Identification

Name
Tasosartan
Accession Number
DB01349
Type
Small Molecule
Groups
Approved
Description

Tasosartan 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
  • Tasosartan
  • WAY-ana-756
External IDs
ANA-756
Categories
UNII
48G92V856H
CAS number
145733-36-4
Weight
Average: 411.4591
Monoisotopic: 411.180758329
Chemical Formula
C23H21N7O
InChI Key
ADXGNEYLLLSOAR-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

Indication

Tasosartan is infrequently in the treatment of hypertension and heart failure.

Structured Indications
Not Available
Pharmacodynamics

By 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 action

Tasosartan 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.

TargetActionsOrganism
AType-1 angiotensin II receptor
antagonist
Human
UType-2 angiotensin II receptor
antagonist
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AceclofenacThe risk or severity of adverse effects can be increased when Tasosartan is combined with Aceclofenac.Approved, Investigational
AcemetacinThe risk or severity of adverse effects can be increased when Tasosartan is combined with Acemetacin.Approved
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
AlclofenacThe risk or severity of adverse effects can be increased when Tasosartan is combined with Alclofenac.Approved, Withdrawn
AliskirenAliskiren may increase the hyperkalemic activities of Tasosartan.Approved, Investigational
AlminoprofenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Alminoprofen.Experimental
AmilorideTasosartan may increase the hyperkalemic activities of Amiloride.Approved
AmiodaroneThe metabolism of Tasosartan can be decreased when combined with Amiodarone.Approved, Investigational
AndrographolideThe risk or severity of adverse effects can be increased when Tasosartan is combined with Andrographolide.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
ApocyninThe risk or severity of adverse effects can be increased when Tasosartan is combined with Apocynin.Investigational
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, Investigational, 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, Investigational
BenazeprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Benazepril.Approved, Investigational
BendazacThe risk or severity of adverse effects can be increased when Tasosartan is combined with Bendazac.Experimental
BenorilateThe risk or severity of adverse effects can be increased when Tasosartan is combined with Benorilate.Experimental
BenoxaprofenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Benoxaprofen.Withdrawn
BevoniumThe risk or severity of adverse effects can be increased when Tasosartan is combined with Bevonium.Experimental
BoceprevirThe metabolism of Tasosartan can be decreased when combined with Boceprevir.Approved, Withdrawn
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
BufexamacThe risk or severity of adverse effects can be increased when Tasosartan is combined with Bufexamac.Experimental
BumadizoneThe risk or severity of adverse effects can be increased when Tasosartan is combined with Bumadizone.Experimental
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
Carbaspirin calciumThe risk or severity of adverse effects can be increased when Tasosartan is combined with Carbaspirin calcium.Experimental, 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, Investigational
ChloroquineThe risk or severity of adverse effects can be increased when Tasosartan is combined with Chloroquine.Approved, Vet Approved
Choline magnesium trisalicylateThe risk or severity of adverse effects can be increased when Tasosartan is combined with Choline magnesium trisalicylate.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
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
DelaprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Delapril.Experimental
DelavirdineThe metabolism of Tasosartan can be decreased when combined with Delavirdine.Approved
DiclofenacThe risk or severity of adverse effects can be increased when Tasosartan is combined with Diclofenac.Approved, Vet Approved
DifenpiramideThe risk or severity of adverse effects can be increased when Tasosartan is combined with Difenpiramide.Experimental
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
E-6201The risk or severity of adverse effects can be increased when Tasosartan is combined with E-6201.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
EtanerceptThe risk or severity of adverse effects can be increased when Tasosartan is combined with Etanercept.Approved, Investigational
EthenzamideThe risk or severity of adverse effects can be increased when Tasosartan is combined with Ethenzamide.Experimental
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, Investigational
EtoricoxibThe risk or severity of adverse effects can be increased when Tasosartan is combined with Etoricoxib.Approved, Investigational
Evening primrose oilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Evening primrose oil.Approved, Investigational
exisulindThe risk or severity of adverse effects can be increased when Tasosartan is combined with exisulind.Investigational
FelbinacThe risk or severity of adverse effects can be increased when Tasosartan is combined with Felbinac.Experimental
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
FentiazacThe risk or severity of adverse effects can be increased when Tasosartan is combined with Fentiazac.Experimental
FeprazoneThe risk or severity of adverse effects can be increased when Tasosartan is combined with Feprazone.Experimental
Ferulic acidThe risk or severity of adverse effects can be increased when Tasosartan is combined with Ferulic acid.Experimental
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
FlunoxaprofenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Flunoxaprofen.Experimental
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
GuacetisalThe risk or severity of adverse effects can be increased when Tasosartan is combined with Guacetisal.Experimental
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
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
Imidazole salicylateThe risk or severity of adverse effects can be increased when Tasosartan is combined with Imidazole salicylate.Experimental
IndinavirThe metabolism of Tasosartan can be decreased when combined with Indinavir.Approved
IndobufenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Indobufen.Investigational
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
LonazolacThe risk or severity of adverse effects can be increased when Tasosartan is combined with Lonazolac.Experimental
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, Investigational
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, Investigational
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, Investigational
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.Investigational, 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
MoexiprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Moexipril.Approved
MofebutazoneThe risk or severity of adverse effects can be increased when Tasosartan is combined with Mofebutazone.Experimental
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.Approved, Investigational
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
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, Investigational
NifenazoneThe risk or severity of adverse effects can be increased when Tasosartan is combined with Nifenazone.Experimental
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, Investigational, 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.Approved, 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, Investigational
ParthenolideThe risk or severity of adverse effects can be increased when Tasosartan is combined with Parthenolide.Investigational
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.Approved, Investigational
PiroxicamThe risk or severity of adverse effects can be increased when Tasosartan is combined with Piroxicam.Approved, Investigational
PirprofenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Pirprofen.Experimental
PosaconazoleThe metabolism of Tasosartan can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PranoprofenThe risk or severity of adverse effects can be increased when Tasosartan is combined with Pranoprofen.Experimental, Investigational
PrimidoneThe metabolism of Tasosartan can be increased when combined with Primidone.Approved, Vet Approved
ProglumetacinThe risk or severity of adverse effects can be increased when Tasosartan is combined with Proglumetacin.Experimental
PropacetamolThe risk or severity of adverse effects can be increased when Tasosartan is combined with Propacetamol.Approved, Investigational
PropyphenazoneThe risk or severity of adverse effects can be increased when Tasosartan is combined with Propyphenazone.Experimental
ProquazoneThe risk or severity of adverse effects can be increased when Tasosartan is combined with Proquazone.Experimental
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.Approved, Experimental, Investigational
ReviparinReviparin may increase the hyperkalemic activities of Tasosartan.Approved, Investigational
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
SemapimodThe risk or severity of adverse effects can be increased when Tasosartan is combined with Semapimod.Investigational
SeratrodastThe risk or severity of adverse effects can be increased when Tasosartan is combined with Seratrodast.Approved
SerrapeptaseThe risk or severity of adverse effects can be increased when Tasosartan is combined with Serrapeptase.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
Sodium phosphateTasosartan may increase the nephrotoxic activities of Sodium phosphate.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.Investigational, 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
SuxibuzoneThe risk or severity of adverse effects can be increased when Tasosartan is combined with Suxibuzone.Experimental
TarenflurbilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Tarenflurbil.Investigational
TelaprevirThe metabolism of Tasosartan can be decreased when combined with Telaprevir.Approved, Withdrawn
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
TenidapThe risk or severity of adverse effects can be increased when Tasosartan is combined with Tenidap.Experimental
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
TribenosideThe risk or severity of adverse effects can be increased when Tasosartan is combined with Tribenoside.Experimental
TrimethoprimTrimethoprim may increase the hyperkalemic activities of Tasosartan.Approved, Vet Approved
TriptolideThe risk or severity of adverse effects can be increased when Tasosartan is combined with Triptolide.Investigational
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, Investigational
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
ZofenoprilThe risk or severity of adverse effects can be increased when Tasosartan is combined with Zofenopril.Experimental
ZomepiracThe risk or severity of adverse effects can be increased when Tasosartan is combined with Zomepirac.Withdrawn
Food Interactions
Not Available

References

General References
Not Available
External Links
Human Metabolome Database
HMDB15439
PubChem Compound
60919
PubChem Substance
46504809
ChemSpider
54890
BindingDB
50040439
ChEBI
135666
ChEMBL
CHEMBL432162
Therapeutic Targets Database
DAP001258
PharmGKB
PA164769057
Wikipedia
Tasosartan
ATC Codes
C09CA05 — Tasosartan

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not 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 FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as biphenyls and derivatives. These are organic compounds containing to benzene rings linked together by a C-C bond.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Biphenyls and derivatives
Direct Parent
Biphenyls and derivatives
Alternative Parents
Phenyltetrazoles and derivatives / Pyridopyrimidines / Pyrimidines and pyrimidine derivatives / Pyridines and derivatives / Imidolactams / Tertiary carboxylic acid amides / Heteroaromatic compounds / Lactams / Azacyclic compounds / Organopnictogen compounds
show 4 more
Substituents
Biphenyl / Phenyltetrazole / Pyridopyrimidine / Pyridine / Pyrimidine / Imidolactam / Azole / Tertiary carboxylic acid amide / Tetrazole / Heteroaromatic compound
show 14 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not 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
Uniprot Name
Type-1 angiotensin II receptor
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
Uniprot Name
Type-2 angiotensin II receptor
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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]

Drug created on June 30, 2007 12:15 / Updated on November 09, 2017 02:59