Details of the Drug

General Information of Drug (ID: DMCF6SX)

• Drug Name: TAK-491
• Synonyms: TAK 491

Indication

Disease Entry	ICD 11	Status	REF
Hypertension	BA00-BA04	Phase 3	[1]

• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 1:
  Molecular Weight (mw); 568.5
  Logarithm of the Partition Coefficient (xlogp); 4.9
  Rotatable Bond Count (rotbonds); 10
  Hydrogen Bond Donor Count (hbonddonor); 1
  Hydrogen Bond Acceptor Count (hbondacc); 10
• Chemical Identifiers:
  Formula: C30H24N4O8
  IUPAC Name: (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-3-[[4-[2-(5-oxo-4H-1,2,4-oxadiazol-3-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylate
  Canonical SMILES: CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NOC(=O)N5)C(=O)OCC6=C(OC(=O)O6)C
  InChI: InChI=1S/C30H24N4O8/c1-3-38-28-31-23-10-6-9-22(27(35)39-16-24-17(2)40-30(37)41-24)25(23)34(28)15-18-11-13-19(14-12-18)20-7-4-5-8-21(20)26-32-29(36)42-33-26/h4-14H,3,15-16H2,1-2H3,(H,32,33,36)
  InChIKey: QJFSABGVXDWMIW-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 135409642
  ChEBI ID: CHEBI:68845
  CAS Number: 863031-21-4
  TTD ID: D0A2RA
  ACDINA ID: D00055

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Angiotensin II receptor type-1 (AGTR1)	TT8DBY3	AGTR1_HUMAN	Modulator	[2]

Molecular Expression Atlas of This Drug

• The Studied Disease: Hypertension
• ICD Disease Classification: BA00-BA04

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Angiotensin II receptor type-1 (AGTR1)	DTT	AGTR1	8.95E-01	1.34E-02	0.07

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as TAK-491

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Disease	REF
Aliskiren	DM1BV7W	Major	Increased risk of hyperkalemia by the combination of TAK-491 and Aliskiren.	Hypertension [BA00-BA04]	[3]

Coadministration of a Drug Treating the Disease Different from TAK-491 (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
OPC-34712	DMHG57U	Moderate	Additive hypotensive effects by the combination of TAK-491 and OPC-34712.	Depression [6A70-6A7Z]	[4]
Ozanimod	DMT6AM2	Moderate	Additive hypotensive effects by the combination of TAK-491 and Ozanimod.	Multiple sclerosis [8A40]	[5]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Fumaric acid	E00420	444972	Acidulant; Antioxidant; Complexing agent; Flavoring agent; Solubilizing agent
Mannitol	E00103	6251	Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Carmellose sodium	E00625	Not Available	Disintegrant
Magnesium stearate	E00208	11177	lubricant
Sodium hydroxide	E00234	14798	Alkalizing agent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Azilsartan medoxomil 40 mg tablet	40 mg	Oral Tablet	Oral
Azilsartan medoxomil 80 mg tablet	80 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] ClinicalTrials.gov (NCT02480764) TAK-491 (Azilsartan Medoxomil) Compared to Valsartan in Chinese Participants With Hypertension.
• [2] 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
• [3] Health Canada "Potential risks of cardiovascular and renal adverse events in patients with type 2 diabetes treated with aliskiren (RASILEZ) or aliskiren/hydrochlorothiazide (RASILEZ HCT)." .
• [4] Aronowitz JS, Chakos MH, Safferman AZ, Lieberman JA "Syncope associated with the combination of clozapine and enalapril." J Clin Psychopharmacol 14 (1994): 429-30. [PMID: 7884028]
• [5] Ban TA "Drug interactions with psychoactive drugs." Dis Nerv Syst 36 (1975): 164-6. [PMID: 1116424]