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esmolol

Trade name: brevibloc

Small moleculeapproved

Approved

Dec 31, 1986

Esmolol (trade name Brevibloc) is a cardioselective beta1 receptor blocker with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilizing activity at therapeutic dosages. Esmolol decreases the force and rate of heart contractions by blocking beta-adrenergic receptors of the sympathetic nervous system, which are found in the heart and other organs of the body. Esmolol prevents the action of two naturally occurring substances: epinephrine and norepinephrine. Esmolol predominantly blocks the beta-1 receptors in cardiac tissue. Used for the rapid control of ventricular rate in patients with atrial fibrillation or atrial flutter in perioperative, postoperative, or other emergent circumstances where short term control of ventricular rate with a short-acting agent is desirable. Also used in noncompensatory sinus tachycardia where the rapid heart rate requires specific intervention. — NCATS

Clinical trial activity

91 trials · 95 clinical orgs · 18 marketing orgs

Phase 1
12
Phase 2
30
Phase 3
13
Phase 4
27

Earliest trial started Nov 1, 2005 (NCT00226096)

Timeline

1980s

  1. Dec 31, 1986

    Earliest FDA Approval

  2. Dec 31, 1986

    Baxalta — NDA Secondary Org

  3. Dec 31, 1986

    Baxter — NDA Secondary Org

2000s

  1. Aug 10, 2004

    West-Ward Pharmaceutical — Marketing Organization

  2. Aug 10, 2004

    Hikma — Marketing Organization

  3. Jan 1, 2005

    Earliest Phase 2 Sponsor(trial)

  4. May 2, 2005

    Fresenius — Marketing Organization

  5. Jan 1, 2006

    Earliest Phase 3 Sponsor(trial)

  6. Jan 1, 2008

    Earliest Phase 1 Sponsor(trial)

2010s

  1. Feb 20, 2015

    Lutipold — Marketing Organization

  2. Feb 20, 2015

    Sankyo — Marketing Organization

  3. Feb 20, 2015

    Daiichi Sankyo — Marketing Organization

  4. Jul 23, 2015

    Aurobindo Pharma — Marketing Organization

  5. Jul 23, 2015

    Eugia Pharma — Marketing Organization

  6. Apr 7, 2016

    Hq Speciality Pharma — NDA Secondary Org

  7. Sep 23, 2016

    Gland Pharma Ltd — Marketing Organization

  8. Jun 8, 2018

    Mylan — Marketing Organization

  9. Jun 8, 2018

    Sagent Pharmaceuticals, Inc. — Marketing Organization

  10. Jun 8, 2018

    Nichi-Iko Pharmaceutical Co., Ltd. — Marketing Organization

  11. Aug 14, 2019

    Fosun — Marketing Organization

2020s

  1. Dec 2, 2022

    Hq Speciality Pharma — Marketing Organization

  2. Dec 13, 2022

    Amneal Pharmaceuticals — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewDec 31, 1986

Chemistry & pharmacology

Loading structure…

SMILES

COC(=O)CCc1ccc(OCC(O)CNC(C)C)cc1
Mol. weight
295.38 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Racemic Mixture
Inorganic
No
Polymer
No
Delivery
Parenteral
Availability
Prescription Only

Oral

No

Parenteral

Yes

Topical

No

Sources

Also known as

  • 3-[4-(2-hydroxy-3-isopropylamino-propoxy)-phenyl]-propionic acid methyl ester
  • 3-[4-(2-hydroxy-3-isopropylamino-propoxy)-phenyl]-propionic acid methyl ester
  • aop200704
  • asl 8052
  • asl-8052
  • asl-8052
  • asl-8052
  • brevibloc
  • brevibloc
  • brevibloc
  • brevibloc
  • brevibloc
  • brevibloc
  • esmolol
  • esmolol
  • esmolol
  • esmolol
  • esmolol
  • esmolol
  • esmolol
  • esmolol
  • esmolol
  • esmolol
  • (±)-esmolol
  • (±)-esmolol
  • esmolol hcl
  • esmolol hcl
  • esmolol hcl
  • esmolol hydrochloride
  • esmolol hydrochloride
  • esmolol hydrochloride
  • esmolol hydrochloride
  • esmolol hydrochloride
  • methyl 4-(2-hydroxy-3-((1-methylethyl)amino)propoxy)benzenepropanoate
  • methyl 4-(2-hydroxy-3-((1-methylethyl)amino)propoxy)benzenepropanoate
  • (±)-methyl p-(2-hydroxy-3-(isopropylamino)propoxy)hydrocinnamate
  • (±)-methyl p-(2-hydroxy-3-(isopropylamino)propoxy)hydrocinnamate
  • methyl p-(2-hydroxy-3-(isopropylamino)propoxy)hydrocinnamate
  • methyl p-(2-hydroxy-3-(isopropylamino)propoxy)hydrocinnamate

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07211399Early Phase 1 (Phase 1)Jan 1, 2026University of Pittsburgh
NCT07019818Phase 4Nov 2, 2025University of Limoges
NCT06958393Phase 4May 20, 2025Shandong Province Qianfoshan Hospital
NCT06620991N/AOct 10, 2024Ain Shams University
NCT06522594Phase 2Jun 1, 2024Erasmus University Rotterdam
NCT06343753N/AMay 1, 2024Ain Shams University
NCT06291363Phase 4Apr 16, 2024Ciusss de L'Est de l'Île de Montréal
NCT06376630N/AJan 29, 2024Government of Russia
NCT06457100Phase 1/Phase 2 (Phase 2)Nov 21, 2023The Second People's Hospital of Huai'an, Xuzhou Medical University
NCT06013319Phase 3Nov 1, 2023Qianfo Mountain Hospital, Shandong Province, Shandong Province Qianfoshan Hospital
NCT05769868Phase 3Apr 18, 2023Consorcio Centro de Investigación Biomédica en Red, M.P., Hospital General Universitario Gregorio Marañon, Universidad Carlos III Madrid
NCT05694585Phase 4Feb 1, 2023Shandong Province Qianfoshan Hospital
NCT05752799N/AJan 1, 2023Aristotle University of Thessaloniki, Gennimatas Hospital, Athens
NCT05703048N/ADec 30, 2022Tanta University
NCT05635877Phase 4Dec 20, 2022Shandong Province Qianfoshan Hospital
NCT05551832Phase 3Oct 10, 2022Yonsei University
NCT05850832Phase 2/Phase 3 (Phase 3)Oct 5, 2022Alexandria University
NCT05567822N/AOct 1, 2022Aretaieion University
NCT06268275N/ASep 19, 2022KhonKaen University
NCT05389176N/AJul 1, 2022Chinese Medical Association, Nanjing University
Showing 20 of 91 trials
Page 1 / 5

Organizations

Research & Development (95)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
BaxaltaFor profit4032010
Shandong Province Qianfoshan HospitalAcademic/Hospital4422022
Ain Shams UniversityAcademic/Hospital3322019
Ankara Yildirim Beyazıt UniversityAcademic/Hospital3212012
AOP Orphan Pharmaceuticals AGFor profit3322011
Cedars-Sinai Medical CenterAcademic/Hospital3312009
Harvard UniversityAcademic/Hospital3112015
University of BrasiliaAcademic/Hospital3312015
Allegiance HealthAcademic/Hospital2212016
American Heart AssociationAcademic/Hospital2012005
Cepha s.r.oFor profit2012012
George Papanicolaou HospitalAcademic/Hospital2212014
National Health and Medical Research Council, AustraliaGovernment2022005
Northwestern UniversityAcademic/Hospital2222013
Novalead Pharma Private LimitedFor profit2222014
The University of Texas, DallasAcademic/Hospital2112005
University of New South WalesAcademic/Hospital2222005
University of Texas, GalvestonAcademic/Hospital2112015
Aarhus UniversityAcademic/Hospital1012006
Alexandria UniversityAcademic/Hospital1112022
95 organizations
Page 1 / 5

Marketing (23)

OrganizationOrg typeRelationshipDate
Amneal PharmaceuticalsFor profitMKTGDec 13, 2022
Aurobindo PharmaFor profitMKTGJul 23, 2015
BaxaltaFor profitNDA2Dec 31, 1986
BaxterFor profitNDA2Dec 31, 1986
Daiichi SankyoFor profitMKTGFeb 20, 2015
DuPontFor profitNDA—
Eugia PharmaFor profitMKTGJul 23, 2015
FosunFor profitMKTGAug 14, 2019
FreseniusFor profitMKTGMay 2, 2005
Gland Pharma LtdFor profitMKTGSep 23, 2016
Gland Pharma LtdFor profitSYNAug 14, 2019
HikmaFor profitSYNAug 10, 2004
HikmaFor profitMKTGAug 10, 2004
Hq Speciality PharmaFor profitNDA2Apr 7, 2016
Hq Speciality PharmaFor profitMKTGDec 2, 2022
LutipoldFor profitMKTGFeb 20, 2015
MylanFor profitSYNMay 2, 2005
MylanFor profitMKTGJun 8, 2018
Nichi-Iko Pharmaceutical Co., Ltd.For profitMKTGJun 8, 2018
Sagent Pharmaceuticals, Inc.For profitMKTGJun 8, 2018
Sagent Pharmaceuticals, Inc.For profitSYNJun 8, 2018
SankyoFor profitMKTGFeb 20, 2015
West-Ward PharmaceuticalFor profitMKTGAug 10, 2004