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Olmesartan

Generic Name
Olmesartan
Brand Names
Azor, Benicar, Benicar Hct, Olmetec, Olmetec Plus, Tribenzor
Drug Type
Small Molecule
Chemical Formula
C24H26N6O3
CAS Number
144689-24-7
Unique Ingredient Identifier
8W1IQP3U10

Overview

Olmesartan belongs to the angiotensin II receptor blocker (ARB) family of drugs, which also includes telmisartan, candesartan, losartan, valsartan, 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, olmesartan's physiologic effects lead to reduced blood pressure, lower aldosterone levels, reduced cardiac activity, and increased excretion of sodium. Olmesartan 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. 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. Olmesartan is commonly used for the management of hypertension and Type 2 Diabetes-associated nephropathy, particularly in patients who are unable to tolerate ACE inhibitors. ARBs such as olmesartan 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. Like other ARBs, olmesartan blockade of RAAS slows the progression of diabetic nephropathy due to its renoprotective effects. Orally available olmesartan is produced as the prodrug olmesartan medoxomil which is rapidly converted in vivo to the pharmacologically active olmesartan. It was developed by Daiichi Sankyo Pharmaceuticals and approved in 2002.

Background

Olmesartan belongs to the angiotensin II receptor blocker (ARB) family of drugs, which also includes telmisartan, candesartan, losartan, valsartan, 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, olmesartan's physiologic effects lead to reduced blood pressure, lower aldosterone levels, reduced cardiac activity, and increased excretion of sodium. Olmesartan 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. 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. Olmesartan is commonly used for the management of hypertension and Type 2 Diabetes-associated nephropathy, particularly in patients who are unable to tolerate ACE inhibitors. ARBs such as olmesartan 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. Like other ARBs, olmesartan blockade of RAAS slows the progression of diabetic nephropathy due to its renoprotective effects. Orally available olmesartan is produced as the prodrug olmesartan medoxomil which is rapidly converted in vivo to the pharmacologically active olmesartan. It was developed by Daiichi Sankyo Pharmaceuticals and approved in 2002.

Indication

Olmesartan is indicated for the treatment of hypertension either alone or in combination with other antihypertensive agents. Olmesartan is also used off-label for the management Type 2 Diabetes-associated nephropathy, heart failure, and post-myocardial infarction, particularly in patients who are unable to tolerate ACE inhibitors. ARBs such as olmesartan 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. Like other ARBs, olmesartan blockade of RAAS slows the progression of diabetic nephropathy due to its renoprotective effects.

Associated Conditions

  • Diabetic Nephropathy
  • Hypertension

Clinical Trials

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Title
Posted
Study ID
Phase
Status
Sponsor
2013/02/07
Phase 3
Completed
2013/01/09
Phase 3
Completed
Daewoong Pharmaceutical Co. LTD.
2012/09/25
Phase 2
Completed
2012/09/13
Phase 4
Completed
2012/06/08
Phase 3
Completed
2012/06/04
Phase 4
Completed
Institut für Pharmakologie und Präventive Medizin
2012/05/15
Phase 3
Completed
2011/12/16
Phase 1
Completed
Daewoong Pharmaceutical Co. LTD.
2011/08/12
Phase 1
Completed
Daewoong Pharmaceutical Co. LTD.
2011/03/07
Phase 3
Completed

FDA Drug Approvals

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Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
Slate Run Pharmaceuticals, LLC
70436-016
ORAL
40 mg in 1 1
5/14/2025
Novadoz Pharmaceuticals LLC
72205-167
ORAL
40 mg in 1 1
11/30/2023
Camber Pharmaceuticals, Inc.
31722-854
ORAL
40 mg in 1 1
5/23/2025
Slate Run Pharmaceuticals, LLC
70436-017
ORAL
40 mg in 1 1
5/14/2025
Bryant Ranch Prepack
63629-8525
ORAL
40 mg in 1 1
1/8/2021
REMEDYREPACK INC.
70518-1648
ORAL
40 mg in 1 1
2/22/2024
Cosette Pharmaceuticals, Inc.
0713-0875
ORAL
40 mg in 1 1
7/12/2023
Camber Pharmaceuticals, Inc.
31722-853
ORAL
20 mg in 1 1
5/23/2025
Micro Labs Limited
42571-238
ORAL
40 mg in 1 1
11/23/2021
Lifestar Pharma LLC
70756-809
ORAL
20 mg in 1 1
12/19/2023

EMA Drug Approvals

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Authorization Holder
Status
Issued Date
No EMA approvals found for this drug.

HSA Drug Approvals

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Approval Number
Dosage Form
Strength
Approval Date
No HSA approvals found for this drug.

NMPA Drug Approvals

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Approval Number
Drug Type
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Approval Date
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PPB Drug Approvals

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Company
Licence No.
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Registration Date
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TGA Drug Approvals

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Approved Product
ARTG ID
Sponsor
Registration Type
Status
Registration Date
TERRY WHITE CHEMISTS OLMESARTAN HCTZ 40/12.5 olmesartan medoxomil 40 mg & hydrochlorothiazide 12.5 mg tablet blister pack
206478
Medicine
A
11/7/2013
OLMERTAN olmesartan medoxomil 20 mg tablet blister pack
235830
Medicine
A
2/25/2016
OLMESARTAN/AMLODIPINE SPR 20/5 olmesartan medoxomil 20 mg and amlodipine (as besilate) 5 mg tablet blister pack
218240
Medicine
A
1/12/2016
OLMESARTAN ASTRON olmesartan medoxomil 10 mg tablet blister pack
358606
Medicine
A
5/19/2022
OLMESARTAN ASTRON olmesartan medoxomil 20 mg tablet blister pack
358603
Medicine
A
5/19/2022
APO-OLMESARTAN/AMLODIPINE/HCTZ 40/5/25 olmesartan medoxomil/amlodipine/hydrochlorothiazide 40/5/25 mg film-coated tablet blister pack
312007
Medicine
A
11/21/2019
OLMAKAR HCT 40/5/12.5 olmesartan medoxomil/amlodipine/hydrochlorothiazide 40/5/12.5 mg film-coated tablet blister pack
312000
Medicine
A
11/21/2019
OLMESART olmesartan medoxomil 20 mg tablet blister pack
287885
Medicine
A
2/2/2018
APO-OLMESARTAN/AMLODIPINE 20/5 olmesartan medoxomil 20 mg / amlodipine (as besilate) 5 mg tablet blister pack
290089
Medicine
A
6/13/2018
Olmesartan HCT GPPL 40/12.5 Olmesartan medoxomil & hydrochlorothiazide 40/12.5 mg tablets blister pack
287861
Medicine
A
2/2/2018
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