doxazosin
Trade name: cardura
Approved
Nov 2, 1990
Doxazosin mesylate is a quinazoline compound sold by Pfizer under the brand name CARDURA. CARDURA is indicated for the treatment of both the urinary outflow obstruction and obstructive and irritative symptoms associated with BPH: obstructive symptoms (hesitation, intermittency, dribbling, weak urinary stream, incomplete emptying of the bladder) and irritative symptoms (nocturia, daytime frequency, urgency, burning). CARDURA may be used in all BPH patients whether hypertensive or normotensive. In patients with hypertension and BPH, both conditions were effectively treated with CARDURA monotherapy. CARDURA provides rapid improvement in symptoms and urinary flow rate in 66–71% of patients. CARDURA is also indicated for the treatment of hypertension. CARDURA may be used alone or in combination with diuretics, beta-adrenergic blocking agents, calcium channel blockers, or angiotensin-converting enzyme inhibitors. Doxazosin acts by inhibiting the postsynaptic alpha(1)-adrenoceptors on vascular smooth muscle. This inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation. — NCATS
Clinical trial activity
52 trials · 92 clinical orgs · 27 marketing orgs
Earliest trial started Aug 1, 1985 (NCT00000522)
Timeline
1980s
- Jan 1, 1985
Earliest Phase 2 Sponsor(trial)
1990s
2000s
- Oct 18, 2000
Actavis — Marketing Organization
- Oct 18, 2000
Ani Pharmaceuticals — Marketing Organization
- Oct 18, 2000
Apotex — Marketing Organization
- Oct 18, 2000
Genpharm — Marketing Organization
- Oct 18, 2000
Teva — Marketing Organization
- Oct 18, 2000
Nesher Pharms — Marketing Organization
- Oct 18, 2000
Watson Pharmaceuticals — Marketing Organization
- Oct 18, 2000
Chartwell Pharmaceuticals — Marketing Organization
- Oct 18, 2000
Fosun — Marketing Organization
- Oct 18, 2000
Medarex — Marketing Organization
- Oct 19, 2000
Mylan — Marketing Organization
- Oct 19, 2000
Aurobindo Pharma — Marketing Organization
- Jun 8, 2001
Pliva — Marketing Organization
- Jun 10, 2004
DAVA Pharmaceuticals — Marketing Organization
- Jun 10, 2004
Strides Pharma Science — Marketing Organization
- Jan 1, 2005
Earliest Phase 1 Sponsor(trial)
2010s
- Jun 11, 2014
Accord Research — Marketing Organization
- Jul 7, 2017
Zydus Discovery DMCC — Marketing Organization
- Feb 13, 2018
Heritage Pharma — Marketing Organization
- Feb 13, 2018
Emcure — Marketing Organization
- Apr 17, 2018
Upsher-Smith Laboratories — Marketing Organization
- Apr 17, 2018
Appco Pharma — Marketing Organization
2020s
- Mar 15, 2022
Pharmgen — Marketing Organization
- Mar 15, 2022
Rising Pharmaceuticals — Marketing Organization
- Jan 10, 2024
Unichem — Marketing Organization
Indications
Studied for
- Alcohol-Induced Disorders · Phase 2
- Alcoholism · Phase 2
- Amphetamine-Related Disorders · Phase 1
- Anxiety · Phase 2
- Cardiomyopathy, Dilated · Phase 4
- Cardiovascular Diseases · Phase 4
- Cocaine-Related Disorders · Phase 2
- Coronary Disease · Phase 3
- COVID-19 · Phase 3
- Diabetes Mellitus · Phase 4
- Diabetic Nephropathies · Phase 4
- Erectile Dysfunction · Phase 1
- Essential Hypertension · Phase 4
- Healthy Volunteers · Phase 1
- Heart Diseases · Phase 3
- Heart Failure · Phase 3
- Hypercholesterolemia · Phase 3
- Kidney Calculi · Phase 3
- Methamphetamine · Phase 1/Phase 2
- Mood Disorders · Phase 1
- Myocardial Infarction · Phase 3
- Myocardial Ischemia · Phase 3
- Paraganglioma · Phase 3
- Pheochromocytoma · Phase 4
- Prostate · Phase 4
- Prostatic Hyperplasia · Phase 4
- Renal Insufficiency · Phase 4
- Renal Insufficiency, Chronic · Phase 4
- Rhinitis, Allergic · Phase 4
- Severe acute respiratory syndrome-related coronavirus · Phase 3
- Smoking · Phase 2
- Stress Disorders, Post-Traumatic · Phase 4
- Stroke · Phase 4
- Substance-Related Disorders · Phase 1
- Urinary Bladder Neck Obstruction · Phase 4
- Urinary Bladder, Overactive · Phase 4
- Vascular Diseases · Phase 2
Mechanism of action
- Adrenergic receptor alpha-1ANTAGONIST
Adrenergic receptor alpha-1 antagonist
Approval history
- approvedNov 2, 1990
Chemistry & pharmacology
SMILES
COc1cc2nc(N3CCN(C(=O)C4COc5ccccc5O4)CC3)nc(N)c2cc1OC- Mol. weight
- 451.48 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
- ChEMBLCHEMBL707 ↗
- WikipediaDoxazosin ↗
- NCATSNW1291F1W8 ↗
- ChEMBLCHEMBL1200561 ↗
Also known as
- 1-(4-amino-6,7-dimethoxy-2-chinazolinyl)-4-(2,3-dihydro-1,4-benzodioxixin-2-ylcarbonyl)piperazin
- 1-(4-amino-6,7-dimethoxy-2-chinazolinyl)-4-(2,3-dihydro-1,4-benzodioxixin-2-ylcarbonyl)piperazin
- 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(1,4-benzodioxan-2-ylcarbonyl)piperazin
- 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(1,4-benzodioxan-2-ylcarbonyl)piperazin
- cardozin xl
- cardura
- cardura
- cardura
- cardura xl
- cardura xl
- cascor
- colixil xl
- doxadura
- doxazosin
- doxazosin
- doxazosin
- doxazosin
- doxazosin
- doxazosin
- doxazosin
- doxazosin
- doxazosin
- doxazosin
- doxazosina
- doxazosina
- doxazosine
- doxazosin mesilate
- doxazosin mesilate
- doxazosin mesilate
- doxazosin mesylate
- doxazosin mesylate
- doxazosin mesylate
- doxazosin mesylate
- doxazosinum
- doxazosinum
- doxzogen xl
- larbex xl
- oxandosin xl
- raporsin xl
- slocinx xl
- uk-3327427
- uk-3327427
- uk-33274-27
- uk-33274-27
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05360953 | Phase 2 | Apr 6, 2022 | German Federal Ministry of Education and Research, Humboldt University |
| NCT04727424 | Phase 3 | Jan 19, 2021 | Cardresearch - Cardiologia Assistencial e de Pesquisa LTDA, Cytel Inc., Eiger BioPharmaceuticals, Fast Grants, McMaster University, RainWater Foundation |
| NCT04371757 | N/A | Apr 30, 2020 | Federal University of Rio Grande do Sul |
| NCT04135846 | Phase 2 | Dec 1, 2019 | Brown University |
| NCT03398252 | Phase 1 | Jun 30, 2018 | University of Texas at Houston |
| NCT03339258 | Phase 2 | Apr 15, 2018 | Department of Defense, Department of Veteran Affairs, Northern California Institute of Research and Education |
| NCT03176693 | Phase 3 | May 5, 2017 | University of California, Los Angeles |
| NCT02989493 | Phase 2 | Apr 12, 2017 | National Institute on Alcohol Abuse and Alcoholism (NIAAA), University of Wisconsin |
| NCT02492334 | Phase 1/Phase 2 (Phase 2) | Jul 1, 2016 | Department of Veteran Affairs, Medical University of South Carolina, University of South Carolina |
| NCT02500602 | Phase 2 | Jun 1, 2016 | Consortium to Alleviate PTSD, Department of Veteran Affairs, Medical University of South Carolina |
| NCT02563405 | Phase 2/Phase 3 (Phase 3) | Sep 1, 2015 | Harbin Medical University |
| NCT02538744 | Phase 1 | Aug 1, 2015 | Baylor University |
| NCT01953432 | Phase 2 | Apr 1, 2014 | Baylor University, Department of Veteran Affairs |
| NCT01959022 | Phase 4 | Oct 1, 2013 | Department of Defense, Department of Veteran Affairs, Northern California Institute of Research and Education |
| NCT01946035 | Phase 4 | Sep 1, 2013 | University of Dundee |
| NCT01730846 | Phase 2 | Feb 1, 2013 | National Institute on Drug Abuse (NIDA), Yale University |
| NCT01678313 | Phase 2 | Aug 1, 2012 | Tzu Chi University |
| NCT01661621 | Phase 4 | Aug 1, 2012 | Tzu Chi University |
| NCT02308202 | Phase 1 | Jan 1, 2012 | Baylor University |
| NCT01379898 | Phase 4 | Dec 1, 2011 | Atrium Medical Center, Canisius-Wilhelmina Hospital, Erasmus University Rotterdam, Free University of Amsterdam, Isala Clinics, Zwolle, The Netherlands, Leiden University, Maastricht University, Medical Center Haaglanden, Medical Center Leeuwarden, Medisch Spectrum Twente, Onze Lieve Vrouw Hospital, Radboud University, St. Antonius Hospital, Nieuwegein, University of Amsterdam, University of Groningen, Utrecht University |
Organizations
Research & Development (92)
Marketing (31)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Accord Research | For profit | MKTG | Jun 11, 2014 |
| Actavis | For profit | MKTG | Oct 18, 2000 |
| Ani Pharmaceuticals | For profit | MKTG | Oct 18, 2000 |
| Ani Pharmaceuticals | For profit | SYN | Oct 18, 2000 |
| Apotex | For profit | MKTG | Oct 18, 2000 |
| Appco Pharma | For profit | MKTG | Apr 17, 2018 |
| Aurobindo Pharma | For profit | MKTG | Oct 19, 2000 |
| Chartwell Pharmaceuticals | For profit | MKTG | Oct 18, 2000 |
| DAVA Pharmaceuticals | For profit | MKTG | Jun 10, 2004 |
| Emcure | For profit | MKTG | Feb 13, 2018 |
| Fosun | For profit | MKTG | Oct 18, 2000 |
| Genpharm | For profit | MKTG | Oct 18, 2000 |
| Heritage Pharma | For profit | MKTG | Feb 13, 2018 |
| Medarex | For profit | MKTG | Oct 18, 2000 |
| Mylan | For profit | MKTG | Oct 19, 2000 |
| Mylan | For profit | SYN | Mar 15, 2022 |
| Nesher Pharms | For profit | MKTG | Oct 18, 2000 |
| Pfizer | For profit | NDA | Nov 2, 1990 |
| Pharmgen | For profit | MKTG | Mar 15, 2022 |
| Pliva | For profit | MKTG | Jun 8, 2001 |
| Rising Pharmaceuticals | For profit | MKTG | Mar 15, 2022 |
| Strides Pharma Science | For profit | MKTG | Jun 10, 2004 |
| Teva | For profit | MKTG | Oct 18, 2000 |
| Teva | For profit | SYN | Oct 18, 2000 |
| Unichem | For profit | MKTG | Jan 10, 2024 |
| Upjohn | For profit | MKTG | Nov 2, 1990 |
| Upsher-Smith Laboratories | For profit | MKTG | Apr 17, 2018 |
| Viatris | For profit | MKTG | Nov 2, 1990 |
| Viatris | For profit | NDA2 | Nov 2, 1990 |
| Watson Pharmaceuticals | For profit | MKTG | Oct 18, 2000 |
| Zydus Discovery DMCC | For profit | MKTG | Jul 7, 2017 |