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 | 136.65 | 14.74 | 347 | 10307 | 588129 | 50006341 |
Product dose omission issue | 65.39 | 14.74 | 129 | 10525 | 183709 | 50410761 |
Abdominal distension | 61.10 | 14.74 | 76 | 10578 | 72827 | 50521643 |
Constipation | 60.90 | 14.74 | 126 | 10528 | 185582 | 50408888 |
Inappropriate schedule of product administration | 37.91 | 14.74 | 60 | 10594 | 71771 | 50522699 |
Off label use | 37.83 | 14.74 | 198 | 10456 | 474228 | 50120242 |
Incorrect dose administered | 35.10 | 14.74 | 47 | 10607 | 48367 | 50546103 |
Headache | 34.76 | 14.74 | 203 | 10451 | 506332 | 50088138 |
Abdominal pain | 33.91 | 14.74 | 118 | 10536 | 236110 | 50358360 |
Migraine | 29.35 | 14.74 | 55 | 10599 | 75225 | 50519245 |
Product dispensing error | 26.92 | 14.74 | 19 | 10635 | 8872 | 50585598 |
Anal incontinence | 26.82 | 14.74 | 21 | 10633 | 11469 | 50583001 |
Flatulence | 25.11 | 14.74 | 31 | 10623 | 29427 | 50565043 |
Pre-existing condition improved | 23.44 | 14.74 | 16 | 10638 | 7081 | 50587389 |
Product physical issue | 22.46 | 14.74 | 13 | 10641 | 4319 | 50590151 |
Intentional product misuse | 20.57 | 14.74 | 36 | 10618 | 46698 | 50547772 |
Feeling abnormal | 19.11 | 14.74 | 64 | 10590 | 125428 | 50469042 |
Anxiety | 18.32 | 14.74 | 80 | 10574 | 177526 | 50416944 |
Muscle spasms | 18.21 | 14.74 | 63 | 10591 | 125490 | 50468980 |
Intervertebral disc compression | 18.07 | 14.74 | 7 | 10647 | 946 | 50593524 |
General physical health deterioration | 17.96 | 14.74 | 4 | 10650 | 142430 | 50452040 |
Maternal exposure during pregnancy | 17.33 | 14.74 | 6 | 10648 | 159772 | 50434698 |
Product packaging quantity issue | 17.22 | 14.74 | 7 | 10647 | 1073 | 50593397 |
Multiple sclerosis relapse | 16.25 | 14.74 | 31 | 10623 | 42933 | 50551537 |
Subacute hepatic failure | 16.09 | 14.74 | 4 | 10650 | 122 | 50594348 |
Lymph node pain | 15.99 | 14.74 | 7 | 10647 | 1288 | 50593182 |
Product storage error | 15.82 | 14.74 | 16 | 10638 | 12208 | 50582262 |
Systemic lupus erythematosus | 15.74 | 14.74 | 5 | 10649 | 140617 | 50453853 |
Surgery | 15.60 | 14.74 | 25 | 10629 | 30180 | 50564290 |
Malaise | 15.43 | 14.74 | 122 | 10532 | 335410 | 50259060 |
Treatment failure | 15.22 | 14.74 | 5 | 10649 | 137632 | 50456838 |
Glossodynia | 15.07 | 14.74 | 3 | 10651 | 115566 | 50478904 |
Dysphagia | 15.01 | 14.74 | 43 | 10611 | 77475 | 50516995 |
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 | 99.12 | 25.61 | 119 | 1984 | 332579 | 29239845 |
Prescribed underdose | 45.30 | 25.61 | 18 | 2085 | 7768 | 29564656 |
Off label use | 39.91 | 25.61 | 74 | 2029 | 300726 | 29271698 |
Drug ineffective | 38.16 | 25.61 | 81 | 2022 | 363089 | 29209335 |
Inappropriate schedule of product administration | 34.20 | 25.61 | 27 | 2076 | 44445 | 29527979 |
Incorrect dose administered | 27.46 | 25.61 | 21 | 2082 | 32963 | 29539461 |
Urinary retention | 25.88 | 25.61 | 20 | 2083 | 31878 | 29540546 |
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 | 85.07 | 16.22 | 262 | 9041 | 722442 | 63766987 |
Product dose omission issue | 56.63 | 16.22 | 101 | 9202 | 194646 | 64294783 |
Constipation | 53.17 | 16.22 | 108 | 9195 | 229229 | 64260200 |
Headache | 45.34 | 16.22 | 173 | 9130 | 529294 | 63960135 |
Incorrect dose administered | 42.47 | 16.22 | 48 | 9255 | 60717 | 64428712 |
Abdominal distension | 37.61 | 16.22 | 57 | 9246 | 95937 | 64393492 |
Inappropriate schedule of product administration | 33.63 | 16.22 | 53 | 9250 | 92233 | 64397196 |
Off label use | 29.26 | 16.22 | 173 | 9130 | 632633 | 63856796 |
Abdominal pain | 24.15 | 16.22 | 99 | 9204 | 312276 | 64177153 |
Dizziness | 22.73 | 16.22 | 122 | 9181 | 430041 | 64059388 |
Anxiety | 22.24 | 16.22 | 72 | 9231 | 202577 | 64286852 |
Flatulence | 21.29 | 16.22 | 26 | 9277 | 35640 | 64453789 |
Nausea | 20.78 | 16.22 | 188 | 9115 | 785612 | 63703817 |
Malaise | 20.67 | 16.22 | 112 | 9191 | 396135 | 64093294 |
Intervertebral disc compression | 20.25 | 16.22 | 7 | 9296 | 1004 | 64488425 |
Acute kidney injury | 20.24 | 16.22 | 21 | 9282 | 449219 | 64040210 |
Multiple sclerosis relapse | 19.87 | 16.22 | 27 | 9276 | 41108 | 64448321 |
Lymph node pain | 18.26 | 16.22 | 7 | 9296 | 1345 | 64488084 |
Feeling abnormal | 16.99 | 16.22 | 50 | 9253 | 133552 | 64355877 |
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 |
16158208 | PUBCHEM_CID |
1307404 | RXNORM |
192786 | MMSL |
28804 | MMSL |
d07902 | MMSL |
014633 | NDDF |
703126002 | SNOMEDCT_US |
703686003 | SNOMEDCT_US |
C2000261 | UMLSCUI |
CHEMBL3301676 | ChEMBL_ID |
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 |