DT-Web

DB01347 - Saprisartan


Identification
Name Saprisartan
Accession Number DB01347
Type small molecule
Description Saprisartan is an AT1 receptor antagonist. It is based on medications of losartan's prototypical chemical structure. The mode of (functional) AT1 receptor antagonism has been characterized as insurmountable/noncompetitive for saprisartan. It is very likely that slow dissociation kinetics from the AT1 receptor underlie insurmountable antagonism.(10579749)
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 611.431
Groups approved
Monoisotopic Weight 610.049723164
Pharmacology
Indication Saprisartan is used in the treatment of hypertension and heart failure.
Mechanism of action Saprisartan is a selective, potent, orally active and long-acting nonpeptide Angiotensin II type 1 (AT1) receptor antagonist. Saprisartan 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. Saprisartan 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.
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
  • Timmermans PB: Pharmacological properties of angiotensin II receptor antagonists. Can J Cardiol. 1999 Nov;15 Suppl F:26F-8F. - 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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