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| Stem definition | Drug id | CAS RN |
|---|---|---|
| histamine-H1 receptor antagonists, tricyclic compounds | 4165 | 147084-10-4 |
None
None
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,CAMK2D,EGFR,EIF2AK3,GRK2,ITK,MAPK10,MET,PDK1,PDK2,PDK4,PRKDC | 12 | |||
| kinase-selectivity-class | AXL,CAMK2D,SIK2 | 3 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 28, 2010 | FDA | ALLERGAN |
| 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 |
|---|---|---|---|---|---|---|
| Ocular hyperaemia | 436.36 | 86.48 | 84 | 419 | 33714 | 90594230 |
| Eye irritation | 209.20 | 86.48 | 46 | 457 | 33932 | 90594012 |
| Scleral hyperaemia | 130.16 | 86.48 | 16 | 487 | 300 | 90627644 |
| Eye pruritus | 107.02 | 86.48 | 26 | 477 | 29001 | 90598943 |
| Eyelid oedema | 95.35 | 86.48 | 20 | 483 | 11514 | 90616430 |
| Eye swelling | 91.52 | 86.48 | 23 | 480 | 29363 | 90598581 |
None
| 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 |
|---|---|---|---|---|---|---|
| Ocular hyperaemia | 343.94 | 101.99 | 66 | 341 | 39220 | 110549672 |
| Eye irritation | 187.61 | 101.99 | 39 | 368 | 33413 | 110555479 |
| Scleral hyperaemia | 136.24 | 101.99 | 16 | 391 | 311 | 110588581 |
None
| Source | Code | Description |
|---|---|---|
| ATC | S01GX11 | SENSORY ORGANS OPHTHALMOLOGICALS DECONGESTANTS AND ANTIALLERGICS Other antiallergics |
| FDA MoA | N0000000190 | Histamine H1 Receptor Antagonists |
| MeSH PA | D006633 | Histamine Antagonists |
| MeSH PA | D006634 | Histamine H1 Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018494 | Histamine Agents |
| FDA EPC | N0000175587 | Histamine-1 Receptor Antagonist |
| CHEBI has role | CHEBI:37955 | H<small><sub>1</sub></small>-receptor antagonist |
| CHEBI has role | CHEBI:50857 | anti-allergic agent |
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Allergic conjunctivitis | indication | 473460002 | DOID:11204 |
None
None
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.27 | Basic |
| pKa2 | 2.99 | Basic |
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 0.25% | LASTACAFT | ABBVIE | N022134 | July 28, 2010 | OTC | SOLUTION/DROPS | OPHTHALMIC | 10617695 | March 19, 2027 | USE OF LASTACAFT TO TEMPORARY RELIEVE ITCHY EYES DUE TO POLLEN, RAGWEED, GRASS, ANIMAL HAIR AND DANDER |
| 0.25% | LASTACAFT | ABBVIE | N022134 | July 28, 2010 | OTC | SOLUTION/DROPS | OPHTHALMIC | 8664215 | Dec. 23, 2027 | USE OF LASTACAFT TO TEMPORARY RELIEVE ITCHY EYES DUE TO POLLEN, RAGWEED, GRASS, ANIMAL HAIR AND DANDER |
None
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Histamine H1 receptor | GPCR | ANTAGONIST | CHEMBL | CHEMBL |
| ID | Source |
|---|---|
| 4030132 | VUID |
| N0000181719 | NUI |
| D06552 | KEGG_DRUG |
| 4030132 | VANDF |
| C2348241 | UMLSCUI |
| CHEBI:71023 | CHEBI |
| CHEMBL1201747 | ChEMBL_ID |
| DB06766 | DRUGBANK_ID |
| C557708 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7587 | IUPHAR_LIGAND_ID |
| 8707 | INN_ID |
| 7Z8O94ECSX | UNII |
| 19371515 | PUBCHEM_CID |
| 1000082 | RXNORM |
| 175605 | MMSL |
| 27322 | MMSL |
| 013612 | NDDF |
| 447208001 | SNOMEDCT_US |
| 447209009 | SNOMEDCT_US |
| 7Z8O94ECSX | INXIGHT DRUGS |
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| LASTACAFT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0023-4290 | SOLUTION/ DROPS | 2.50 mg | OPHTHALMIC | NDA | 24 sections |
| LASTACAFT | HUMAN OTC DRUG LABEL | 1 | 0023-4291 | SOLUTION/ DROPS | 2.50 mg | OPHTHALMIC | NDA | 13 sections |
| LASTACAFT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42254-288 | SOLUTION/ DROPS | 2.50 mg | OPHTHALMIC | NDA | 23 sections |
| LASTACAFT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-6294 | SOLUTION/ DROPS | 2.50 mg | OPHTHALMIC | NDA | 23 sections |
| Alcaftadine | Human OTC Drug Label | 1 | 58602-605 | SOLUTION/ DROPS | 2.50 mg | OPHTHALMIC | ANDA | 13 sections |
| alcaftadine | Human OTC Drug Label | 1 | 62332-147 | SOLUTION/ DROPS | 2.50 mg | OPHTHALMIC | ANDA | 12 sections |
| Alcaftadine | Human OTC Drug Label | 1 | 68083-649 | SOLUTION/ DROPS | 2.50 mg | OPHTHALMIC | ANDA | 12 sections |