nebivolol

Trade name: bystolic

Small moleculeapproved

Approved

Dec 17, 2007

Nebivolol is a competitive and highly selective beta-1 receptor antagonist with mild vasodilating properties, possibly due to an interaction with the L-arginine/nitric oxide pathway. In preclinical studies, nebivolol has been shown to induce endothelium-dependent arterial relaxation in a dose dependent manner, by stimulation of the release of endothelial nitric oxide. Nitric oxide acts to relax vascular smooth muscle cells and inhibits platelet aggregation and adhesion. Activation of β1-receptors by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Nebivolol blocks these receptors which reverses the effects of epinephrine, lowering the heart rate and blood pressure. In addition, beta blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels. At high enough concentrations, this drug may also bind beta 2 receptors. Marketed under the brand name BYSTOLIC, Nebivolol is indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. — NCATS

Clinical trial activity

98 trials · 83 clinical orgs · 26 marketing orgs

Phase 1
6
Phase 2
25
Phase 3
22
Phase 4
48

Earliest trial started Mar 1, 2000 (NCT00295542)

Timeline

2000s

  1. Jan 1, 2001

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2001

    Earliest Phase 3 Sponsor(trial)

  3. Jan 1, 2002

    Earliest Phase 2 Sponsor(trial)

  4. Dec 17, 2007

    Earliest FDA Approval

  5. Dec 17, 2007

    Allergan — NDA Secondary Org

  6. Dec 17, 2007

    GlaxoSmithKline — NDA Secondary Org

2010s

  1. Apr 16, 2015

    Amerigen Pharmaceuticals — Marketing Organization

  2. Apr 16, 2015

    Ani Pharmaceuticals — Marketing Organization

  3. Jun 24, 2015

    Alkem Labs Ltd — Marketing Organization

  4. Jul 29, 2015

    Indchemie Health — Marketing Organization

  5. Nov 27, 2015

    Watson Pharmaceuticals — Marketing Organization

  6. Nov 27, 2015

    Allergan PLC (2015) — Marketing Organization

  7. Jun 3, 2016

    AbbVie — NDA Secondary Org

  8. May 25, 2017

    Glenmark Pharmaceuticals — Marketing Organization

  9. Mar 2, 2018

    Torrent Pharmaceuticals Limited — Marketing Organization

  10. Dec 28, 2018

    Micro Labs Ltd India — Marketing Organization

2020s

  1. Nov 3, 2020

    Hetero Labs Ltd — Marketing Organization

  2. Dec 17, 2021

    Aurobindo Pharma — Marketing Organization

  3. Dec 17, 2021

    Cadila Healthcare — Marketing Organization

  4. Dec 17, 2021

    Reyoung Pharma Co Ltd — Marketing Organization

  5. Mar 15, 2022

    Unichem — Marketing Organization

  6. Mar 31, 2022

    Ajanta Pharma Ltd — Marketing Organization

  7. Mar 31, 2022

    Chartwell Pharmaceuticals — Marketing Organization

  8. Apr 7, 2022

    Prinston Inc — Marketing Organization

  9. Nov 14, 2022

    Mankind Pharma — Marketing Organization

  10. Mar 30, 2023

    Beximco — Marketing Organization

  11. Feb 27, 2024

    Apotex — Marketing Organization

  12. Oct 1, 2024

    MSN Laboratories — Marketing Organization

  13. Jan 28, 2025

    Macleods Pharmaceuticals, Ltd — Marketing Organization

Indications

Approved for

Mechanism of action

Combination products

Approval history

  • approvedDec 17, 2007

Chemistry & pharmacology

Loading structure…

SMILES

OC(CNCC(O)C1CCc2cc(F)ccc2O1)C1CCc2cc(F)ccc2O1
Mol. weight
405.44 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Racemic Mixture
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • 1,1'-[bis(6-fluoro-3,4-dihydro-2h-1-benzopyran-2-yl)]-2,2'-iminodiethanol
  • 1,1'-[bis(6-fluoro-3,4-dihydro-2h-1-benzopyran-2-yl)]-2,2'-iminodiethanol
  • 1,1'-bis(6-fluoro-3,4-dihydro-2h-1-benzopyran-2-yl)-2,2'-iminodiethanol
  • 1,1'-bis(6-fluoro-3,4-dihydro-2h-1-benzopyran-2-yl)-2,2'-iminodiethanol
  • alpha,alpha'-(iminobismethylene)bis-(6-fluoro-3,4-dihydro-2h-1-benzopyran-2-methanol)
  • alpha,alpha'-(iminobismethylene)bis-(6-fluoro-3,4-dihydro-2h-1-benzopyran-2-methanol)
  • alpha,alpha'-(iminodimethylene)bis-(6-fluoro-2-chromanmethanol)
  • alpha,alpha'-(iminodimethylene)bis-(6-fluoro-2-chromanmethanol)
  • bystolic
  • bystolic
  • bystolic
  • bystolic
  • hypoloc
  • narbivolol
  • narbivolol
  • nebilet
  • nebilet
  • nebivolol
  • nebivolol
  • nebivolol
  • nebivolol
  • nebivolol
  • nebivolol
  • nebivolol
  • nebivolol
  • nebivolol
  • nebivolol
  • nebivolol hcl
  • nebivolol hcl
  • nebivolol hcl
  • nebivolol hydrochloride
  • nebivolol hydrochloride
  • nebivolol hydrochloride
  • nebivolol hydrochloride
  • nebivolol hydrochloride
  • nebivololum
  • nebivololum
  • nevibolol
  • r-65824
  • r-65824
  • ro-67555
  • ro-67555
  • vasoxen

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06755801Phase 3Apr 1, 2025Spanish Society of Cardiology
NCT07233499Phase 2Jan 1, 2025Ain Shams University, National Cancer Institute, Egypt
NCT06249802Phase 4Jan 1, 2025Jagiellonian University, Szpital Uniwersytecki w Krakowie
NCT06424834Phase 2/Phase 3 (Phase 3)Aug 29, 2024American Heart Association, Stanford University
NCT06248099Phase 1Jul 9, 2024Bio-innova Co., Ltd
NCT06201611Phase 2/Phase 3 (Phase 3)Jul 1, 2024St. John's Research Institute
NCT06035978Phase 4Nov 30, 2023University of Ostrava
NCT06104423Phase 4Oct 2, 2023Menarini Group, University of Roma La Sapienza
NCT05513937Phase 4May 12, 2022Menarini Group, University of Roma La Sapienza
NCT04845061Phase 4Oct 1, 2021Ain Shams University
NCT04888728Phase 1Jun 30, 2021Daewoong Pharmaceutical Co. LTD., Paik hospital
NCT05257148Phase 4Apr 28, 2021Menarini Group, University of Roma La Sapienza
NCT04910100Phase 2Apr 15, 2021Novaliq GmbH, Summit Analytical, LLC, Trial Runners, LLC
NCT04513509N/AAug 7, 2020National Taiwan University
NCT04432610Phase 4Mar 1, 2020Clinical Hospital Center Zemun
NCT04130438Phase 2Nov 1, 2019Stanford University
NCT05328310N/AJan 6, 2019Korea University
NCT05728632Phase 3Jan 1, 2019Agenzia Italiana del Farmaco, Humanitas University
NCT03778554Phase 4Dec 17, 2018Central Denmark Region, Danish Heart Foundation, Novo Nordisk, Region of Southern Denmark, Region Zealand, The Capital Region of Denmark, The North Denmark Region, University of Copenhagen
NCT03655964Phase 2Aug 20, 2018Aristotle University of Thessaloniki
Showing 20 of 98 trials
Page 1 / 5

Organizations

Research & Development (83)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Forest LaboratoriesFor profit381342007
MylanFor profit10932001
Menarini GroupFor profit8532005
Emory UniversityAcademic/Hospital3312009
University of Roma La SapienzaAcademic/Hospital3012021
Vanderbilt UniversityAcademic/Hospital3332001
Ain Shams UniversityAcademic/Hospital2222021
Aristotle University of ThessalonikiAcademic/Hospital2222010
Harvard UniversityAcademic/Hospital2222012
Korea UniversityAcademic/Hospital2222016
Mayo ClinicAcademic/Hospital2222012
Stanford UniversityAcademic/Hospital2222019
The University of Texas, DallasAcademic/Hospital2212009
Torrent Pharmaceuticals LimitedFor profit2212011
University of California, San DiegoAcademic/Hospital2212010
University of ChicagoAcademic/Hospital2212009
University of Colorado, BoulderAcademic/Hospital2212011
University of FloridaAcademic/Hospital2212010
University of MississippiAcademic/Hospital2212009
University of TartuAcademic/Hospital2112006
83 organizations
Page 1 / 5

Marketing (28)

OrganizationOrg typeRelationshipDate
AbbVieFor profitNDA2Jun 3, 2016
Ajanta Pharma LtdFor profitMKTGMar 31, 2022
Alkem Labs LtdFor profitMKTGJun 24, 2015
AllerganFor profitNDA2Dec 17, 2007
AllerganFor profitSYNDec 17, 2007
Allergan PLC (2015)For profitMKTGNov 27, 2015
Amerigen PharmaceuticalsFor profitMKTGApr 16, 2015
Ani PharmaceuticalsFor profitSYNApr 16, 2015
Ani PharmaceuticalsFor profitMKTGApr 16, 2015
ApotexFor profitMKTGFeb 27, 2024
Aurobindo PharmaFor profitMKTGDec 17, 2021
BeximcoFor profitMKTGMar 30, 2023
Cadila HealthcareFor profitMKTGDec 17, 2021
Chartwell PharmaceuticalsFor profitMKTGMar 31, 2022
Forest LaboratoriesFor profitNDA
GlaxoSmithKlineFor profitNDA2Dec 17, 2007
Glenmark PharmaceuticalsFor profitMKTGMay 25, 2017
Hetero Labs LtdFor profitMKTGNov 3, 2020
Indchemie HealthFor profitMKTGJul 29, 2015
MSN LaboratoriesFor profitMKTGOct 1, 2024
Macleods Pharmaceuticals, LtdFor profitMKTGJan 28, 2025
Mankind PharmaFor profitMKTGNov 14, 2022
Micro Labs Ltd IndiaFor profitMKTGDec 28, 2018
Prinston IncFor profitMKTGApr 7, 2022
Reyoung Pharma Co LtdFor profitMKTGDec 17, 2021
Torrent Pharmaceuticals LimitedFor profitMKTGMar 2, 2018
UnichemFor profitMKTGMar 15, 2022
Watson PharmaceuticalsFor profitMKTGNov 27, 2015