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Identification
NameTasosartan
Accession NumberDB01349
TypeSmall Molecule
GroupsApproved
DescriptionTasosartan is a long-acting angiotensin II (AngII) receptor blocker. Its long duration of action has been attributed to its active metabolite enoltasosartan. It is used to treat patients with essential hypertension
Structure
Thumb
Synonyms
ANA-756
Tasosartan
WAY-ana-756
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII48G92V856H
CAS number145733-36-4
WeightAverage: 411.4591
Monoisotopic: 411.180758329
Chemical FormulaC23H21N7O
InChI KeyADXGNEYLLLSOAR-UHFFFAOYSA-N
InChI
InChI=1S/C23H21N7O/c1-14-18-11-12-21(31)30(23(18)25-15(2)24-14)13-16-7-9-17(10-8-16)19-5-3-4-6-20(19)22-26-28-29-27-22/h3-10H,11-13H2,1-2H3,(H,26,27,28,29)
IUPAC Name
2,4-dimethyl-8-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-5H,6H,7H,8H-pyrido[2,3-d]pyrimidin-7-one
SMILES
CC1=NC(C)=C2CCC(=O)N(CC3=CC=C(C=C3)C3=CC=CC=C3C3=NNN=N3)C2=N1
Pharmacology
IndicationTasosartan is infrequently in the treatment of hypertension and heart failure.
Structured Indications Not Available
PharmacodynamicsBy blocking the angiotensin II (AT1) receptor, the drug ultimately causes vasodilation, reduced secretion of vasopressin (ADH), reduced production and secretion of aldosterone, amongst other actions leading to the combined effect of a reduction of blood pressure.
Mechanism of actionTasosartan is a selective, potent, orally active and long-acting nonpeptide Angiotensin II type 1 (AT1) receptor antagonist. Tasosartan blocks the renin-angiotensin-aldosterone system (RAAS) at the level of the AT1 receptor that mediates most, if not all, of the important actions of Ang II. Tasosartan binds reversibly to the AT1 receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance. AT1 receptor antagonists avoid the nonspecificity of the Ang I converting enzyme (ACE) inhibitors.
TargetKindPharmacological actionActionsOrganismUniProt ID
Type-1 angiotensin II receptorProteinyes
antagonist
HumanP30556 details
Type-2 angiotensin II receptorProteinunknown
antagonist
HumanP50052 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AceclofenacThe risk or severity of adverse effects can be increased when Tasosartan is combined with Aceclofenac.Approved
AcetovanilloneThe risk or severity of adverse effects can be increased when Tasosartan is combined with Acetovanillone.Investigational
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Tasosartan is combined with Acetylsalicylic acid.Approved, Vet Approved
AdapaleneThe risk or severity of adverse effects can be increased when Tasosartan is combined with Adapalene.Approved
AliskirenAliskiren may increase the hyperkalemic activities of Tasosartan.Approved, Investigational
AmilorideTasosartan may increase the hyperkalemic activities of Amiloride.Approved
AmiodaroneThe metabolism of Tasosartan can be decreased when combined with Amiodarone.Approved, Investigational
AnisodamineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Anisodamine.Investigational
AntipyrineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Antipyrine.Approved
ApremilastThe risk or severity of adverse effects can be increased when Tasosartan is combined with Apremilast.Approved, Investigational
AprepitantThe serum concentration of Tasosartan can be increased when it is combined with Aprepitant.Approved, Investigational
ArdeparinArdeparin may increase the hyperkalemic activities of Tasosartan.Approved, Withdrawn
AtazanavirThe metabolism of Tasosartan can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Tasosartan can be decreased when combined with Atomoxetine.Approved
AzapropazoneThe risk or severity of adverse effects can be increased when Tasosartan is combined with Azapropazone.Withdrawn
AzelastineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Azelastine.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Tasosartan is combined with Balsalazide.Approved, Investigational
BemiparinBemiparin may increase the hyperkalemic activities of Tasosartan.Approved
BenazeprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Benazepril.Approved, Investigational
BenoxaprofenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Benoxaprofen.Withdrawn
Betulinic AcidThe risk or severity of adverse effects can be increased when Tasosartan is combined with Betulinic Acid.Investigational
BexaroteneThe serum concentration of Tasosartan can be decreased when it is combined with Bexarotene.Approved, Investigational
BoceprevirThe metabolism of Tasosartan can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Tasosartan can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Tasosartan can be decreased when it is combined with Bosentan.Approved, Investigational
BromfenacThe risk or severity of adverse effects can be increased when Tasosartan is combined with Bromfenac.Approved
BucillamineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Bucillamine.Investigational
CanagliflozinCanagliflozin may increase the hyperkalemic activities of Tasosartan.Approved
CandoxatrilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Candoxatril.Experimental
CaptoprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Captopril.Approved
CarbamazepineThe metabolism of Tasosartan can be increased when combined with Carbamazepine.Approved, Investigational
CarprofenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Carprofen.Approved, Vet Approved, Withdrawn
CastanospermineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Castanospermine.Experimental
CelecoxibThe risk or severity of adverse effects can be increased when Tasosartan is combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Tasosartan can be increased when it is combined with Ceritinib.Approved
CertoparinCertoparin may increase the hyperkalemic activities of Tasosartan.Approved
ChloroquineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Chloroquine.Approved, Vet Approved
CilazaprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Cilazapril.Approved
CiprofloxacinTasosartan may increase the arrhythmogenic activities of Ciprofloxacin.Approved, Investigational
ClarithromycinThe metabolism of Tasosartan can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Tasosartan can be decreased when combined with Clemastine.Approved
ClonixinThe risk or severity of adverse effects can be increased when Tasosartan is combined with Clonixin.Approved
ClotrimazoleThe metabolism of Tasosartan can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Tasosartan can be decreased when combined with Cobicistat.Approved
ConivaptanThe serum concentration of Tasosartan can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Tasosartan can be decreased when combined with Crizotinib.Approved
CurcuminThe risk or severity of adverse effects can be increased when Tasosartan is combined with Curcumin.Investigational
CyclosporineThe metabolism of Tasosartan can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CyclosporineTasosartan may increase the hyperkalemic activities of Cyclosporine.Approved, Investigational, Vet Approved
D-LimoneneThe risk or severity of adverse effects can be increased when Tasosartan is combined with D-Limonene.Investigational
DabrafenibThe serum concentration of Tasosartan can be decreased when it is combined with Dabrafenib.Approved
DalteparinDalteparin may increase the hyperkalemic activities of Tasosartan.Approved
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Tasosartan.Investigational
DarunavirThe metabolism of Tasosartan can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Tasosartan can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Tasosartan can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Tasosartan can be decreased when combined with Delavirdine.Approved
DexamethasoneThe serum concentration of Tasosartan can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DiclofenacThe risk or severity of adverse effects can be increased when Tasosartan is combined with Diclofenac.Approved, Vet Approved
DiflunisalThe risk or severity of adverse effects can be increased when Tasosartan is combined with Diflunisal.Approved
DihydroergotamineThe metabolism of Tasosartan can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Tasosartan can be decreased when combined with Diltiazem.Approved
DoxycyclineThe metabolism of Tasosartan can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Tasosartan can be decreased when combined with Dronedarone.Approved
DrospirenoneTasosartan may increase the hyperkalemic activities of Drospirenone.Approved
DroxicamThe risk or severity of adverse effects can be increased when Tasosartan is combined with Droxicam.Approved
DuvelisibThe risk or severity of adverse effects can be increased when Tasosartan is combined with Duvelisib.Investigational
E6201The risk or severity of adverse effects can be increased when Tasosartan is combined with E6201.Investigational
EbselenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Ebselen.Investigational
EfavirenzThe serum concentration of Tasosartan can be decreased when it is combined with Efavirenz.Approved, Investigational
EnalaprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Enalapril.Approved, Vet Approved
EnalaprilatThe risk or severity of adverse effects can be increased when Tasosartan is combined with Enalaprilat.Approved
EnoxaparinEnoxaparin may increase the hyperkalemic activities of Tasosartan.Approved
EnzalutamideThe serum concentration of Tasosartan can be decreased when it is combined with Enzalutamide.Approved
EpirizoleThe risk or severity of adverse effects can be increased when Tasosartan is combined with Epirizole.Approved
EplerenoneEplerenone may increase the hyperkalemic activities of Tasosartan.Approved
ErythromycinThe metabolism of Tasosartan can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Tasosartan can be decreased when it is combined with Eslicarbazepine acetate.Approved
EtanerceptThe risk or severity of adverse effects can be increased when Tasosartan is combined with Etanercept.Approved, Investigational
EtodolacThe risk or severity of adverse effects can be increased when Tasosartan is combined with Etodolac.Approved, Investigational, Vet Approved
EtofenamateThe risk or severity of adverse effects can be increased when Tasosartan is combined with Etofenamate.Approved
EtoricoxibThe risk or severity of adverse effects can be increased when Tasosartan is combined with Etoricoxib.Approved, Investigational
EtravirineThe serum concentration of Tasosartan can be decreased when it is combined with Etravirine.Approved
Evening primrose oilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Evening primrose oil.Approved
exisulindThe risk or severity of adverse effects can be increased when Tasosartan is combined with exisulind.Investigational
FenbufenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Fenbufen.Approved
FenoprofenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Fenoprofen.Approved
FloctafenineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Floctafenine.Approved, Withdrawn
FluconazoleThe metabolism of Tasosartan can be decreased when combined with Fluconazole.Approved
FlunixinThe risk or severity of adverse effects can be increased when Tasosartan is combined with Flunixin.Vet Approved
FlurbiprofenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Flurbiprofen.Approved, Investigational
FluvoxamineThe metabolism of Tasosartan can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Tasosartan can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Tasosartan can be increased when it is combined with Fosaprepitant.Approved
FosinoprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Fosinopril.Approved
FosphenytoinThe metabolism of Tasosartan can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Tasosartan can be increased when it is combined with Fusidic Acid.Approved
HeparinHeparin may increase the hyperkalemic activities of Tasosartan.Approved, Investigational
HigenamineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Higenamine.Investigational
HMPL-004The risk or severity of adverse effects can be increased when Tasosartan is combined with HMPL-004.Investigational
IbuprofenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Ibuprofen.Approved
IbuproxamThe risk or severity of adverse effects can be increased when Tasosartan is combined with Ibuproxam.Withdrawn
IcatibantThe risk or severity of adverse effects can be increased when Tasosartan is combined with Icatibant.Approved
IdelalisibThe serum concentration of Tasosartan can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Tasosartan can be decreased when combined with Imatinib.Approved
ImidaprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Imidapril.Investigational
IndinavirThe metabolism of Tasosartan can be decreased when combined with Indinavir.Approved
IndomethacinThe risk or severity of adverse effects can be increased when Tasosartan is combined with Indomethacin.Approved, Investigational
IndoprofenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Indoprofen.Withdrawn
IsavuconazoniumThe metabolism of Tasosartan can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoxicamThe risk or severity of adverse effects can be increased when Tasosartan is combined with Isoxicam.Withdrawn
IsradipineThe metabolism of Tasosartan can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Tasosartan can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Tasosartan can be increased when it is combined with Ivacaftor.Approved
KebuzoneThe risk or severity of adverse effects can be increased when Tasosartan is combined with Kebuzone.Experimental
KetoconazoleThe metabolism of Tasosartan can be decreased when combined with Ketoconazole.Approved, Investigational
KetoprofenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Ketoprofen.Approved, Vet Approved
KetorolacThe risk or severity of adverse effects can be increased when Tasosartan is combined with Ketorolac.Approved
LeflunomideThe risk or severity of adverse effects can be increased when Tasosartan is combined with Leflunomide.Approved, Investigational
LisinoprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Lisinopril.Approved, Investigational
LisofyllineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Lisofylline.Investigational
LithiumThe serum concentration of Lithium can be increased when it is combined with Tasosartan.Approved
LopinavirThe metabolism of Tasosartan can be decreased when combined with Lopinavir.Approved
LornoxicamThe risk or severity of adverse effects can be increased when Tasosartan is combined with Lornoxicam.Approved
LovastatinThe metabolism of Tasosartan can be decreased when combined with Lovastatin.Approved, Investigational
LoxoprofenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Loxoprofen.Approved
LuliconazoleThe serum concentration of Tasosartan can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Tasosartan can be increased when combined with Lumacaftor.Approved
LumiracoxibThe risk or severity of adverse effects can be increased when Tasosartan is combined with Lumiracoxib.Approved, Investigational
Magnesium salicylateThe risk or severity of adverse effects can be increased when Tasosartan is combined with Magnesium salicylate.Approved
MasoprocolThe risk or severity of adverse effects can be increased when Tasosartan is combined with Masoprocol.Approved
Meclofenamic acidThe risk or severity of adverse effects can be increased when Tasosartan is combined with Meclofenamic acid.Approved, Vet Approved
Mefenamic acidThe risk or severity of adverse effects can be increased when Tasosartan is combined with Mefenamic acid.Approved
MeloxicamThe risk or severity of adverse effects can be increased when Tasosartan is combined with Meloxicam.Approved, Vet Approved
MesalazineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Mesalazine.Approved
MetamizoleThe risk or severity of adverse effects can be increased when Tasosartan is combined with Metamizole.Withdrawn
MifepristoneThe serum concentration of Tasosartan can be increased when it is combined with Mifepristone.Approved, Investigational
MitotaneThe serum concentration of Tasosartan can be decreased when it is combined with Mitotane.Approved
MizoribineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Mizoribine.Investigational
ModafinilThe serum concentration of Tasosartan can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Moexipril.Approved
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Mycophenolate mofetil.Approved, Investigational
Mycophenolic acidThe risk or severity of adverse effects can be increased when Tasosartan is combined with Mycophenolic acid.Approved
NabumetoneThe risk or severity of adverse effects can be increased when Tasosartan is combined with Nabumetone.Approved
NadroparinNadroparin may increase the hyperkalemic activities of Tasosartan.Approved
NafamostatThe risk or severity of adverse effects can be increased when Tasosartan is combined with Nafamostat.Investigational
NafcillinThe serum concentration of Tasosartan can be decreased when it is combined with Nafcillin.Approved
NaftifineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Naftifine.Approved
NaproxenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Naproxen.Approved, Vet Approved
NCX 4016The risk or severity of adverse effects can be increased when Tasosartan is combined with NCX 4016.Investigational
NefazodoneThe metabolism of Tasosartan can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Tasosartan can be decreased when combined with Nelfinavir.Approved
NepafenacThe risk or severity of adverse effects can be increased when Tasosartan is combined with Nepafenac.Approved
NetupitantThe serum concentration of Tasosartan can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Tasosartan can be increased when combined with Nevirapine.Approved
NicorandilNicorandil may increase the hyperkalemic activities of Tasosartan.Approved
Niflumic AcidThe risk or severity of adverse effects can be increased when Tasosartan is combined with Niflumic Acid.Approved
NilotinibThe metabolism of Tasosartan can be decreased when combined with Nilotinib.Approved, Investigational
NimesulideThe risk or severity of adverse effects can be increased when Tasosartan is combined with Nimesulide.Approved, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Tasosartan is combined with Nitroaspirin.Investigational
OlaparibThe metabolism of Tasosartan can be decreased when combined with Olaparib.Approved
OlopatadineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Olopatadine.Approved
OlsalazineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Olsalazine.Approved
OmapatrilatThe risk or severity of adverse effects can be increased when Tasosartan is combined with Omapatrilat.Investigational
OrgoteinThe risk or severity of adverse effects can be increased when Tasosartan is combined with Orgotein.Vet Approved
OsimertinibThe serum concentration of Tasosartan can be increased when it is combined with Osimertinib.Approved
OxaprozinThe risk or severity of adverse effects can be increased when Tasosartan is combined with Oxaprozin.Approved
OxyphenbutazoneThe risk or severity of adverse effects can be increased when Tasosartan is combined with Oxyphenbutazone.Withdrawn
PalbociclibThe serum concentration of Tasosartan can be increased when it is combined with Palbociclib.Approved
ParecoxibThe risk or severity of adverse effects can be increased when Tasosartan is combined with Parecoxib.Approved
ParnaparinParnaparin may increase the hyperkalemic activities of Tasosartan.Approved
PentobarbitalThe metabolism of Tasosartan can be increased when combined with Pentobarbital.Approved, Vet Approved
PerindoprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Perindopril.Approved
PhenobarbitalThe metabolism of Tasosartan can be increased when combined with Phenobarbital.Approved
PhenylbutazoneThe risk or severity of adverse effects can be increased when Tasosartan is combined with Phenylbutazone.Approved, Vet Approved
PhenytoinThe metabolism of Tasosartan can be increased when combined with Phenytoin.Approved, Vet Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Tasosartan is combined with Pimecrolimus.Approved, Investigational
PirfenidoneThe risk or severity of adverse effects can be increased when Tasosartan is combined with Pirfenidone.Investigational
PiroxicamThe risk or severity of adverse effects can be increased when Tasosartan is combined with Piroxicam.Approved, Investigational
PosaconazoleThe metabolism of Tasosartan can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Tasosartan can be increased when combined with Primidone.Approved, Vet Approved
PropacetamolThe risk or severity of adverse effects can be increased when Tasosartan is combined with Propacetamol.Approved
PTC299The risk or severity of adverse effects can be increased when Tasosartan is combined with PTC299.Investigational
QuinaprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Quinapril.Approved, Investigational
RamiprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Ramipril.Approved
RanolazineThe metabolism of Tasosartan can be decreased when combined with Ranolazine.Approved, Investigational
RescinnamineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Rescinnamine.Approved
ResveratrolThe risk or severity of adverse effects can be increased when Tasosartan is combined with Resveratrol.Experimental, Investigational
ReviparinReviparin may increase the hyperkalemic activities of Tasosartan.Approved
RifabutinThe metabolism of Tasosartan can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Tasosartan can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Tasosartan can be increased when combined with Rifapentine.Approved
RitonavirThe metabolism of Tasosartan can be decreased when combined with Ritonavir.Approved, Investigational
RofecoxibThe risk or severity of adverse effects can be increased when Tasosartan is combined with Rofecoxib.Investigational, Withdrawn
SalicylamideThe risk or severity of adverse effects can be increased when Tasosartan is combined with Salicylamide.Approved
Salicylic acidThe risk or severity of adverse effects can be increased when Tasosartan is combined with Salicylic acid.Approved, Vet Approved
SalsalateThe risk or severity of adverse effects can be increased when Tasosartan is combined with Salsalate.Approved
SaquinavirThe metabolism of Tasosartan can be decreased when combined with Saquinavir.Approved, Investigational
SeratrodastThe risk or severity of adverse effects can be increased when Tasosartan is combined with Seratrodast.Approved, Investigational
SildenafilThe metabolism of Tasosartan can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Tasosartan can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Tasosartan can be increased when it is combined with Simeprevir.Approved
SpiraprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Spirapril.Approved
SpironolactoneTasosartan may increase the hyperkalemic activities of Spironolactone.Approved
SRT501The risk or severity of adverse effects can be increased when Tasosartan is combined with SRT501.Investigational
St. John's WortThe serum concentration of Tasosartan can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Tasosartan can be increased when it is combined with Stiripentol.Approved
SulfasalazineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Sulfasalazine.Approved
SulfisoxazoleThe metabolism of Tasosartan can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulindacThe risk or severity of adverse effects can be increased when Tasosartan is combined with Sulindac.Approved
SuprofenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Suprofen.Approved, Withdrawn
TelaprevirThe metabolism of Tasosartan can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Tasosartan can be decreased when combined with Telithromycin.Approved
TemocaprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Temocapril.Experimental, Investigational
TenoxicamThe risk or severity of adverse effects can be increased when Tasosartan is combined with Tenoxicam.Approved
TepoxalinThe risk or severity of adverse effects can be increased when Tasosartan is combined with Tepoxalin.Vet Approved
TeriflunomideThe risk or severity of adverse effects can be increased when Tasosartan is combined with Teriflunomide.Approved
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Tasosartan is combined with Tiaprofenic acid.Approved
TiclopidineThe metabolism of Tasosartan can be decreased when combined with Ticlopidine.Approved
TinoridineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Tinoridine.Investigational
TinzaparinTinzaparin may increase the hyperkalemic activities of Tasosartan.Approved
TocilizumabThe serum concentration of Tasosartan can be decreased when it is combined with Tocilizumab.Approved
Tolfenamic AcidThe risk or severity of adverse effects can be increased when Tasosartan is combined with Tolfenamic Acid.Approved
TolmetinThe risk or severity of adverse effects can be increased when Tasosartan is combined with Tolmetin.Approved
TolvaptanTolvaptan may increase the hyperkalemic activities of Tasosartan.Approved
TrandolaprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Trandolapril.Approved
TranilastThe risk or severity of adverse effects can be increased when Tasosartan is combined with Tranilast.Approved, Investigational
TriamtereneTasosartan may increase the hyperkalemic activities of Triamterene.Approved
TrimethoprimTrimethoprim may increase the hyperkalemic activities of Tasosartan.Approved, Vet Approved
Trisalicylate-cholineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Trisalicylate-choline.Approved
ValdecoxibThe risk or severity of adverse effects can be increased when Tasosartan is combined with Valdecoxib.Investigational, Withdrawn
VenlafaxineThe metabolism of Tasosartan can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Tasosartan can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Tasosartan can be decreased when combined with Voriconazole.Approved, Investigational
ZaltoprofenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Zaltoprofen.Approved
ZileutonThe risk or severity of adverse effects can be increased when Tasosartan is combined with Zileuton.Approved, Investigational, Withdrawn
ZiprasidoneThe metabolism of Tasosartan can be decreased when combined with Ziprasidone.Approved
ZomepiracThe risk or severity of adverse effects can be increased when Tasosartan is combined with Zomepirac.Withdrawn
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesC09CA05
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9849
Caco-2 permeable+0.5626
P-glycoprotein substrateSubstrate0.5771
P-glycoprotein inhibitor IInhibitor0.7645
P-glycoprotein inhibitor IIInhibitor0.5378
Renal organic cation transporterInhibitor0.524
CYP450 2C9 substrateNon-substrate0.7978
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7408
CYP450 1A2 substrateNon-inhibitor0.864
CYP450 2C9 inhibitorInhibitor0.6924
CYP450 2D6 inhibitorInhibitor0.5465
CYP450 2C19 inhibitorInhibitor0.8163
CYP450 3A4 inhibitorInhibitor0.5112
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8338
Ames testNon AMES toxic0.5066
CarcinogenicityNon-carcinogens0.8061
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8079 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6971
hERG inhibition (predictor II)Non-inhibitor0.5487
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0325 mg/mLALOGPS
logP3.07ALOGPS
logP4.18ChemAxon
logS-4.1ALOGPS
pKa (Strongest Acidic)7.4ChemAxon
pKa (Strongest Basic)2.79ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area100.55 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity130.61 m3·mol-1ChemAxon
Polarizability44.34 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as biphenyltetrazoles and derivatives. These are organic compounds containing a biphenyl attached to a tetrazole. A carbon atom of the biphenyl moiety is boned to a carbon or the nitrogen atom of the tetrazole moiety.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassAzoles
Sub ClassTetrazoles
Direct ParentBiphenyltetrazoles and derivatives
Alternative Parents
Substituents
  • Biphenyltetrazole
  • Biphenyl
  • Pyridopyrimidine
  • Phenylmethylamine
  • Benzylamine
  • Imidolactam
  • Benzenoid
  • Pyrimidine
  • Pyridine
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Tertiary carboxylic acid amide
  • Tertiary amine
  • Lactam
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
Receptor for angiotensin II. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
Gene Name:
AGTR1
Uniprot ID:
P30556
Molecular Weight:
41060.53 Da
References
  1. Elokdah HM, Friedrichs GS, Chai SY, Harrison BL, Primeau J, Chlenov M, Crandall DL: Novel human metabolites of the angiotensin-II antagonist tasosartan and their pharmacological effects. Bioorg Med Chem Lett. 2002 Aug 5;12(15):1967-71. [PubMed:12113820 ]
  2. Unger T: Pharmacology of AT1-receptor blockers. Blood Press Suppl. 2001;(3):5-10. [PubMed:11683476 ]
  3. Maillard MP, Rossat J, Brunner HR, Burnier M: Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding. J Pharmacol Exp Ther. 2000 Nov;295(2):649-54. [PubMed:11046101 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Receptor antagonist activity
Specific Function:
Receptor for angiotensin II. Cooperates with MTUS1 to inhibit ERK2 activation and cell proliferation.
Gene Name:
AGTR2
Uniprot ID:
P50052
Molecular Weight:
41183.45 Da
References
  1. Unger T: Pharmacology of AT1-receptor blockers. Blood Press Suppl. 2001;(3):5-10. [PubMed:11683476 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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Drug created on June 30, 2007 12:15 / Updated on August 17, 2016 12:23