Small molecule
PubChem CID 3961
Losartan
Cozaar
- Mechanism of action
- Angiotensin II receptor (AT1) blocker
- In plain language
- Blocks a hormone signal that tightens blood vessels, so vessels relax and blood pressure comes down.
- How it works
- Losartan and its pharmacologically active carboxylic acid metabolite selectively and competitively antagonize the AT1 receptor subtype, blocking angiotensin II-mediated vasoconstriction and aldosterone secretion without agonist activity. Neither losartan nor its metabolite inhibits ACE, so bradykinin degradation is unaffected, distinguishing its profile from ACE inhibitors. The active metabolite is 10-40 times more potent than the parent compound and binds with roughly 1000-fold greater affinity for AT1 over AT2 receptors. The net effect is reduced peripheral vascular resistance and lowered blood pressure, along with reduced intraglomerular pressure that slows progression of diabetic nephropathy.
- Therapeutic applications
- Indicated for the treatment of hypertension in adults and pediatric patients 6 years of age and older; for reduction of the risk of stroke in patients with hypertension and left ventricular hypertrophy; and for treatment of diabetic nephropathy with elevated serum creatinine and proteinuria in patients with type 2 diabetes and a history of hypertension, to slow progression.
- Class
- Small molecule
- Therapeutic area
- Cardiovascular
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