drug

LOSARTAN POTASSIUM

Marketedupdated 2mo ago

by $SCNX Scienture Holdings, Inc.

Approved

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Small molecule drug with a maximum clinical stage of Approval (across all indications), with 7 approved and 6 investigational indications.

indications

investigational

Hypertension

all catalysts(29)

approval · 29

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brand

LOSARTAN POTASSIUM

generic

LOSARTAN POTASSIUM

MOA

12.1 Mechanism of Action Angiotensin II [formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE, kininase II)] is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system, and an important component in the pathophysiology of hypertension. It also stimulates aldosterone secretion by the adrenal cortex. Losartan and its principal active metabolite block the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT 1 receptor found in many tissues, (e.g., vascular smooth muscle, adrenal gland). There is also an AT 2 receptor found in many tissues, but it is not known to be associated with cardiovascular homeostasis. Neither losartan nor its principal active metabolite exhibits any partial agonist activity at the AT 1 receptor, and both have much greater affinity (about 1,000-fold) for the AT 1 receptor than for the AT 2 receptor. In vitro binding studies indicate that losartan is a reversible, competitive inhibitor of the AT 1 receptor. The active metabolite is 10 to 40 times more potent by weight than losartan and appears to be a reversible, noncompetitive inhibitor of the AT 1 receptor. Neither losartan nor its active metabolite inhibits ACE (kininase II, the enzyme that converts angiotensin I to angiotensin II and degrades bradykinin), nor do they bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.

indication

Hypertension

phase

marketed

LOSARTAN POTASSIUM

indications

all catalysts(29)

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Trials studying LOSARTAN POTASSIUM