DT-Web

DB01342 - Forasartan


Identification
Name Forasartan
Accession Number DB01342
Type small molecule
Description Forasartan, a specific angiotensin II antagonist, is used alone or with other antihypertensive agents to treat hypertension. Forasartan competes with angiotensin II for binding at the AT1 receptor subtype. As angiotensin II is a vasoconstrictor which also stimulates the synthesis and release of aldosterone, blockage of its effects results in a decreases in systemic vascular resistance.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 416.522
Groups approved
Monoisotopic Weight 416.243692936
Pharmacology
Indication For the treatment of hypertension.
Mechanism of action Forasartan competes with angiotensin II for binding at the AT1 receptor subtype. As angiotensin II is a vasoconstrictor which also stimulates the synthesis and release of aldosterone, blockage of its effects results in a decreases in systemic vascular resistance. Also, since angiotensin causes vasoconstriction, the inhibition of this receptor decreases vasoconstriction, which consequently also decreases vascular resistnace.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Amiloride Increased risk of hyperkalemia
Lithium The ARB increases serum levels of lithium
Potassium Increased risk of hyperkalemia
Triamterene Increased risk of hyperkalemia
Food Interactions Not Available

Targets


Type-1 angiotensin II receptor
Name Type-1 angiotensin II receptor
Gene Name AGTR1
Pharmacological action yes
Actions antagonist
References
  • Tokunaga R, Kushiku K, Yamada K, Yamada H, Furukawa T: Possible involvement of calcium-calmodulin pathways in the positive chronotropic response to angiotensin II on the canine cardiac sympathetic ganglia. Jpn J Pharmacol. 2001 Aug;86(4):381-9. - Pubmed
  • Usune S, Furukawa T: Effects of SC-52458, a new nonpeptide angiotensin II receptor antagonist, on increase in cytoplasmic Ca2+ concentrations and contraction induced by angiotensin II and K(+)-depolarization in guinea-pig taenia coli. Gen Pharmacol. 1996 Oct;27(7):1179-85. - Pubmed
  • Hagmann M, Nussberger J, Naudin RB, Burns TS, Karim A, Waeber B, Brunner HR: SC-52458, an orally active angiotensin II-receptor antagonist: inhibition of blood pressure response to angiotensin II challenges and pharmacokinetics in normal volunteers. J Cardiovasc Pharmacol. 1997 Apr;29(4):444-50. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 0.6666

Predictions


Id Partner name Gene Name Score
5852 Type-2 angiotensin II receptor AGTR2 0.0627
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0503
4757 Cytochrome P450 2C9 CYP2C9 0.0459
6157 Solute carrier organic anion transporter family member 1B3 SLCO1B3 0.037
1490 Solute carrier organic anion transporter family member 1B1 SLCO1B1 0.0321
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0313
4512 Cytochrome P450 3A4 CYP3A4 0.0233
1588 Multidrug resistance protein 1 ABCB1 0.0206
4924 Cytochrome P450 2C8 CYP2C8 0.0195
20 Prostaglandin G/H synthase 1 PTGS1 0.0182
587 Serum albumin ALB 0.0162
1629 Transcription factor AP-1 JUN 0.0146
6179 UDP-glucuronosyltransferase 2B17 UGT2B17 0.0133
238 Peroxisome proliferator-activated receptor gamma PPARG 0.0132
6016 Cytochrome P450 2C19 CYP2C19 0.0128
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.011
4200 Cytochrome P450 1A2 CYP1A2 0.0096
6177 UDP-glucuronosyltransferase 1-10 UGT1A10 0.0077
4119 Cytochrome P450 2D6 CYP2D6 0.0057
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.0055
6022 UDP-glucuronosyltransferase 1-1 UGT1A1 0.0053
1729 Solute carrier family 22 member 6 SLC22A6 0.0041
4118 Cytochrome P450 3A5 CYP3A5 0.0038
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