | 12 | 4637 | 6891 | 42609795 |
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 |
|---|---|---|---|---|---|---|
| Hepatic function abnormal | 60.62 | 14.11 | 62 | 12469 | 89233 | 110487535 |
| Ileus | 51.62 | 14.11 | 36 | 12495 | 30693 | 110546075 |
| Toxic optic neuropathy | 45.12 | 14.11 | 13 | 12518 | 1315 | 110575453 |
| Decreased appetite | 44.01 | 14.11 | 136 | 12395 | 475710 | 110101058 |
| Urine chloride decreased | 43.80 | 14.11 | 8 | 12523 | 101 | 110576667 |
| Chest discomfort | 41.13 | 14.11 | 72 | 12459 | 173776 | 110402992 |
| Pneumonia aspiration | 40.54 | 14.11 | 48 | 12483 | 81185 | 110495583 |
| Dyspnoea | 37.20 | 14.11 | 233 | 12298 | 1106639 | 109470129 |
| Urine sodium decreased | 36.30 | 14.11 | 8 | 12523 | 271 | 110576497 |
| Constipation | 35.63 | 14.11 | 105 | 12426 | 357681 | 110219087 |
| Interstitial lung disease | 34.64 | 14.11 | 59 | 12472 | 139275 | 110437493 |
| Altered state of consciousness | 32.02 | 14.11 | 36 | 12495 | 57590 | 110519178 |
| Stoma site discharge | 31.94 | 14.11 | 12 | 12519 | 2783 | 110573985 |
| Hypokalaemia | 31.37 | 14.11 | 66 | 12465 | 182382 | 110394386 |
| Immobilisation syndrome | 27.22 | 14.11 | 8 | 12523 | 868 | 110575900 |
| Drug intolerance | 25.94 | 14.11 | 7 | 12524 | 406505 | 110170263 |
| Marasmus | 25.84 | 14.11 | 9 | 12522 | 1682 | 110575086 |
| Dyskinesia | 25.00 | 14.11 | 30 | 12501 | 51416 | 110525352 |
| Enterocolitis | 24.58 | 14.11 | 19 | 12512 | 18930 | 110557838 |
| Nausea | 23.01 | 14.11 | 227 | 12304 | 1235463 | 109341305 |
| Blood pressure decreased | 22.59 | 14.11 | 44 | 12487 | 115047 | 110461721 |
| Diarrhoea | 22.52 | 14.11 | 212 | 12319 | 1139293 | 109437475 |
| Gastric cancer | 21.11 | 14.11 | 14 | 12517 | 10994 | 110565774 |
| Metabolic alkalosis | 21.03 | 14.11 | 11 | 12520 | 5584 | 110571184 |
| Cardiac failure chronic | 20.48 | 14.11 | 15 | 12516 | 13796 | 110562972 |
| Stoma site erythema | 20.30 | 14.11 | 8 | 12523 | 2109 | 110574659 |
| Infusion related reaction | 20.12 | 14.11 | 9 | 12522 | 381153 | 110195615 |
| Rheumatoid arthritis | 19.41 | 14.11 | 5 | 12526 | 299608 | 110277160 |
| Renal impairment | 19.39 | 14.11 | 56 | 12475 | 188389 | 110388379 |
| Pneumonia bacterial | 19.21 | 14.11 | 19 | 12512 | 26242 | 110550526 |
| Abdominal distension | 18.96 | 14.11 | 53 | 12478 | 175050 | 110401718 |
| Cholangitis | 18.24 | 14.11 | 15 | 12516 | 16320 | 110560448 |
| Colon cancer | 18.16 | 14.11 | 15 | 12516 | 16428 | 110560340 |
| Colitis ischaemic | 17.16 | 14.11 | 15 | 12516 | 17735 | 110559033 |
| Loss of consciousness | 17.08 | 14.11 | 55 | 12476 | 196251 | 110380517 |
| Erythema multiforme | 16.82 | 14.11 | 16 | 12515 | 21081 | 110555687 |
| Arthropathy | 16.46 | 14.11 | 6 | 12525 | 287516 | 110289252 |
| Cholecystitis chronic | 15.65 | 14.11 | 11 | 12520 | 9489 | 110567279 |
| Toxicity to various agents | 15.50 | 14.11 | 19 | 12512 | 480536 | 110096232 |
| Disseminated intravascular coagulation | 15.22 | 14.11 | 21 | 12510 | 41265 | 110535503 |
| Dysphagia | 15.18 | 14.11 | 45 | 12486 | 153555 | 110423213 |
| Dehydration | 14.92 | 14.11 | 67 | 12464 | 279444 | 110297324 |
| Upper respiratory tract inflammation | 14.75 | 14.11 | 8 | 12523 | 4363 | 110572405 |
| Shunt occlusion | 14.70 | 14.11 | 6 | 12525 | 1731 | 110575037 |
| Contraindicated product administered | 14.52 | 14.11 | 5 | 12526 | 248262 | 110328506 |
| Drug ineffective | 14.49 | 14.11 | 107 | 12424 | 1520433 | 109056335 |
| Platelet count decreased | 14.44 | 14.11 | 58 | 12473 | 230385 | 110346383 |
| Tremor | 14.39 | 14.11 | 53 | 12478 | 202179 | 110374589 |
| Urinary tract infection | 14.38 | 14.11 | 74 | 12457 | 326208 | 110250560 |
| Cerebral infarction | 14.28 | 14.11 | 23 | 12508 | 51815 | 110524953 |
| Feeling abnormal | 14.26 | 14.11 | 49 | 12482 | 180662 | 110396106 |
| Thyroiditis | 14.17 | 14.11 | 9 | 12522 | 6564 | 110570204 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A06AX03 | ALIMENTARY TRACT AND METABOLISM DRUGS FOR CONSTIPATION DRUGS FOR CONSTIPATION Other drugs for constipation |
| FDA MoA | N0000175456 | Chloride Channel Activators |
| FDA EPC | N0000175573 | Chloride Channel Activator |
| MeSH PA | D049990 | Membrane Transport Modulators |
| MeSH PA | D065101 | Chloride Channel Agonists |
| CHEBI has role | CHEBI:35480 | analgesic |
| CHEBI has role | CHEBI:50503 | laxative |
| CHEBI has role | CHEBI:53784 | antispasmodic drug |
| CHEBI has role | CHEBI:64946 | anti-HIV agent |
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 |
|---|---|---|---|
| Chronic idiopathic constipation | indication | 82934008 | |
| Irritable bowel syndrome characterized by constipation | indication | 440630006 | |
| Gastrointestinal obstruction | contraindication | 126765001 | |
| Pregnancy, function | contraindication | 289908002 | |
| Severe diarrhea | contraindication | 409587002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.76 | acidic |
| pKa2 | 12.62 | acidic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Chloride channel protein 2 | Ion channel | OPENER | DRUGBANK | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4025090 | VUID |
| N0000175352 | NUI |
| D04790 | KEGG_DRUG |
| 136790-76-6 | SECONDARY_CAS_RN |
| 4025090 | VANDF |
| C1684405 | UMLSCUI |
| CHEBI:34945 | CHEBI |
| CHEMBL1201134 | ChEMBL_ID |
| D000068238 | MESH_DESCRIPTOR_UI |
| DB01046 | DRUGBANK_ID |
| 4242 | IUPHAR_LIGAND_ID |
| 8254 | INN_ID |
| 7662KG2R6K | UNII |
| 157920 | PUBCHEM_CID |
| 615205 | RXNORM |
| 21067 | MMSL |
| 342325 | MMSL |
| 76092 | MMSL |
| d05736 | MMSL |
| 011200 | NDDF |
| 420304008 | SNOMEDCT_US |
| 421856003 | SNOMEDCT_US |
| 7662KG2R6K | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0254-3028 | CAPSULE, GELATIN COATED | 8 ug | ORAL | NDA AUTHORIZED GENERIC | 29 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0254-3029 | CAPSULE, GELATIN COATED | 24 ug | ORAL | NDA authorized generic | 29 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0406-6408 | CAPSULE, GELATIN COATED | 8 ug | ORAL | NDA AUTHORIZED GENERIC | 29 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0406-6424 | CAPSULE, GELATIN COATED | 24 ug | ORAL | NDA authorized generic | 29 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0480-3479 | CAPSULE, GELATIN COATED | 8 ug | ORAL | ANDA | 26 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0480-4138 | CAPSULE, GELATIN COATED | 24 ug | ORAL | ANDA | 26 sections |
| AMITIZA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-622 | CAPSULE, GELATIN COATED | 8 ug | ORAL | NDA | 26 sections |
| Amitiza | HUMAN PRESCRIPTION DRUG LABEL | 1 | 23635-508 | CAPSULE, GELATIN COATED | 8 ug | ORAL | NDA | 27 sections |
| Amitiza | HUMAN PRESCRIPTION DRUG LABEL | 1 | 23635-524 | CAPSULE, GELATIN COATED | 24 ug | ORAL | NDA | 27 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-403 | CAPSULE | 0.01 mg | ORAL | ANDA | 17 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-404 | CAPSULE | 0.02 mg | ORAL | ANDA | 17 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-475 | CAPSULE | 8 ug | ORAL | ANDA | 25 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-476 | CAPSULE | 24 ug | ORAL | ANDA | 25 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-163 | CAPSULE, GELATIN COATED | 8 ug | ORAL | NDA AUTHORIZED GENERIC | 29 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-168 | CAPSULE, GELATIN COATED | 24 ug | ORAL | NDA AUTHORIZED GENERIC | 29 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43602-548 | CAPSULE | 0.01 mg | ORAL | ANDA | 17 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43602-549 | CAPSULE | 0.02 mg | ORAL | ANDA | 17 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51407-744 | CAPSULE, GELATIN COATED | 8 ug | ORAL | NDA authorized generic | 28 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51407-745 | CAPSULE, GELATIN COATED | 24 ug | ORAL | NDA authorized generic | 28 sections |
| Amitiza | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5971 | CAPSULE, GELATIN COATED | 24 ug | ORAL | NDA | 25 sections |
| Amitiza | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-6153 | CAPSULE, GELATIN COATED | 8 ug | ORAL | NDA | 25 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55700-963 | CAPSULE, GELATIN COATED | 24 ug | ORAL | NDA AUTHORIZED GENERIC | 29 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60687-816 | CAPSULE, GELATIN COATED | 8 ug | ORAL | ANDA | 26 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60687-827 | CAPSULE, GELATIN COATED | 24 ug | ORAL | ANDA | 26 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63304-351 | CAPSULE, GELATIN COATED | 8 ug | ORAL | NDA authorized generic | 28 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63304-351 | CAPSULE, GELATIN COATED | 8 ug | ORAL | NDA authorized generic | 28 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63304-352 | CAPSULE, GELATIN COATED | 24 ug | ORAL | NDA authorized generic | 28 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63304-352 | CAPSULE, GELATIN COATED | 24 ug | ORAL | NDA authorized generic | 28 sections |
| Amitiza | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64764-080 | CAPSULE, GELATIN COATED | 8 ug | ORAL | NDA | 27 sections |
| Amitiza | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64764-240 | CAPSULE, GELATIN COATED | 24 ug | ORAL | NDA | 27 sections |