lubiprostone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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 |
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 | 87.60 | 14.20 | 234 | 7715 | 547374 | 50049801 |
| Chest discomfort | 66.03 | 14.20 | 77 | 7872 | 92645 | 50504530 |
| Urine chloride decreased | 43.09 | 14.20 | 8 | 7941 | 78 | 50597097 |
| Urine sodium decreased | 38.08 | 14.20 | 8 | 7941 | 153 | 50597022 |
| Constipation | 31.06 | 14.20 | 81 | 7868 | 185627 | 50411548 |
| Nausea | 22.04 | 14.20 | 187 | 7762 | 705211 | 49891964 |
| Ileus | 20.82 | 14.20 | 17 | 7932 | 13212 | 50583963 |
| Metabolic alkalosis | 18.83 | 14.20 | 9 | 7940 | 2722 | 50594453 |
| Drug intolerance | 17.99 | 14.20 | 6 | 7943 | 219098 | 50378077 |
| Chest pain | 17.27 | 14.20 | 64 | 7885 | 176818 | 50420357 |
| Subacute hepatic failure | 17.26 | 14.20 | 4 | 7945 | 122 | 50597053 |
| Rheumatoid arthritis | 15.85 | 14.20 | 6 | 7943 | 202544 | 50394631 |
| Impaired gastric emptying | 15.42 | 14.20 | 12 | 7937 | 8706 | 50588469 |
| Colitis ischaemic | 14.53 | 14.20 | 12 | 7937 | 9471 | 50587704 |
| Abdominal distension | 14.48 | 14.20 | 34 | 7915 | 72869 | 50524306 |
| Feeling abnormal | 14.48 | 14.20 | 48 | 7901 | 125444 | 50471731 |
| Cholecystitis chronic | 14.33 | 14.20 | 12 | 7937 | 9657 | 50587518 |
| Hepatobiliary scan abnormal | 14.20 | 14.20 | 3 | 7946 | 59 | 50597116 |
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 | 44.88 | 18.88 | 35 | 2997 | 39224 | 29532271 |
| Toxic optic neuropathy | 43.82 | 18.88 | 11 | 3021 | 730 | 29570765 |
| Decreased appetite | 26.87 | 18.88 | 51 | 2981 | 145291 | 29426204 |
| Ileus | 23.64 | 18.88 | 16 | 3016 | 14386 | 29557109 |
| Pneumonia aspiration | 20.65 | 18.88 | 22 | 3010 | 36715 | 29534780 |
| Constipation | 19.77 | 18.88 | 39 | 2993 | 114121 | 29457374 |
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 |
|---|---|---|---|---|---|---|
| Chest discomfort | 45.91 | 15.06 | 68 | 8929 | 116038 | 64373697 |
| Dyspnoea | 45.46 | 15.06 | 209 | 8788 | 718465 | 63771270 |
| Hepatic function abnormal | 43.25 | 15.06 | 49 | 8948 | 64264 | 64425471 |
| Urine chloride decreased | 42.91 | 15.06 | 8 | 8989 | 91 | 64489644 |
| Toxic optic neuropathy | 42.25 | 15.06 | 12 | 8985 | 935 | 64488800 |
| Urine sodium decreased | 34.73 | 15.06 | 8 | 8989 | 268 | 64489467 |
| Ileus | 33.79 | 15.06 | 27 | 8970 | 22939 | 64466796 |
| Altered state of consciousness | 25.68 | 15.06 | 29 | 8968 | 37873 | 64451862 |
| Decreased appetite | 24.94 | 15.06 | 91 | 8906 | 281198 | 64208537 |
| Toxicity to various agents | 24.57 | 15.06 | 10 | 8987 | 363503 | 64126232 |
| Nausea | 23.38 | 15.06 | 188 | 8809 | 785612 | 63704123 |
| Metabolic alkalosis | 22.55 | 15.06 | 11 | 8986 | 3917 | 64485818 |
| Constipation | 21.00 | 15.06 | 75 | 8922 | 229262 | 64260473 |
| Diarrhoea | 20.45 | 15.06 | 171 | 8826 | 722533 | 63767202 |
| Hypokalaemia | 19.92 | 15.06 | 49 | 8948 | 121854 | 64367881 |
| Abdominal distension | 17.20 | 15.06 | 40 | 8957 | 95954 | 64393781 |
| Interstitial lung disease | 16.73 | 15.06 | 40 | 8957 | 97692 | 64392043 |
| Colitis ischaemic | 16.05 | 15.06 | 14 | 8983 | 13400 | 64476335 |
| Stoma site pain | 15.98 | 15.06 | 6 | 8991 | 1127 | 64488608 |
| Enterocolitis | 15.31 | 15.06 | 13 | 8984 | 12005 | 64477730 |
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 | D065101 | Chloride Channel Agonists |
| MeSH PA | D049990 | Membrane Transport Modulators |
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)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 24MCG | AMITIZA | SUCAMPO PHARMA LLC | N021908 | Jan. 31, 2006 | RX | CAPSULE | ORAL | 7064148 | Aug. 30, 2022 | METHOD FOR TREATING CONSTIPATION BY OPENING CIC CHANNELS IN A MAMMALIAN SUBJECT |
| 24MCG | AMITIZA | SUCAMPO PHARMA LLC | N021908 | Jan. 31, 2006 | RX | CAPSULE | ORAL | 7064148 | Aug. 30, 2022 | METHOD FOR TREATING CONSTIPATION IN A PATIENT WITH OPIOID-INDUCED CONSTIPATION BY OPENING CIC CHANNELS |
| 8MCG | AMITIZA | SUCAMPO PHARMA LLC | N021908 | April 29, 2008 | RX | CAPSULE | ORAL | 7064148 | Aug. 30, 2022 | METHOD FOR TREATING CONSTIPATION BY OPENING CIC CHANNELS IN A MAMMALIAN SUBJECT |
| 8MCG | AMITIZA | SUCAMPO PHARMA LLC | N021908 | April 29, 2008 | RX | CAPSULE | ORAL | 7064148 | Aug. 30, 2022 | METHOD OF TREATING CONSTIPATION IN A PATIENT WITH IRRITABLE BOWEL SYNDROME BY OPENING CHLORIDE CHANNELS (CIC) |
| 24MCG | AMITIZA | SUCAMPO PHARMA LLC | N021908 | Jan. 31, 2006 | RX | CAPSULE | ORAL | 8097653 | Nov. 14, 2022 | METHOD FOR RELIEVING CONSTIPATION IN A HUMAN PATIENT THAT COMPRISES ADMINISTERING TO THE PATIENT A DOSAGE UNIT COMPRISING (I) 24MCG+/- 10% OF A DRUG SUBSTANCE AND (II) A PHARMACEUTICALLY SUITABLE EXCIPIENT |
| 24MCG | AMITIZA | SUCAMPO PHARMA LLC | N021908 | Jan. 31, 2006 | RX | CAPSULE | ORAL | 8097653 | Nov. 14, 2022 | METHOD FOR RELIEVING CONSTIPATION IN A PATIENT WITH OPIOID-INDUCED CONSTIPATION THAT COMPRISES ADMINISTERING TO THE PATIENT A DOSAGE UNIT COMPRISING(I)24MICROG+/- 10% OF A DRUG SUBSTANCE AND (II) A PHARMACEUTICALLY SUITABLE EXCIPIENT |
| 24MCG | AMITIZA | SUCAMPO PHARMA LLC | N021908 | Jan. 31, 2006 | RX | CAPSULE | ORAL | 8389542 | Nov. 14, 2022 | USE IN RELIEVING OR PREVENTING CONSTIPATION IN A HUMAN PATIENT WITH A DOSAGE UNIT COMPRISING 24MICROG+/- 10% OF A DRUG SUBSTANCE AND A PHARMACEUTICALLY SUITABLE EXCIPIENT |
| 24MCG | AMITIZA | SUCAMPO PHARMA LLC | N021908 | Jan. 31, 2006 | RX | CAPSULE | ORAL | 8389542 | Nov. 14, 2022 | USE IN RELIEVING OR PREVENTING CONSTIPATION IN A PATIENT WITH OPIOID-INDUCED CONSTIPATION WITH A DOSAGE UNIT COMPRISING 24MICROG +/- 10% OF A DRUG SUBSTANCE AND A PHARMACEUTICALLY SUITABLE EXCIPIENT |
| 24MCG | AMITIZA | SUCAMPO PHARMA LLC | N021908 | Jan. 31, 2006 | RX | CAPSULE | ORAL | 6982283 | Dec. 4, 2022 | METHOD FOR TREATING OPIOID-INDUCED CONSTIPATION |
| 8MCG | AMITIZA | SUCAMPO PHARMA LLC | N021908 | April 29, 2008 | RX | CAPSULE | ORAL | 7795312 | Sept. 17, 2024 | METHOD FOR TREATING IRRITABLE BOWEL SYNDROME AND METHOD FOR TREATING ABDOMINAL DISCOMFORT ASSOCIATED WITH IRRITABLE BOWEL SYNDROME |
| 24MCG | AMITIZA | SUCAMPO PHARMA LLC | N021908 | Jan. 31, 2006 | RX | CAPSULE | ORAL | 8748481 | Sept. 1, 2025 | METHOD FOR THE LONG TERM TREATMENT OF CHRONIC CONSTIPATION IN A HUMAN SUBJECT |
| 8MCG | AMITIZA | SUCAMPO PHARMA LLC | N021908 | April 29, 2008 | RX | CAPSULE | ORAL | 8748481 | Sept. 1, 2025 | METHOD FOR THE LONG TERM TREATMENT OF CHRONIC CONSTIPATION IN A HUMAN SUBJECT WITH IRRITABLE BOWEL SYNDROME |
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 |
| 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 |
| 136790-76-6 | SECONDARY_CAS_RN |
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 |
| AMITIZA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-622 | CAPSULE, GELATIN COATED | 8 ug | ORAL | NDA | 26 sections |
| Amitiza | HUMAN PRESCRIPTION DRUG LABEL | 1 | 35356-500 | CAPSULE, GELATIN COATED | 24 ug | ORAL | NDA | 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 |
| 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 |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-841 | CAPSULE | 8 ug | ORAL | ANDA | 25 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-841 | CAPSULE | 8 ug | ORAL | ANDA | 25 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-842 | CAPSULE | 24 ug | ORAL | ANDA | 25 sections |
| Lubiprostone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-842 | CAPSULE | 24 ug | ORAL | ANDA | 25 sections |
| Amitiza | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68151-5003 | CAPSULE, GELATIN COATED | 24 ug | ORAL | NDA | 26 sections |