azilsartan

Trade name: edarbi

Small moleculeapproved

Approved

Feb 25, 2011

Azilsartan medoxomil (trade name Edarb) is an angiotensin II receptor blocker (ARB) that lowers blood pressure by blocking the action of angiotensin II, a vasopressor hormone. It is indicated for the treatment of hypertension to lower blood pressure which reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. Azilsartan medoxomil may be used either alone or in combination with other antihypertensive agents such as chlorthalidone (CLD). As an ARB, azilsartan medoxomil selectively inhibits angiotensin II from binding to the angiotensin II type-1 receptor (AT1). This receptor inhibition provides the antihypertensive activity of azilsartan medoxomil because it blocks the pressor effects of angiotensin II. Azilsartan medoxomil is a prodrug of azilsartan. It is hydrolyzed to the active moiety, azilsartan, in the gastrointestinal (GI) tract during the absorption phase. Azilsartan medoxomil, in combination with the thiazide-like diuretic chlorthalidone, was more effective in lowering systolic BP than azilsartan plus HCTZ. — NCATS

Clinical trial activity

51 trials · 15 clinical orgs · 6 marketing orgs

Phase 1
11
Phase 2
32
Phase 3
30
Phase 4
4

Earliest trial started Jul 1, 2004 (NCT00762736)

Timeline

2000s

  1. Jan 1, 2004

    Takeda — Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2006

    Takeda — Earliest Phase 3 Sponsor(trial)

2010s

  1. Jan 1, 2010

    Takeda — Earliest Phase 1 Sponsor(trial)

  2. Feb 25, 2011

    Earliest FDA Approval

  3. Feb 25, 2011

    Azurity — NDA Secondary Org

  4. Feb 25, 2011

    Arbor Pharmaceuticals — NDA Secondary Org

2020s

  1. Jul 20, 2022

    Lupin — Marketing Organization

  2. Jan 21, 2025

    Alkem Labs Ltd — Marketing Organization

  3. Mar 19, 2025

    Hetero Labs Ltd — Marketing Organization

Indications

Approved for

Mechanism of action

Combination products

Approval history

  • approvedFeb 25, 2011

Chemistry & pharmacology

Loading structure…

SMILES

CCOc1nc2cccc(C(=O)OCc3oc(=O)oc3C)c2n1Cc1ccc(-c2ccccc2-c2noc(=O)[nH]2)cc1
Mol. weight
568.54 g/mol
Lipinski Ro5
2 violation(s)
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Black box warningProdrug

Sources

Also known as

  • 2-ethoxy-1-((2'-(5-oxo-2,5-dihydro-1,2,4-oxadiazol-3-yl)-biphenyl-4-yl)methyl)-1h-benzimidazole-7-carboxylic acid
  • azilsartan
  • azilsartan
  • azilsartan
  • azilsartan
  • azilsartan
  • azilsartan
  • azilsartan
  • azilsartan kamedoxomil
  • azilsartan kamedoxomil
  • azilsartan kamedoxomil
  • azilsartan kamedoxomil
  • azilsartan kamedoxomil
  • azilsartan medoximil
  • azilsartan medoxomil
  • azilsartan medoxomil
  • azilsartan medoxomil
  • azilsartan medoxomil
  • azilsartan medoxomil
  • azilsartan medoxomil
  • azilsartan medoxomil
  • azilsartan medoxomil
  • azilsartan medoxomil
  • azilsartan medoxomil
  • azilsartan médoxomil
  • azilsartan médoxomil
  • azilsartán medoxomilo
  • azilsartán medoxomilo
  • azilsartanum medoxomilum
  • azilsartanum medoxomilum
  • edarbi
  • edarbi
  • edarbi
  • edarbi
  • tak491
  • tak 491
  • tak 491
  • tak 491
  • tak 491
  • tak 491
  • tak 491
  • tak-491
  • tak-491
  • tak-491
  • tak-491
  • tak-536
  • tak-536
  • tak-536
  • tak-536
  • tak-536ccb

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06990204Phase 1Jun 6, 2025Gedeon Richter Ltd.
NCT05002244Phase 1Jul 23, 2021Celltrion
NCT04668157Phase 3Feb 8, 2021Takeda
NCT03434977Phase 1Feb 10, 2018Takeda
NCT03652792Phase 1Jan 22, 2018Lee's Pharmaceutical, Zhaoke (Guangzhou) Pharmaceutical Limited
NCT03042299Phase 1Feb 3, 2017Takeda
NCT02791438Phase 3Aug 31, 2016Takeda
NCT02786082Phase 1Jun 1, 2016Lee's Pharmaceutical
NCT02541669Phase 1Nov 20, 2015Takeda
NCT02480764Phase 3Sep 21, 2015Takeda
NCT02517866Phase 4Aug 1, 2015Takeda
NCT02451150Phase 3Aug 1, 2015Takeda
NCT02609490Phase 3Jul 1, 2015Lee's Pharmaceutical
NCT02400775Phase 4Mar 1, 2015Takeda
NCT02401464Phase 1Mar 1, 2015Takeda
NCT02348658Phase 1Jan 1, 2015Takeda
NCT02407210Phase 3Jan 1, 2015Hengrui Therapeutics, Inc.
NCT02235909Phase 3Dec 1, 2014Arbor Pharmaceuticals
NCT02277691Phase 3Nov 1, 2014Takeda
NCT02203916Phase 3Jul 1, 2014Takeda
Showing 20 of 51 trials
Page 1 / 3

Organizations

Research & Development (15)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
TakedaFor profit413952004
Lee's PharmaceuticalFor profit3322015
Arbor PharmaceuticalsFor profit1112014
CelltrionFor profit1112021
EPS CorporationFor profit1112012
Gedeon Richter Ltd.For profit1112025
Hengrui Therapeutics, Inc.For profit1112015
Hospital General de México Dr. Eduardo LiceagaAcademic/Hospital1112014
Jiangsu Hansoh Pharmaceutical Co., Ltd.For profit1112013
Jichi Medical UniversityAcademic/Hospital1012012
Nara Medical UniversityAcademic/Hospital1112012
Osaka UniversityAcademic/Hospital1012007
TEDA International Cardiovascular HospitalAcademic/Hospital1012013
University of ChicagoAcademic/Hospital1112013
Zhaoke (Guangzhou) Pharmaceutical LimitedGovernment1012018
15 organizations
Page 1 / 1

Marketing (7)

OrganizationOrg typeRelationshipDate
Alkem Labs LtdFor profitMKTGJan 21, 2025
Arbor PharmaceuticalsFor profitNDA2Feb 25, 2011
AzurityFor profitNDA2Feb 25, 2011
Hetero Labs LtdFor profitMKTGMar 19, 2025
LupinFor profitMKTGJul 20, 2022
LupinFor profitSYNJul 20, 2022
TakedaFor profitNDA