Stem definition | Drug id | CAS RN |
---|---|---|
integrin antagonists | 5174 | 1025967-78-5 |
None
None
Date | Agency | Company | Orphan |
---|---|---|---|
July 11, 2016 | FDA | SHIRE DEV LLC |
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 |
---|---|---|---|---|---|---|
Instillation site pain | 2900.96 | 35.61 | 400 | 6603 | 463 | 56284601 |
Instillation site reaction | 2283.19 | 35.61 | 300 | 6703 | 149 | 56284915 |
Eye irritation | 1723.02 | 35.61 | 411 | 6592 | 18617 | 56266447 |
Vision blurred | 1331.20 | 35.61 | 465 | 6538 | 82478 | 56202586 |
Dysgeusia | 772.47 | 35.61 | 260 | 6743 | 40655 | 56244409 |
Instillation site irritation | 593.54 | 35.61 | 78 | 6925 | 37 | 56285027 |
Instillation site pruritus | 555.02 | 35.61 | 71 | 6932 | 14 | 56285050 |
Instillation site erythema | 513.11 | 35.61 | 67 | 6936 | 27 | 56285037 |
Eye pain | 480.29 | 35.61 | 170 | 6833 | 30677 | 56254387 |
Instillation site lacrimation | 428.86 | 35.61 | 54 | 6949 | 3 | 56285061 |
Dry eye | 423.20 | 35.61 | 161 | 6842 | 35555 | 56249509 |
Ocular hyperaemia | 329.94 | 35.61 | 118 | 6885 | 21861 | 56263203 |
Lacrimation increased | 280.95 | 35.61 | 100 | 6903 | 18248 | 56266816 |
Eye discharge | 264.90 | 35.61 | 72 | 6931 | 5381 | 56279683 |
Instillation site discharge | 258.31 | 35.61 | 33 | 6970 | 6 | 56285058 |
Instillation site swelling | 215.84 | 35.61 | 27 | 6976 | 0 | 56285064 |
Product container issue | 206.65 | 35.61 | 46 | 6957 | 1488 | 56283576 |
Eye pruritus | 193.33 | 35.61 | 71 | 6932 | 14135 | 56270929 |
Product quality issue | 171.13 | 35.61 | 82 | 6921 | 31654 | 56253410 |
Instillation site discomfort | 167.87 | 35.61 | 21 | 6982 | 0 | 56285064 |
Ocular discomfort | 147.54 | 35.61 | 42 | 6961 | 3713 | 56281351 |
Visual impairment | 143.31 | 35.61 | 98 | 6905 | 74104 | 56210960 |
Product use complaint | 141.53 | 35.61 | 36 | 6967 | 2073 | 56282991 |
Eye disorder | 116.78 | 35.61 | 55 | 6948 | 20397 | 56264667 |
Instillation site dryness | 92.46 | 35.61 | 12 | 6991 | 4 | 56285060 |
Eyelid margin crusting | 89.82 | 35.61 | 21 | 6982 | 847 | 56284217 |
Instillation site inflammation | 87.92 | 35.61 | 11 | 6992 | 0 | 56285064 |
Product packaging quantity issue | 87.78 | 35.61 | 22 | 6981 | 1192 | 56283872 |
Foreign body sensation in eyes | 86.83 | 35.61 | 24 | 6979 | 1903 | 56283161 |
Eye swelling | 82.25 | 35.61 | 44 | 6959 | 21332 | 56263732 |
Instillation site foreign body sensation | 77.31 | 35.61 | 10 | 6993 | 3 | 56285061 |
Taste disorder | 74.12 | 35.61 | 32 | 6971 | 9683 | 56275381 |
Instillation site burn | 71.94 | 35.61 | 9 | 6994 | 0 | 56285064 |
Inappropriate schedule of product administration | 70.47 | 35.61 | 68 | 6935 | 83319 | 56201745 |
Superficial injury of eye | 68.33 | 35.61 | 13 | 6990 | 188 | 56284876 |
Instillation site hypersensitivity | 55.95 | 35.61 | 7 | 6996 | 0 | 56285064 |
Product taste abnormal | 51.79 | 35.61 | 16 | 6987 | 1872 | 56283192 |
Product dose omission issue | 48.11 | 35.61 | 89 | 6914 | 204664 | 56080400 |
Instillation site paraesthesia | 47.96 | 35.61 | 6 | 6997 | 0 | 56285064 |
Swelling of eyelid | 47.47 | 35.61 | 16 | 6987 | 2469 | 56282595 |
Madarosis | 45.87 | 35.61 | 16 | 6987 | 2737 | 56282327 |
Asthenopia | 37.96 | 35.61 | 13 | 6990 | 2104 | 56282960 |
Product dispensing issue | 35.96 | 35.61 | 7 | 6996 | 115 | 56284949 |
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 |
---|---|---|---|---|---|---|
Instillation site reaction | 604.20 | 100.89 | 67 | 1068 | 19 | 31696190 |
Vision blurred | 547.63 | 100.89 | 149 | 986 | 41766 | 31654443 |
Instillation site pain | 506.86 | 100.89 | 58 | 1077 | 40 | 31696169 |
Eye irritation | 467.98 | 100.89 | 93 | 1042 | 6425 | 31689784 |
Lacrimation increased | 136.34 | 100.89 | 35 | 1100 | 7447 | 31688762 |
Instillation site lacrimation | 129.41 | 100.89 | 14 | 1121 | 0 | 31696209 |
Dry eye | 105.30 | 100.89 | 29 | 1106 | 8043 | 31688166 |
Eye pain | 101.72 | 100.89 | 31 | 1104 | 12273 | 31683936 |
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 |
---|---|---|---|---|---|---|
Instillation site pain | 2348.68 | 45.22 | 292 | 3423 | 394 | 70924335 |
Instillation site reaction | 1836.05 | 45.22 | 218 | 3497 | 129 | 70924600 |
Vision blurred | 827.13 | 45.22 | 271 | 3444 | 94713 | 70830016 |
Eye irritation | 550.19 | 45.22 | 137 | 3578 | 17651 | 70907078 |
Instillation site irritation | 430.85 | 45.22 | 50 | 3665 | 14 | 70924715 |
Instillation site erythema | 422.01 | 45.22 | 49 | 3666 | 14 | 70924715 |
Dysgeusia | 415.58 | 45.22 | 138 | 3577 | 49364 | 70875365 |
Instillation site pruritus | 364.08 | 45.22 | 42 | 3673 | 9 | 70924720 |
Instillation site lacrimation | 304.63 | 45.22 | 35 | 3680 | 6 | 70924723 |
Eye pain | 189.21 | 45.22 | 70 | 3645 | 34032 | 70890697 |
Instillation site swelling | 186.06 | 45.22 | 21 | 3694 | 0 | 70924729 |
Ocular hyperaemia | 179.86 | 45.22 | 62 | 3653 | 24577 | 70900152 |
Product quality issue | 159.50 | 45.22 | 60 | 3655 | 30501 | 70894228 |
Instillation site discomfort | 159.47 | 45.22 | 18 | 3697 | 0 | 70924729 |
Instillation site discharge | 159.47 | 45.22 | 18 | 3697 | 0 | 70924729 |
Eye discharge | 148.37 | 45.22 | 38 | 3677 | 5409 | 70919320 |
Lacrimation increased | 141.03 | 45.22 | 49 | 3666 | 19850 | 70904879 |
Dry eye | 111.24 | 45.22 | 47 | 3668 | 32235 | 70892494 |
Product container issue | 110.10 | 45.22 | 22 | 3693 | 1020 | 70923709 |
Eye pruritus | 88.28 | 45.22 | 32 | 3683 | 14615 | 70910114 |
Instillation site burn | 79.73 | 45.22 | 9 | 3706 | 0 | 70924729 |
Visual impairment | 73.36 | 45.22 | 48 | 3667 | 80202 | 70844527 |
Instillation site inflammation | 70.87 | 45.22 | 8 | 3707 | 0 | 70924729 |
Product dose omission issue | 68.96 | 45.22 | 70 | 3645 | 217398 | 70707331 |
Instillation site foreign body sensation | 62.01 | 45.22 | 7 | 3708 | 0 | 70924729 |
Eye swelling | 54.50 | 45.22 | 26 | 3689 | 23588 | 70901141 |
Inappropriate schedule of product administration | 52.27 | 45.22 | 44 | 3671 | 107511 | 70817218 |
Foreign body sensation in eyes | 50.86 | 45.22 | 13 | 3702 | 1829 | 70922900 |
Instillation site dryness | 50.72 | 45.22 | 6 | 3709 | 3 | 70924726 |
Product use complaint | 50.27 | 45.22 | 13 | 3702 | 1915 | 70922814 |
Eye disorder | 45.28 | 45.22 | 22 | 3693 | 20763 | 70903966 |
None
Source | Code | Description |
---|---|---|
ATC | S01XA25 | SENSORY ORGANS OPHTHALMOLOGICALS OTHER OPHTHALMOLOGICALS Other ophthalmologicals |
MeSH PA | D009883 | Ophthalmic Solutions |
MeSH PA | D019999 | Pharmaceutical Solutions |
FDA MoA | N0000192700 | Lymphocyte Function-Associated Antigen-1 Antagonists |
FDA EPC | N0000192701 | Lymphocyte Function-Associated Antigen-1 Antagonist |
CHEBI has role | CHEBI:35472 | anti-inflammatory drugs |
CHEBI has role | CHEBI:133024 | lymphocyte function-associated antigen-1 antagonists |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Tear film insufficiency | indication | 46152009 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 3.42 | acidic |
pKa2 | 12.3 | acidic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
5% | XIIDRA | NOVARTIS | N208073 | July 11, 2016 | RX | SOLUTION/DROPS | OPHTHALMIC | 10124000 | Nov. 5, 2024 | TREATMENT OF THE SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED) |
5% | XIIDRA | NOVARTIS | N208073 | July 11, 2016 | RX | SOLUTION/DROPS | OPHTHALMIC | 7745460 | Nov. 5, 2024 | TREATMENT OF SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED) |
5% | XIIDRA | NOVARTIS | N208073 | July 11, 2016 | RX | SOLUTION/DROPS | OPHTHALMIC | 7790743 | Nov. 5, 2024 | TREATMENT OF SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED) |
5% | XIIDRA | NOVARTIS | N208073 | July 11, 2016 | RX | SOLUTION/DROPS | OPHTHALMIC | 8592450 | May 17, 2026 | TREATMENT OF SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED) |
5% | XIIDRA | NOVARTIS | N208073 | July 11, 2016 | RX | SOLUTION/DROPS | OPHTHALMIC | 8367701 | April 15, 2029 | TREATMENT OF SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED) |
5% | XIIDRA | NOVARTIS | N208073 | July 11, 2016 | RX | SOLUTION/DROPS | OPHTHALMIC | 9447077 | April 15, 2029 | TREATMENT OF THE SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED) |
5% | XIIDRA | NOVARTIS | N208073 | July 11, 2016 | RX | SOLUTION/DROPS | OPHTHALMIC | 8168655 | May 9, 2029 | TREATMENT OF SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED) |
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Integrin alpha-L/beta-2 | Adhesion | ANTAGONIST | IC50 | 8.05 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
Intercellular adhesion molecule 1 | Antibody | IC50 | 8.53 | CHEMBL |
ID | Source |
---|---|
038E5L962W | UNII |
D10374 | KEGG_DRUG |
C3713860 | UMLSCUI |
CHEBI:133023 | CHEBI |
CHEMBL2048028 | ChEMBL_ID |
11965427 | PUBCHEM_CID |
DB11611 | DRUGBANK_ID |
CHEMBL2048409 | ChEMBL_ID |
9584 | INN_ID |
7533 | IUPHAR_LIGAND_ID |
1801820 | RXNORM |
243704 | MMSL |
31873 | MMSL |
016935 | NDDF |
720489009 | SNOMEDCT_US |
763569006 | SNOMEDCT_US |
4035938 | VANDF |
C575157 | MESH_SUPPLEMENTAL_RECORD_UI |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Xiidra | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0911 | SOLUTION/ DROPS | 50 mg | OPHTHALMIC | NDA | 24 sections |
Xiidra | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0911 | SOLUTION/ DROPS | 50 mg | OPHTHALMIC | NDA | 24 sections |
Xiidra | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54092-606 | SOLUTION/ DROPS | 50 mg | OPHTHALMIC | NDA | 23 sections |