Stem definition | Drug id | CAS RN |
---|---|---|
peptides and glycopeptides | 4622 | 851199-59-2 |
Dose | Unit | Route |
---|---|---|
0.29 | mg | O |
None
Date | Agency | Company | Orphan |
---|---|---|---|
Aug. 30, 2012 | FDA | FOREST LABS LLC | |
Dec. 19, 2016 | PMDA | ASTELLAS PHARMA INC. |
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 |
---|---|---|---|---|---|---|
Diarrhoea | 135.33 | 15.02 | 358 | 11184 | 638149 | 55642376 |
Constipation | 102.41 | 15.02 | 163 | 11379 | 201780 | 56078745 |
Product dose omission issue | 80.95 | 15.02 | 148 | 11394 | 204605 | 56075920 |
Abdominal distension | 62.05 | 15.02 | 78 | 11464 | 77548 | 56202977 |
Abdominal pain | 38.91 | 15.02 | 129 | 11413 | 258676 | 56021849 |
Rheumatoid arthritis | 38.81 | 15.02 | 15 | 11527 | 382589 | 55897936 |
Inappropriate schedule of product administration | 37.67 | 15.02 | 64 | 11478 | 83323 | 56197202 |
Headache | 35.30 | 15.02 | 215 | 11327 | 558829 | 55721696 |
Incorrect dose administered | 34.55 | 15.02 | 48 | 11494 | 52499 | 56228026 |
Off label use | 33.28 | 15.02 | 211 | 11331 | 555969 | 55724556 |
Migraine | 33.27 | 15.02 | 62 | 11480 | 86735 | 56193790 |
Anal incontinence | 30.38 | 15.02 | 23 | 11519 | 12275 | 56268250 |
Product dispensing error | 26.67 | 15.02 | 19 | 11523 | 9245 | 56271280 |
Pre-existing condition improved | 25.61 | 15.02 | 17 | 11525 | 7381 | 56273144 |
Product physical issue | 24.77 | 15.02 | 14 | 11528 | 4568 | 56275957 |
Flatulence | 24.28 | 15.02 | 31 | 11511 | 31257 | 56249268 |
Feeling abnormal | 23.15 | 15.02 | 70 | 11472 | 133532 | 56146993 |
General physical health deterioration | 22.24 | 15.02 | 4 | 11538 | 170006 | 56110519 |
Systemic lupus erythematosus | 21.97 | 15.02 | 5 | 11537 | 180073 | 56100452 |
Illness | 21.90 | 15.02 | 31 | 11511 | 34480 | 56246045 |
Maternal exposure during pregnancy | 21.70 | 15.02 | 6 | 11536 | 189547 | 56090978 |
Glossodynia | 21.26 | 15.02 | 3 | 11539 | 152455 | 56128070 |
Surgery | 20.34 | 15.02 | 29 | 11513 | 32457 | 56248068 |
Treatment failure | 20.26 | 15.02 | 5 | 11537 | 170387 | 56110138 |
Anxiety | 18.84 | 15.02 | 84 | 11458 | 193088 | 56087437 |
Intentional product misuse | 18.74 | 15.02 | 36 | 11506 | 51468 | 56229057 |
Muscle spasms | 18.43 | 15.02 | 66 | 11476 | 137305 | 56143220 |
Intervertebral disc compression | 18.05 | 15.02 | 7 | 11535 | 974 | 56279551 |
Malaise | 17.44 | 15.02 | 132 | 11410 | 367728 | 55912797 |
Arthropathy | 16.98 | 15.02 | 10 | 11532 | 200265 | 56080260 |
Product storage error | 16.94 | 15.02 | 17 | 11525 | 13196 | 56267329 |
Wound | 16.64 | 15.02 | 4 | 11538 | 138800 | 56141725 |
Product packaging quantity issue | 16.61 | 15.02 | 7 | 11535 | 1207 | 56279318 |
Drug intolerance | 16.48 | 15.02 | 18 | 11524 | 264800 | 56015725 |
Therapy interrupted | 16.23 | 15.02 | 23 | 11519 | 25602 | 56254923 |
Contraindicated product administered | 16.22 | 15.02 | 9 | 11533 | 186277 | 56094248 |
Subacute hepatic failure | 16.20 | 15.02 | 4 | 11538 | 122 | 56280403 |
Thrombocytopenia | 16.18 | 15.02 | 4 | 11538 | 136220 | 56144305 |
Lymph node pain | 15.97 | 15.02 | 7 | 11535 | 1328 | 56279197 |
Impaired gastric emptying | 15.87 | 15.02 | 14 | 11528 | 9249 | 56271276 |
Multiple sclerosis relapse | 15.86 | 15.02 | 31 | 11511 | 44872 | 56235653 |
Gastrointestinal infection | 15.71 | 15.02 | 13 | 11529 | 7881 | 56272644 |
Infusion related reaction | 15.61 | 15.02 | 12 | 11530 | 208919 | 56071606 |
Nausea | 15.60 | 15.02 | 231 | 11311 | 763947 | 55516578 |
Completed suicide | 15.22 | 15.02 | 61 | 11481 | 133772 | 56146753 |
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 |
---|---|---|---|---|---|---|
Diarrhoea | 99.48 | 23.73 | 123 | 2141 | 352286 | 31342794 |
Constipation | 51.12 | 23.73 | 53 | 2211 | 123938 | 31571142 |
Prescribed underdose | 44.14 | 23.73 | 18 | 2246 | 8260 | 31686820 |
Off label use | 41.59 | 23.73 | 82 | 2182 | 347192 | 31347888 |
Drug ineffective | 34.28 | 23.73 | 82 | 2182 | 395491 | 31299589 |
Inappropriate schedule of product administration | 30.93 | 23.73 | 27 | 2237 | 50796 | 31644284 |
Incorrect dose administered | 25.88 | 23.73 | 21 | 2243 | 35731 | 31659349 |
Urinary retention | 24.81 | 23.73 | 20 | 2244 | 33705 | 31661375 |
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 |
---|---|---|---|---|---|---|
Constipation | 100.61 | 16.36 | 149 | 9849 | 252289 | 70666157 |
Diarrhoea | 86.80 | 16.36 | 274 | 9724 | 783067 | 70135379 |
Product dose omission issue | 66.74 | 16.36 | 114 | 9884 | 217354 | 70701092 |
Headache | 45.84 | 16.36 | 182 | 9816 | 580223 | 70338223 |
Incorrect dose administered | 41.36 | 16.36 | 49 | 9949 | 66670 | 70851776 |
Abdominal distension | 37.63 | 16.36 | 59 | 9939 | 104610 | 70813836 |
Inappropriate schedule of product administration | 29.83 | 16.36 | 54 | 9944 | 107501 | 70810945 |
Abdominal pain | 26.67 | 16.36 | 107 | 9891 | 342020 | 70576426 |
Off label use | 26.47 | 16.36 | 187 | 9811 | 742873 | 70175573 |
Malaise | 23.73 | 16.36 | 122 | 9876 | 432810 | 70485636 |
Nausea | 23.46 | 16.36 | 202 | 9796 | 851886 | 70066560 |
Dizziness | 22.85 | 16.36 | 127 | 9871 | 464014 | 70454432 |
Acute kidney injury | 20.54 | 16.36 | 22 | 9976 | 474602 | 70443844 |
Anxiety | 20.53 | 16.36 | 73 | 9925 | 220257 | 70698189 |
Flatulence | 20.35 | 16.36 | 26 | 9972 | 38155 | 70880291 |
Intervertebral disc compression | 20.13 | 16.36 | 7 | 9991 | 1046 | 70917400 |
Feeling abnormal | 19.59 | 16.36 | 54 | 9944 | 142265 | 70776181 |
Multiple sclerosis relapse | 19.41 | 16.36 | 27 | 9971 | 42990 | 70875456 |
Migraine | 18.43 | 16.36 | 35 | 9963 | 72203 | 70846243 |
Lymph node pain | 17.98 | 16.36 | 7 | 9991 | 1436 | 70917010 |
Anal incontinence | 17.20 | 16.36 | 16 | 9982 | 16474 | 70901972 |
Oesophageal hypomotility | 17.16 | 16.36 | 4 | 9994 | 140 | 70918306 |
Rheumatoid arthritis | 17.04 | 16.36 | 10 | 9988 | 291795 | 70626651 |
None
Source | Code | Description |
---|---|---|
ATC | A06AX04 | ALIMENTARY TRACT AND METABOLISM DRUGS FOR CONSTIPATION DRUGS FOR CONSTIPATION Other drugs for constipation |
MeSH PA | D020536 | Enzyme Activators |
MeSH PA | D005765 | Gastrointestinal Agents |
MeSH PA | D000074268 | Guanylyl Cyclase C Agonists |
FDA MoA | N0000185499 | Guanylate Cyclase Activators |
FDA EPC | N0000185500 | Guanylate Cyclase-C Agonist |
CHEBI has role | CHEBI:68553 | GC-C agonists |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Irritable bowel syndrome | indication | 10743008 | DOID:9778 |
Chronic idiopathic constipation | indication | 82934008 | |
Irritable bowel syndrome characterized by constipation | indication | 440630006 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 3.46 | acidic |
pKa2 | 4.13 | acidic |
pKa3 | 9.65 | acidic |
pKa4 | 10.31 | acidic |
pKa5 | 12.22 | acidic |
pKa6 | 12.57 | acidic |
pKa7 | 12.94 | acidic |
pKa8 | 13.17 | acidic |
pKa9 | 13.37 | acidic |
pKa10 | 13.69 | acidic |
pKa11 | 13.86 | acidic |
pKa12 | 13.98 | acidic |
pKa13 | 6.73 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
145MCG | LINZESS | ALLERGAN | N202811 | Aug. 30, 2012 | RX | CAPSULE | ORAL | 8110553 | Jan. 28, 2024 | METHOD OF TREATING IRRITABLE BOWEL SYNDROME WITH CONSTIPATION IN ADULTS |
290MCG | LINZESS | ALLERGAN | N202811 | Aug. 30, 2012 | RX | CAPSULE | ORAL | 8110553 | Jan. 28, 2024 | METHOD OF TREATING IRRITABLE BOWEL SYNDROME WITH CONSTIPATION IN ADULTS |
72MCG | LINZESS | ALLERGAN | N202811 | Jan. 25, 2017 | RX | CAPSULE | ORAL | 8110553 | Jan. 28, 2024 | METHOD OF TREATING CHRONIC IDIOPATHIC CONSTIPATION IN ADULT PATIENTS. |
145MCG | LINZESS | ALLERGAN | N202811 | Aug. 30, 2012 | RX | CAPSULE | ORAL | 7304036 | Aug. 30, 2026 | METHOD OF TREATING CHRONIC IDIOPATHIC CONSTIPATION IN ADULT PATIENTS. |
145MCG | LINZESS | ALLERGAN | N202811 | Aug. 30, 2012 | RX | CAPSULE | ORAL | 7304036 | Aug. 30, 2026 | METHOD OF TREATING IRRITABLE BOWEL SYNDROME WITH CONSTIPATION IN ADULTS |
290MCG | LINZESS | ALLERGAN | N202811 | Aug. 30, 2012 | RX | CAPSULE | ORAL | 7304036 | Aug. 30, 2026 | METHOD OF TREATING CHRONIC IDIOPATHIC CONSTIPATION IN ADULT PATIENTS. |
290MCG | LINZESS | ALLERGAN | N202811 | Aug. 30, 2012 | RX | CAPSULE | ORAL | 7304036 | Aug. 30, 2026 | METHOD OF TREATING IRRITABLE BOWEL SYNDROME WITH CONSTIPATION IN ADULTS |
72MCG | LINZESS | ALLERGAN | N202811 | Jan. 25, 2017 | RX | CAPSULE | ORAL | 7304036 | Aug. 30, 2026 | METHOD OF TREATING CHRONIC IDIOPATHIC CONSTIPATION IN ADULT PATIENTS. |
72MCG | LINZESS | ALLERGAN | N202811 | Jan. 25, 2017 | RX | CAPSULE | ORAL | 8933030 | Feb. 17, 2031 | METHOD OF TREATING CHRONIC IDIOPATHIC CONSTIPATION IN ADULT PATIENTS. |
72MCG | LINZESS | ALLERGAN | N202811 | Jan. 25, 2017 | RX | CAPSULE | ORAL | 10702576 | Aug. 11, 2031 | METHOD OF TREATING CHRONIC IDIOPATHIC CONSTIPATION IN ADULT PATIENTS. |
145MCG | LINZESS | ALLERGAN | N202811 | Aug. 30, 2012 | RX | CAPSULE | ORAL | 8748573 | Oct. 30, 2031 | METHOD OF TREATING CHRONIC IDIOPATHIC CONSTIPATION IN ADULT PATIENTS. |
145MCG | LINZESS | ALLERGAN | N202811 | Aug. 30, 2012 | RX | CAPSULE | ORAL | 8748573 | Oct. 30, 2031 | METHOD OF TREATING IRRITABLE BOWEL SYNDROME WITH CONSTIPATION IN ADULT PATIENTS. |
290MCG | LINZESS | ALLERGAN | N202811 | Aug. 30, 2012 | RX | CAPSULE | ORAL | 8748573 | Oct. 30, 2031 | METHOD OF TREATING CHRONIC IDIOPATHIC CONSTIPATION IN ADULT PATIENTS. |
290MCG | LINZESS | ALLERGAN | N202811 | Aug. 30, 2012 | RX | CAPSULE | ORAL | 8748573 | Oct. 30, 2031 | METHOD OF TREATING IRRITABLE BOWEL SYNDROME WITH CONSTIPATION IN ADULT PATIENTS. |
145MCG | LINZESS | ALLERGAN | N202811 | Aug. 30, 2012 | RX | CAPSULE | ORAL | 9708371 | Aug. 16, 2033 | METHOD OF TREATING CHRONIC IDIOPATHIC CONSTIPATION IN ADULT PATIENTS. |
145MCG | LINZESS | ALLERGAN | N202811 | Aug. 30, 2012 | RX | CAPSULE | ORAL | 9708371 | Aug. 16, 2033 | METHOD OF TREATING IRRITABLE BOWEL SYNDROME WITH CONSTIPATION IN ADULT PATIENTS. |
290MCG | LINZESS | ALLERGAN | N202811 | Aug. 30, 2012 | RX | CAPSULE | ORAL | 9708371 | Aug. 16, 2033 | METHOD OF TREATING IRRITABLE BOWEL SYNDROME WITH CONSTIPATION IN ADULT PATIENTS. |
72MCG | LINZESS | ALLERGAN | N202811 | Jan. 25, 2017 | RX | CAPSULE | ORAL | 9708371 | Aug. 16, 2033 | METHOD OF TREATING CHRONIC IDIOPATHIC CONSTIPATION IN ADULT PATIENTS. |
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Heat-stable enterotoxin receptor | Enzyme | AGONIST | Ki | 8.91 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
Heat-stable enterotoxin receptor | Enzyme | AGONIST | Ki | 8.38 | IUPHAR |
ID | Source |
---|---|
D06612 | KEGG_DRUG |
4031965 | VANDF |
CHEBI:68551 | CHEBI |
CHEMBL3301675 | ChEMBL_ID |
C523483 | MESH_SUPPLEMENTAL_RECORD_UI |
5017 | IUPHAR_LIGAND_ID |
8802 | INN_ID |
851199-60-5 | SECONDARY_CAS_RN |
DB08890 | DRUGBANK_ID |
N0TXR0XR5X | UNII |
1307404 | RXNORM |
192786 | MMSL |
28804 | MMSL |
d07902 | MMSL |
014633 | NDDF |
703126002 | SNOMEDCT_US |
703686003 | SNOMEDCT_US |
C2000261 | UMLSCUI |
CHEMBL3301676 | ChEMBL_ID |
16158208 | PUBCHEM_CID |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Linzess | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0456-1201 | CAPSULE, GELATIN COATED | 145 ug | ORAL | NDA | 29 sections |
Linzess | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0456-1202 | CAPSULE, GELATIN COATED | 290 ug | ORAL | NDA | 29 sections |
Linzess | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0456-1203 | CAPSULE, GELATIN COATED | 72 ug | ORAL | NDA | 29 sections |