nebivolol
Trade name: bystolic
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
Earliest trial started Mar 1, 2000 (NCT00295542)
Timeline
2000s
- Jan 1, 2001
Earliest Phase 1 Sponsor(trial)
- Jan 1, 2001
Earliest Phase 3 Sponsor(trial)
- Jan 1, 2002
Earliest Phase 2 Sponsor(trial)
- Dec 17, 2007
Earliest FDA Approval
- Dec 17, 2007
Allergan — NDA Secondary Org
- Dec 17, 2007
GlaxoSmithKline — NDA Secondary Org
2010s
- Apr 16, 2015
Amerigen Pharmaceuticals — Marketing Organization
- Apr 16, 2015
Ani Pharmaceuticals — Marketing Organization
- Jun 24, 2015
Alkem Labs Ltd — Marketing Organization
- Jul 29, 2015
Indchemie Health — Marketing Organization
- Nov 27, 2015
Watson Pharmaceuticals — Marketing Organization
- Nov 27, 2015
Allergan PLC (2015) — Marketing Organization
- Jun 3, 2016
AbbVie — NDA Secondary Org
- May 25, 2017
Glenmark Pharmaceuticals — Marketing Organization
- Mar 2, 2018
Torrent Pharmaceuticals Limited — Marketing Organization
- Dec 28, 2018
Micro Labs Ltd India — Marketing Organization
2020s
- Nov 3, 2020
Hetero Labs Ltd — Marketing Organization
- Dec 17, 2021
Aurobindo Pharma — Marketing Organization
- Dec 17, 2021
Cadila Healthcare — Marketing Organization
- Dec 17, 2021
Reyoung Pharma Co Ltd — Marketing Organization
- Mar 15, 2022
Unichem — Marketing Organization
- Mar 31, 2022
Ajanta Pharma Ltd — Marketing Organization
- Mar 31, 2022
Chartwell Pharmaceuticals — Marketing Organization
- Apr 7, 2022
Prinston Inc — Marketing Organization
- Nov 14, 2022
Mankind Pharma — Marketing Organization
- Mar 30, 2023
Beximco — Marketing Organization
- Feb 27, 2024
Apotex — Marketing Organization
- Oct 1, 2024
MSN Laboratories — Marketing Organization
- Jan 28, 2025
Macleods Pharmaceuticals, Ltd — Marketing Organization
Indications
Approved for
Studied for
- Altitude · Phase 4
- Angina Pectoris · Phase 2/Phase 3
- Arterial Pressure · Phase 4
- Atherosclerosis · Phase 4
- Breast Neoplasms · Phase 3
- Cardiomyopathies · Phase 3
- Cardiotoxicity · Phase 3
- Cardiovascular Diseases · Phase 4
- Coronary Artery Disease · Phase 4
- Coronary Disease · Phase 3
- Coronary Vasospasm · Phase 4
- Diabetes Mellitus · Phase 2/Phase 3
- Diabetes Mellitus, Type 2 · Phase 4
- Drug-Related Side Effects and Adverse Reactions · Phase 4
- Endothelial Cells · Phase 4
- Endothelium · Phase 4
- Erectile Dysfunction · Phase 4
- Essential Hypertension · Phase 4
- Glaucoma, Open-Angle · Phase 2
- Healthy Volunteers · Phase 1
- Heart Failure · Phase 4
- Heart Failure, Diastolic · Phase 4
- Heart Failure, Systolic · Phase 4
- Hypertension, Pulmonary · Phase 4
- Hypoxia · Phase 4
- Idiopathic Pulmonary Fibrosis · Phase 1
- Intracranial Aneurysm · Phase 4
- Ischemic Stroke · Phase 2
- Lymphoma, Large B-Cell, Diffuse · Phase 3
- Marfan Syndrome · Phase 3
- Metabolic Syndrome · Phase 4
- Microvascular Angina · Phase 4
- Muscular Dystrophy, Duchenne · Phase 3
- Myocardial Bridging · Phase 2/Phase 3
- Myocardial Infarction · Phase 4
- Ocular Hypertension · Phase 2
- Peripheral Arterial Disease · Phase 3
- Prehypertension · Phase 4
- Pulmonary Disease, Chronic Obstructive · Phase 4
- Renal Insufficiency, Chronic · Phase 4
- Sleep Apnea, Obstructive · Phase 4
- ST Elevation Myocardial Infarction · Phase 4
- Stroke · Phase 4
- Ventricular Dysfunction, Left · Phase 3
Mechanism of action
- Beta-1 adrenergic receptorANTAGONIST
ADRB1 antagonist
- Beta-2 adrenergic receptorANTAGONIST
ADRB2 antagonist
Combination products
byvalson
with valsartan
Approval history
- approvedDec 17, 2007
Chemistry & pharmacology
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
- ChEMBLCHEMBL434394 ↗
- WikipediaNebivolol ↗
- NCATS030Y90569U ↗
- ChEMBLCHEMBL1201731 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06755801 | Phase 3 | Apr 1, 2025 | Spanish Society of Cardiology |
| NCT07233499 | Phase 2 | Jan 1, 2025 | Ain Shams University, National Cancer Institute, Egypt |
| NCT06249802 | Phase 4 | Jan 1, 2025 | Jagiellonian University, Szpital Uniwersytecki w Krakowie |
| NCT06424834 | Phase 2/Phase 3 (Phase 3) | Aug 29, 2024 | American Heart Association, Stanford University |
| NCT06248099 | Phase 1 | Jul 9, 2024 | Bio-innova Co., Ltd |
| NCT06201611 | Phase 2/Phase 3 (Phase 3) | Jul 1, 2024 | St. John's Research Institute |
| NCT06035978 | Phase 4 | Nov 30, 2023 | University of Ostrava |
| NCT06104423 | Phase 4 | Oct 2, 2023 | Menarini Group, University of Roma La Sapienza |
| NCT05513937 | Phase 4 | May 12, 2022 | Menarini Group, University of Roma La Sapienza |
| NCT04845061 | Phase 4 | Oct 1, 2021 | Ain Shams University |
| NCT04888728 | Phase 1 | Jun 30, 2021 | Daewoong Pharmaceutical Co. LTD., Paik hospital |
| NCT05257148 | Phase 4 | Apr 28, 2021 | Menarini Group, University of Roma La Sapienza |
| NCT04910100 | Phase 2 | Apr 15, 2021 | Novaliq GmbH, Summit Analytical, LLC, Trial Runners, LLC |
| NCT04513509 | N/A | Aug 7, 2020 | National Taiwan University |
| NCT04432610 | Phase 4 | Mar 1, 2020 | Clinical Hospital Center Zemun |
| NCT04130438 | Phase 2 | Nov 1, 2019 | Stanford University |
| NCT05328310 | N/A | Jan 6, 2019 | Korea University |
| NCT05728632 | Phase 3 | Jan 1, 2019 | Agenzia Italiana del Farmaco, Humanitas University |
| NCT03778554 | Phase 4 | Dec 17, 2018 | Central 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 |
| NCT03655964 | Phase 2 | Aug 20, 2018 | Aristotle University of Thessaloniki |
Organizations
Research & Development (83)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Forest Laboratories | For profit | 38 | 13 | 4 | 2007 |
| Mylan | For profit | 10 | 9 | 3 | 2001 |
| Menarini Group | For profit | 8 | 5 | 3 | 2005 |
| Emory University | Academic/Hospital | 3 | 3 | 1 | 2009 |
| University of Roma La Sapienza | Academic/Hospital | 3 | 0 | 1 | 2021 |
| Vanderbilt University | Academic/Hospital | 3 | 3 | 3 | 2001 |
| Ain Shams University | Academic/Hospital | 2 | 2 | 2 | 2021 |
| Aristotle University of Thessaloniki | Academic/Hospital | 2 | 2 | 2 | 2010 |
| Harvard University | Academic/Hospital | 2 | 2 | 2 | 2012 |
| Korea University | Academic/Hospital | 2 | 2 | 2 | 2016 |
| Mayo Clinic | Academic/Hospital | 2 | 2 | 2 | 2012 |
| Stanford University | Academic/Hospital | 2 | 2 | 2 | 2019 |
| The University of Texas, Dallas | Academic/Hospital | 2 | 2 | 1 | 2009 |
| Torrent Pharmaceuticals Limited | For profit | 2 | 2 | 1 | 2011 |
| University of California, San Diego | Academic/Hospital | 2 | 2 | 1 | 2010 |
| University of Chicago | Academic/Hospital | 2 | 2 | 1 | 2009 |
| University of Colorado, Boulder | Academic/Hospital | 2 | 2 | 1 | 2011 |
| University of Florida | Academic/Hospital | 2 | 2 | 1 | 2010 |
| University of Mississippi | Academic/Hospital | 2 | 2 | 1 | 2009 |
| University of Tartu | Academic/Hospital | 2 | 1 | 1 | 2006 |
Marketing (28)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| AbbVie | For profit | NDA2 | Jun 3, 2016 |
| Ajanta Pharma Ltd | For profit | MKTG | Mar 31, 2022 |
| Alkem Labs Ltd | For profit | MKTG | Jun 24, 2015 |
| Allergan | For profit | NDA2 | Dec 17, 2007 |
| Allergan | For profit | SYN | Dec 17, 2007 |
| Allergan PLC (2015) | For profit | MKTG | Nov 27, 2015 |
| Amerigen Pharmaceuticals | For profit | MKTG | Apr 16, 2015 |
| Ani Pharmaceuticals | For profit | SYN | Apr 16, 2015 |
| Ani Pharmaceuticals | For profit | MKTG | Apr 16, 2015 |
| Apotex | For profit | MKTG | Feb 27, 2024 |
| Aurobindo Pharma | For profit | MKTG | Dec 17, 2021 |
| Beximco | For profit | MKTG | Mar 30, 2023 |
| Cadila Healthcare | For profit | MKTG | Dec 17, 2021 |
| Chartwell Pharmaceuticals | For profit | MKTG | Mar 31, 2022 |
| Forest Laboratories | For profit | NDA | — |
| GlaxoSmithKline | For profit | NDA2 | Dec 17, 2007 |
| Glenmark Pharmaceuticals | For profit | MKTG | May 25, 2017 |
| Hetero Labs Ltd | For profit | MKTG | Nov 3, 2020 |
| Indchemie Health | For profit | MKTG | Jul 29, 2015 |
| MSN Laboratories | For profit | MKTG | Oct 1, 2024 |
| Macleods Pharmaceuticals, Ltd | For profit | MKTG | Jan 28, 2025 |
| Mankind Pharma | For profit | MKTG | Nov 14, 2022 |
| Micro Labs Ltd India | For profit | MKTG | Dec 28, 2018 |
| Prinston Inc | For profit | MKTG | Apr 7, 2022 |
| Reyoung Pharma Co Ltd | For profit | MKTG | Dec 17, 2021 |
| Torrent Pharmaceuticals Limited | For profit | MKTG | Mar 2, 2018 |
| Unichem | For profit | MKTG | Mar 15, 2022 |
| Watson Pharmaceuticals | For profit | MKTG | Nov 27, 2015 |