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| Stem definition | Drug id | CAS RN |
|---|---|---|
| angiotensin II receptor antagonists, antihypertensive (non-peptidic) | 4322 | 863031-21-4 |
| Dose | Unit | Route |
|---|---|---|
| 40 | mg | O |
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 60 % |
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,ERBB2,GRK2,GSK3B,ITK,JAK2,MAP3K21,MAP3K7,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PRKDC,STK33,TEK,TTK | 35 | |||
| kinase-selectivity-class | AXL,GRK2,MAP2K6,TEK | 4 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 25, 2011 | FDA | ARBOR PHARMS IRELAND | |
| Dec. 7, 2011 | EMA | Takeda Pharma A/S | |
| Jan. 18, 2001 | PMDA | TAKEDA PHARMACEUTICAL COMPANY LIMITED |
| 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 |
|---|---|---|---|---|---|---|
| Renal impairment | 105.51 | 24.20 | 59 | 3301 | 105362 | 90519725 |
| Platelet count decreased | 88.76 | 24.20 | 58 | 3302 | 136911 | 90488176 |
| Hepatic function abnormal | 78.52 | 24.20 | 37 | 3323 | 46251 | 90578836 |
| Cerebral infarction | 73.57 | 24.20 | 30 | 3330 | 26566 | 90598521 |
| Hyperkalaemia | 50.74 | 24.20 | 31 | 3329 | 64933 | 90560154 |
| Decreased appetite | 46.26 | 24.20 | 63 | 3297 | 376477 | 90248610 |
| Interstitial lung disease | 46.13 | 24.20 | 31 | 3329 | 76374 | 90548713 |
| Cardiac failure | 38.25 | 24.20 | 32 | 3328 | 109464 | 90515623 |
| Proteinuria | 37.58 | 24.20 | 18 | 3342 | 23273 | 90601814 |
| Altered state of consciousness | 35.19 | 24.20 | 19 | 3341 | 31513 | 90593574 |
| Glomerular filtration rate decreased | 27.05 | 24.20 | 13 | 3347 | 16919 | 90608168 |
| Blood creatinine increased | 26.20 | 24.20 | 25 | 3335 | 101361 | 90523726 |
| Palmar-plantar erythrodysaesthesia syndrome | 26.12 | 24.20 | 15 | 3345 | 28008 | 90597079 |
| Malignant neoplasm progression | 25.08 | 24.20 | 25 | 3335 | 106845 | 90518242 |
| Blood pressure decreased | 24.32 | 24.20 | 21 | 3339 | 74874 | 90550213 |
| 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 |
|---|---|---|---|---|---|---|
| Cerebral infarction | 123.54 | 20.57 | 61 | 4230 | 31108 | 42585936 |
| Renal impairment | 103.92 | 20.57 | 87 | 4204 | 110141 | 42506903 |
| Hepatic function abnormal | 85.08 | 20.57 | 57 | 4234 | 51510 | 42565534 |
| Interstitial lung disease | 69.87 | 20.57 | 60 | 4231 | 78402 | 42538642 |
| Fibrillary glomerulonephritis | 48.64 | 20.57 | 8 | 4283 | 59 | 42616985 |
| Proteinuria | 46.72 | 20.57 | 29 | 4262 | 22954 | 42594090 |
| Decreased appetite | 44.70 | 20.57 | 74 | 4217 | 193063 | 42423981 |
| Pemphigoid | 38.24 | 20.57 | 20 | 4271 | 11447 | 42605597 |
| Palmar-plantar erythrodysaesthesia syndrome | 36.92 | 20.57 | 24 | 4267 | 20558 | 42596486 |
| Altered state of consciousness | 35.83 | 20.57 | 27 | 4264 | 29232 | 42587812 |
| Cardiac failure | 31.74 | 20.57 | 46 | 4245 | 106810 | 42510234 |
| Nephrotic syndrome | 31.35 | 20.57 | 16 | 4275 | 8702 | 42608342 |
| Thalamus haemorrhage | 30.55 | 20.57 | 9 | 4282 | 1110 | 42615934 |
| Thrombotic cerebral infarction | 28.05 | 20.57 | 7 | 4284 | 462 | 42616582 |
| Hyperkalaemia | 27.40 | 20.57 | 37 | 4254 | 80421 | 42536623 |
| Hepatocellular carcinoma | 26.49 | 20.57 | 14 | 4277 | 8180 | 42608864 |
| Liver disorder | 24.91 | 20.57 | 25 | 4266 | 39619 | 42577425 |
| Cerebral haemorrhage | 23.44 | 20.57 | 24 | 4267 | 38942 | 42578102 |
| Intestinal ischaemia | 22.04 | 20.57 | 13 | 4278 | 9375 | 42607669 |
| Hyperuricaemia | 21.99 | 20.57 | 13 | 4278 | 9411 | 42607633 |
| Blood pressure decreased | 21.66 | 20.57 | 28 | 4263 | 58304 | 42558740 |
| Gastric ulcer haemorrhage | 21.32 | 20.57 | 11 | 4280 | 6116 | 42610928 |
| Gastrointestinal hypomotility | 21.03 | 20.57 | 7 | 4284 | 1286 | 42615758 |
| Fulminant type 1 diabetes mellitus | 20.61 | 20.57 | 7 | 4284 | 1367 | 42615677 |
| 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 |
|---|---|---|---|---|---|---|
| Renal impairment | 193.87 | 18.06 | 136 | 7706 | 188309 | 110393148 |
| Cerebral infarction | 189.23 | 18.06 | 86 | 7756 | 51752 | 110529705 |
| Hepatic function abnormal | 155.66 | 18.06 | 90 | 7752 | 89205 | 110492252 |
| Interstitial lung disease | 114.71 | 18.06 | 88 | 7754 | 139246 | 110442211 |
| Decreased appetite | 79.68 | 18.06 | 130 | 7712 | 475716 | 110105741 |
| Proteinuria | 79.56 | 18.06 | 44 | 7798 | 39974 | 110541483 |
| Platelet count decreased | 76.83 | 18.06 | 88 | 7754 | 230355 | 110351102 |
| Altered state of consciousness | 69.56 | 18.06 | 46 | 7796 | 57580 | 110523877 |
| Hyperkalaemia | 68.95 | 18.06 | 65 | 7777 | 135731 | 110445726 |
| Cardiac failure | 64.80 | 18.06 | 73 | 7769 | 187553 | 110393904 |
| Palmar-plantar erythrodysaesthesia syndrome | 55.04 | 18.06 | 35 | 7807 | 40990 | 110540467 |
| Thalamus haemorrhage | 50.70 | 18.06 | 14 | 7828 | 1950 | 110579507 |
| Fibrillary glomerulonephritis | 50.22 | 18.06 | 8 | 7834 | 70 | 110581387 |
| Pemphigoid | 48.54 | 18.06 | 25 | 7817 | 19682 | 110561775 |
| Malignant neoplasm progression | 47.23 | 18.06 | 60 | 7782 | 174507 | 110406950 |
| Blood pressure decreased | 45.31 | 18.06 | 48 | 7794 | 115043 | 110466414 |
| Thrombotic cerebral infarction | 41.86 | 18.06 | 10 | 7832 | 784 | 110580673 |
| Cerebral haemorrhage | 38.62 | 18.06 | 34 | 7808 | 64934 | 110516523 |
| Nephrotic syndrome | 38.32 | 18.06 | 19 | 7823 | 13812 | 110567645 |
| Aortic dissection | 38.01 | 18.06 | 14 | 7828 | 4919 | 110576538 |
| Hyperuricaemia | 37.43 | 18.06 | 19 | 7823 | 14512 | 110566945 |
| Glomerular filtration rate decreased | 34.65 | 18.06 | 23 | 7819 | 28933 | 110552524 |
| Hypothyroidism | 33.39 | 18.06 | 33 | 7809 | 72866 | 110508591 |
| Dehydration | 33.35 | 18.06 | 66 | 7776 | 279445 | 110302012 |
| Liver disorder | 32.46 | 18.06 | 45 | 7797 | 142198 | 110439259 |
| Fulminant type 1 diabetes mellitus | 31.06 | 18.06 | 10 | 7832 | 2353 | 110579104 |
| Pyelonephritis | 30.08 | 18.06 | 20 | 7822 | 25230 | 110556227 |
| Sinus node dysfunction | 29.81 | 18.06 | 14 | 7828 | 9033 | 110572424 |
| Hepatocellular carcinoma | 28.64 | 18.06 | 14 | 7828 | 9866 | 110571591 |
| Blood creatinine increased | 27.86 | 18.06 | 48 | 7794 | 182841 | 110398616 |
| Renal disorder | 27.63 | 18.06 | 25 | 7817 | 49454 | 110532003 |
| Enterocolitis | 27.50 | 18.06 | 17 | 7825 | 18932 | 110562525 |
| Cholangitis | 27.18 | 18.06 | 16 | 7826 | 16319 | 110565138 |
| Pain | 24.72 | 18.06 | 19 | 7823 | 954936 | 109626521 |
| Immune-mediated enterocolitis | 22.45 | 18.06 | 12 | 7830 | 10173 | 110571284 |
| Anaemia | 22.21 | 18.06 | 87 | 7755 | 546999 | 110034458 |
| Secondary adrenocortical insufficiency | 21.51 | 18.06 | 9 | 7833 | 4425 | 110577032 |
| Confusional state | 20.82 | 18.06 | 4 | 7838 | 468676 | 110112781 |
| Urinary retention | 20.50 | 18.06 | 25 | 7817 | 69658 | 110511799 |
| Diarrhoea | 20.26 | 18.06 | 144 | 7698 | 1139361 | 109442096 |
| Rhabdomyolysis | 20.19 | 18.06 | 33 | 7809 | 120368 | 110461089 |
| Gastric ulcer haemorrhage | 19.78 | 18.06 | 11 | 7831 | 10083 | 110571374 |
| Intestinal ischaemia | 19.72 | 18.06 | 13 | 7829 | 16166 | 110565291 |
| Joint swelling | 19.21 | 18.06 | 4 | 7838 | 442841 | 110138616 |
| Pneumonia aspiration | 18.97 | 18.06 | 26 | 7816 | 81207 | 110500250 |
| Erythema multiforme | 18.81 | 18.06 | 14 | 7828 | 21083 | 110560374 |
| Dyslalia | 18.72 | 18.06 | 6 | 7836 | 1391 | 110580066 |
| Shunt stenosis | 18.64 | 18.06 | 6 | 7836 | 1410 | 110580047 |
| Haemorrhagic cerebral infarction | 18.32 | 18.06 | 6 | 7836 | 1489 | 110579968 |
| Spinal compression fracture | 18.21 | 18.06 | 13 | 7829 | 18379 | 110563078 |
None
| Source | Code | Description |
|---|---|---|
| ATC | C09CA09 | CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), PLAIN Angiotensin II receptor blockers (ARBs), plain |
| ATC | C09DA09 | CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS Angiotensin II receptor blockers (ARBs) and diuretics |
| FDA EPC | N0000175561 | Angiotensin 2 Receptor Blocker |
| MeSH PA | D047228 | Angiotensin II Type 1 Receptor Blockers |
| MeSH PA | D057911 | Angiotensin Receptor Antagonists |
| FDA PE | N0000178477 | Decreased Blood Pressure |
| FDA MoA | N0000180999 | Angiotensin 2 Type 1 Receptor Antagonists |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
| CHEBI has role | CHEBI:50266 | prodrug |
| CHEBI has role | CHEBI:61016 | angiotensin receptor antagonist |
| CHEBI has role | CHEBI:22587 | antiviral agent |
| CHEBI has role | CHEBI:35526 | hypoglycemic agent |
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
| Hypovolemia | contraindication | 28560003 | |
| Low blood pressure | contraindication | 45007003 | |
| Hyponatremia | contraindication | 89627008 | |
| Impaired renal function disorder | contraindication | 197663003 | |
| Pregnancy, function | contraindication | 289908002 | |
| Renal artery stenosis | contraindication | 302233006 |
None
None
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.11 | acidic |
| pKa2 | 3.02 | Basic |
| pKa3 | 2.4 | Basic |
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 40MG MEDOXOMIL;12.5MG | EDARBYCLOR | AZURITY | N202331 | Dec. 20, 2011 | RX | TABLET | ORAL | 9387249 | July 1, 2031 | TREATMENT OF HYPERTENSION |
| EQ 40MG MEDOXOMIL;25MG | EDARBYCLOR | AZURITY | N202331 | Dec. 20, 2011 | RX | TABLET | ORAL | 9387249 | July 1, 2031 | TREATMENT OF HYPERTENSION |
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 40MG MEDOXOMIL | AZILSARTAN MEDOXOMIL | LUPIN | A214489 | July 20, 2022 | RX | TABLET | ORAL | Dec. 12, 2026 | PATENT CHALLENGE |
| EQ 80MG MEDOXOMIL | AZILSARTAN MEDOXOMIL | LUPIN | A214489 | July 20, 2022 | RX | TABLET | ORAL | Dec. 12, 2026 | PATENT CHALLENGE |
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Type-1 angiotensin II receptor | GPCR | ANTAGONIST | IC50 | 8.13 | IUPHAR | CHEMBL | |||
| Type-2 angiotensin II receptor | GPCR | IC50 | 8.59 | CHEMBL | |||||
| Type-1 angiotensin II receptor | GPCR | IC50 | 6.38 | CHEMBL |
| ID | Source |
|---|---|
| D08067 | KEGG_DRUG |
| 4030593 | VANDF |
| 4030594 | VANDF |
| C2698291 | UMLSCUI |
| CHEBI:68845 | CHEBI |
| CHEMBL2028661 | ChEMBL_ID |
| CHEMBL2103795 | ChEMBL_ID |
| DB08822 | DRUGBANK_ID |
| C557413 | MESH_SUPPLEMENTAL_RECORD_UI |
| 6900 | IUPHAR_LIGAND_ID |
| 8874 | INN_ID |
| LL0G25K7I2 | UNII |
| 135409642 | PUBCHEM_CID |
| 1091642 | RXNORM |
| 180314 | MMSL |
| 27787 | MMSL |
| 403028 | MMSL |
| d07754 | MMSL |
| 013661 | NDDF |
| 013662 | NDDF |
| 448917007 | SNOMEDCT_US |
| 449042005 | SNOMEDCT_US |
| 449561004 | SNOMEDCT_US |
| C1958569 | UMLSCUI |
| A1IPH | PDB_CHEM_ID |
| CHEMBL57242 | ChEMBL_ID |
| 147403-03-0 | SECONDARY_CAS_RN |
| 135415867 | PUBCHEM_CID |
| 6901 | IUPHAR_LIGAND_ID |
| 8724 | INN_ID |
| C521273 | MESH_SUPPLEMENTAL_RECORD_UI |
| F9NUX55P23 | UNII |
| CHEBI:68850 | CHEBI |
| F9NUX55P23 | INXIGHT DRUGS |
| LL0G25K7I2 | INXIGHT DRUGS |
None