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| Stem definition | Drug id | CAS RN |
|---|---|---|
| immunomodulators, both stimulant/suppressive and stimulant | 5747 | 1206123-37-6 |
| Dose | Unit | Route |
|---|---|---|
| 2 | mg | O |
None
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EGFR,EIF2AK3,ERBB2,GRK2,IKBKB,ITK,MAP2K6,MAPK7,MAPKAPK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CG,PRKDC,TEK,TGFBR1 | 26 | |||
| kinase-selectivity-class | EIF2AK3,MAP2K6 | 2 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 1 |
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 10, 2023 | FDA | PFIZER 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 |
|---|---|---|---|---|---|---|
| Diabetic eye disease | 196.85 | 51.83 | 23 | 806 | 157 | 90627461 |
| Condition aggravated | 83.93 | 51.83 | 57 | 772 | 595488 | 90032130 |
| Drug ineffective | 55.70 | 51.83 | 65 | 764 | 1384233 | 89243385 |
| Type 2 diabetes mellitus | 52.98 | 51.83 | 29 | 800 | 203215 | 90424403 |
| 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 |
|---|---|---|---|---|---|---|
| Diabetic eye disease | 260.08 | 67.18 | 29 | 589 | 67 | 42620650 |
| Type 2 diabetes mellitus | 146.73 | 67.18 | 37 | 581 | 18434 | 42602283 |
| Drug ineffective | 84.81 | 67.18 | 70 | 548 | 630127 | 41990590 |
| Condition aggravated | 71.65 | 67.18 | 45 | 573 | 260709 | 42360008 |
| 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 |
|---|---|---|---|---|---|---|
| Diabetic eye disease | 466.02 | 51.74 | 52 | 1169 | 175 | 110587903 |
| Type 2 diabetes mellitus | 169.88 | 51.74 | 66 | 1155 | 177166 | 110410912 |
| Condition aggravated | 142.49 | 51.74 | 92 | 1129 | 734744 | 109853334 |
| Haematochezia | 96.25 | 51.74 | 39 | 1182 | 115485 | 110472593 |
| Colitis | 86.77 | 51.74 | 35 | 1186 | 102288 | 110485790 |
| Drug ineffective | 85.46 | 51.74 | 93 | 1128 | 1520447 | 109067631 |
| Colitis ulcerative | 85.20 | 51.74 | 32 | 1189 | 77331 | 110510747 |
| Rectal haemorrhage | 65.30 | 51.74 | 30 | 1191 | 119803 | 110468275 |
| Defaecation urgency | 55.85 | 51.74 | 14 | 1207 | 8733 | 110579345 |
| Faecal calprotectin increased | 54.30 | 51.74 | 13 | 1208 | 6706 | 110581372 |
None
| Source | Code | Description |
|---|---|---|
| ATC | L04AE05 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Sphingosine-1-phosphate (S1P) receptor modulators |
| MeSH PA | D000091369 | Immunomodulating Agents |
| MeSH PA | D007155 | Immunologic Factors |
| CHEBI has role | CHEBI:33282 | antibacterial agent |
| CHEBI has role | CHEBI:35472 | anti-inflammatory drug |
| CHEBI has role | CHEBI:35705 | immunosuppressive agent |
| CHEBI has role | CHEBI:50177 | dermatologic drug |
| CHEBI has role | CHEBI:67079 | anti-inflammatory agent |
| CHEBI has role | CHEBI:144998 | sphingosine-1-phosphate receptor 1 antagonist |
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Moderately to severely active ulcerative colitis | indication | 64766004 | DOID:8577 |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Mobitz type II atrioventricular block | contraindication | 28189009 | DOID:11312 |
| Sick sinus syndrome | contraindication | 36083008 | DOID:13884 |
| Angina pectoris | contraindication | 194828000 | |
| Decompensated cardiac failure | contraindication | 195111005 | |
| Cerebrovascular accident | contraindication | 230690007 | |
| Transient ischemic attack | contraindication | 266257000 | DOID:224 |
None
None
None
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 2MG BASE | VELSIPITY | PFIZER | N216956 | Oct. 12, 2023 | RX | TABLET | ORAL | 9126932 | July 22, 2029 | A METHOD FOR TREATING ULCERATIVE COLITIS BY ADMINISTERING A THERAPEUTICALLY EFFECTIVE AMOUNT OF ESTRASIMOD ARGININE |
| EQ 2MG BASE | VELSIPITY | PFIZER | N216956 | Oct. 12, 2023 | RX | TABLET | ORAL | 11007175 | Jan. 6, 2036 | A METHOD FOR TREATING ULCERATIVE COLITIS BY ADMINISTERING ESTRASIMOD ARGININE IN AN AMOUNT EQUIVALENT TO ABOUT 2.0 MG OF ESTRASIMOD |
| EQ 2MG BASE | VELSIPITY | PFIZER | N216956 | Oct. 12, 2023 | RX | TABLET | ORAL | 12156866 | Jan. 6, 2036 | A METHOD FOR TREATING ULCERATIVE COLITIS BY ADMINISTERING A THERAPEUTICALLY EFFECTIVE AMOUNT OF ESTRASIMOD ARGININE AS CLAIMED |
| EQ 2MG BASE | VELSIPITY | PFIZER | N216956 | Oct. 12, 2023 | RX | TABLET | ORAL | 12377071 | Jan. 6, 2036 | A METHOD FOR TREATING ULCERATIVE COLITIS BY ADMINISTERING ESTRASIMOD L-ARGININE IN AN AMOUNT EQUIVALENT TO ABOUT 2.0 MG OF ESTRASIMOD |
| EQ 2MG BASE | VELSIPITY | PFIZER | N216956 | Oct. 12, 2023 | RX | TABLET | ORAL | 10676435 | June 21, 2036 | A METHOD FOR TREATING ULCERATIVE COLITIS BY ADMINISTERING A THERAPEUTICALLY EFFECTIVE AMOUNT OF THE FORM OF ESTRASIMOD ARGININE AS CLAIMED |
| EQ 2MG BASE | VELSIPITY | PFIZER | N216956 | Oct. 12, 2023 | RX | TABLET | ORAL | 11884626 | June 21, 2036 | A METHOD FOR TREATING ULCERATIVE COLITIS BY ADMINISTERING A THERAPEUTICALLY EFFECTIVE AMOUNT OF THE FORM OF ESTRASIMOD ARGININE AS CLAIMED |
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 2MG BASE | VELSIPITY | PFIZER | N216956 | Oct. 12, 2023 | RX | TABLET | ORAL | Oct. 12, 2028 | NEW CHEMICAL ENTITY |
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Sphingosine 1-phosphate receptor 4 | GPCR | AGONIST | EC50 | 6.85 | DRUG LABEL | ||||
| Sphingosine 1-phosphate receptor 3 | GPCR | PARTIAL AGONIST | EC50 | 5.22 | DRUG LABEL | ||||
| Adenosine receptor A3 | GPCR | IC50 | 5.48 | CHEMBL | |||||
| Sphingosine 1-phosphate receptor 1 | GPCR | AGONIST | EC50 | 7.36 | DRUG LABEL | ||||
| Sphingosine 1-phosphate receptor 5 | GPCR | AGONIST | EC50 | 7.20 | DRUG LABEL |
| ID | Source |
|---|---|
| CHEBI:229230 | CHEBI |
| CHEMBL3358920 | ChEMBL_ID |
| C000656249 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9331 | IUPHAR_LIGAND_ID |
| DB14766 | DRUGBANK_ID |
| 4042709 | VANDF |
| C5139928 | UMLSCUI |
| CHEMBL3989933 | ChEMBL_ID |
| 10435 | INN_ID |
| 1206123-97-8 | SECONDARY_CAS_RN |
| 44623998 | PUBCHEM_CID |
| 372266 | MMSL |
| 42073 | MMSL |
| d10119 | MMSL |
| 019580 | NDDF |
| 019581 | NDDF |
| 6WH8495MMH | UNII |
| 2668045 | RXNORM |
| D10930 | KEGG_DRUG |
| 6WH8495MMH | INXIGHT DRUGS |
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Velsipity | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0069-0274 | TABLET, FILM COATED | 2 mg | ORAL | NDA | 29 sections |