2D 3D
	ID	DDInter1915
	Drug Type	small molecule
	Molecular Formula	C24H29N5O3
	Molecular Weight	435.519
	CAS Number	137862-53-4
	Description	Valsartan belongs to the angiotensin II receptor blocker (ARB) family of drugs, which also includes [telmisartan], [candesartan], [losartan], [olmesartan], and [irbesartan]. ARBs selectively bind to angiotensin receptor 1 (AT1) and prevent the protein angiotensin II from binding and exerting its hypertensive effects, which include vasoconstriction, stimulation and synthesis of aldosterone and ADH, cardiac stimulation, and renal reabsorption of sodium, among others. Overall, valsartan's physiologic effects lead to reduced blood pressure, lower aldosterone levels, reduced cardiac activity, and increased excretion of sodium. Valsartan also affects the renin-angiotensin aldosterone system (RAAS), which plays an important role in hemostasis and regulation of kidney, vascular, and cardiac functions. Pharmacological blockade of RAAS via AT1 receptor blockade inhibits negative regulatory feedback within RAAS, which is a contributing factor to the pathogenesis and progression of cardiovascular disease, heart failure, and renal disease. In particular, heart failure is associated with chronic activation of RAAS, leading to inappropriate fluid retention, vasoconstriction, and ultimately a further decline in left ventricular function. ARBs have been shown to have a protective effect on the heart by improving cardiac function, reducing afterload, increasing cardiac output and preventing ventricular hypertrophy and remodelling.[A174154] By comparison, the angiotensin-converting enzyme inhibitor (ACEI) class of medications (which includes drugs such as [ramipril], [lisinopril], and [perindopril]) inhibit the conversion of angiotensin I to angiotensin II through inhibition of the ACE enzyme. However, this does not prevent the formation of all angiotensin II within the body. The angiotensin II receptor blocker (ARB) family of drugs unique in that it blocks all angiotensin II activity, regardless of where or how it was synthesized. Valsartan is commonly used for the management of hypertension, heart failure, and Type 2 Diabetes-associated nephropathy, particularly in patients who are unable to tolerate ACE inhibitors. ARBs such as valsartan have been shown in a number of large-scale clinical outcomes trials to improve cardiovascular outcomes including reducing risk of myocardial infarction, stroke, the progression of heart failure, and hospitalization.[A174124,A178153,A173869,A185324,A185327,A185333,A185342,A185345] Valsartan also slows the progression of diabetic nephropathy due to its renoprotective effects.[A174157,A174160,A174163] Improvements in chronic kidney disease with valsartan include both clinically and statistically significant decreases in urinary albumin and protein excretion in patients diagnosed with type 2 diabetes and in nondiabetic patients diagnosed with chronic kidney disease.[A174124,A173869] Valsartan was initially approved in 1996 in Europe for the treatment of hypertension in adults. Shortly after, in 1997, this drug was approved in the United States.[A174124] Valsartan is generally well-tolerated with a side-effect profile superior to that of other antihypertensive drugs.[A174130,A174133]
	ATC Classification	C09DX05 C10BX10 C09DA03 C09CA03 C09DX02 C09DX01 C09DB08 C09DB01 C09DX04
IUPAC Name	(2S)-3-methyl-2-(N-{[2'-(2H-1,2,3,4-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl]methyl}pentanamido)butanoic acid
InChI	ACWBQPMHZXGDFX-QFIPXVFZSA-N
Canonical SMILES	CCCCC(=O)N(CC1=CC=C(C=C1)C1=CC=CC=C1C1=NNN=N1)[C@@H](C(C)C)C(O)=O
Useful Links	DrugBank ChEBI PubChem Substance KEGG Drug ChemSpider BindingDB PharmGKB Therapeutic Targets Database Guide to Pharmacology Wikipedia ChEMBL ZINC