doxazosin

Trade name: cardura

Small moleculeapproved

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

Phase 1
12
Phase 2
18
Phase 3
6
Phase 4
18

Earliest trial started Aug 1, 1985 (NCT00000522)

Timeline

1980s

  1. Jan 1, 1985

    Earliest Phase 2 Sponsor(trial)

1990s

  1. Nov 2, 1990

    Pfizer — Earliest FDA Approval

  2. Nov 2, 1990

    Viatris — Marketing Organization

  3. Nov 2, 1990

    Pfizer — NDA Organization

  4. Nov 2, 1990

    Upjohn — Marketing Organization

  5. Nov 2, 1990

    Viatris — NDA Secondary Org

  6. Jan 1, 1993

    Earliest Phase 3 Sponsor(trial)

2000s

  1. Oct 18, 2000

    Actavis — Marketing Organization

  2. Oct 18, 2000

    Ani Pharmaceuticals — Marketing Organization

  3. Oct 18, 2000

    Apotex — Marketing Organization

  4. Oct 18, 2000

    Genpharm — Marketing Organization

  5. Oct 18, 2000

    Teva — Marketing Organization

  6. Oct 18, 2000

    Nesher Pharms — Marketing Organization

  7. Oct 18, 2000

    Watson Pharmaceuticals — Marketing Organization

  8. Oct 18, 2000

    Chartwell Pharmaceuticals — Marketing Organization

  9. Oct 18, 2000

    Fosun — Marketing Organization

  10. Oct 18, 2000

    Medarex — Marketing Organization

  11. Oct 19, 2000

    Mylan — Marketing Organization

  12. Oct 19, 2000

    Aurobindo Pharma — Marketing Organization

  13. Jun 8, 2001

    Pliva — Marketing Organization

  14. Jun 10, 2004

    DAVA Pharmaceuticals — Marketing Organization

  15. Jun 10, 2004

    Strides Pharma Science — Marketing Organization

  16. Jan 1, 2005

    Earliest Phase 1 Sponsor(trial)

2010s

  1. Jun 11, 2014

    Accord Research — Marketing Organization

  2. Jul 7, 2017

    Zydus Discovery DMCC — Marketing Organization

  3. Feb 13, 2018

    Heritage Pharma — Marketing Organization

  4. Feb 13, 2018

    Emcure — Marketing Organization

  5. Apr 17, 2018

    Upsher-Smith Laboratories — Marketing Organization

  6. Apr 17, 2018

    Appco Pharma — Marketing Organization

2020s

  1. Mar 15, 2022

    Pharmgen — Marketing Organization

  2. Mar 15, 2022

    Rising Pharmaceuticals — Marketing Organization

  3. Jan 10, 2024

    Unichem — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedNov 2, 1990

Chemistry & pharmacology

Loading structure…

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

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 IDPhaseStart dateSponsor(s)
NCT05360953Phase 2Apr 6, 2022German Federal Ministry of Education and Research, Humboldt University
NCT04727424Phase 3Jan 19, 2021Cardresearch - Cardiologia Assistencial e de Pesquisa LTDA, Cytel Inc., Eiger BioPharmaceuticals, Fast Grants, McMaster University, RainWater Foundation
NCT04371757N/AApr 30, 2020Federal University of Rio Grande do Sul
NCT04135846Phase 2Dec 1, 2019Brown University
NCT03398252Phase 1Jun 30, 2018University of Texas at Houston
NCT03339258Phase 2Apr 15, 2018Department of Defense, Department of Veteran Affairs, Northern California Institute of Research and Education
NCT03176693Phase 3May 5, 2017University of California, Los Angeles
NCT02989493Phase 2Apr 12, 2017National Institute on Alcohol Abuse and Alcoholism (NIAAA), University of Wisconsin
NCT02492334Phase 1/Phase 2 (Phase 2)Jul 1, 2016Department of Veteran Affairs, Medical University of South Carolina, University of South Carolina
NCT02500602Phase 2Jun 1, 2016Consortium to Alleviate PTSD, Department of Veteran Affairs, Medical University of South Carolina
NCT02563405Phase 2/Phase 3 (Phase 3)Sep 1, 2015Harbin Medical University
NCT02538744Phase 1Aug 1, 2015Baylor University
NCT01953432Phase 2Apr 1, 2014Baylor University, Department of Veteran Affairs
NCT01959022Phase 4Oct 1, 2013Department of Defense, Department of Veteran Affairs, Northern California Institute of Research and Education
NCT01946035Phase 4Sep 1, 2013University of Dundee
NCT01730846Phase 2Feb 1, 2013National Institute on Drug Abuse (NIDA), Yale University
NCT01678313Phase 2Aug 1, 2012Tzu Chi University
NCT01661621Phase 4Aug 1, 2012Tzu Chi University
NCT02308202Phase 1Jan 1, 2012Baylor University
NCT01379898Phase 4Dec 1, 2011Atrium 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
Showing 20 of 52 trials
Page 1 / 3

Organizations

Research & Development (92)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Baylor UniversityAcademic/Hospital9631995
National Institute on Drug Abuse (NIDA)Government6022009
Department of Veteran AffairsGovernment5422013
National Heart, Lung, and Blood Institute (NHLBI)Government3131985
PfizerFor profit3322003
Sungkyunkwan UniversityAcademic/Hospital3322007
Brown UniversityAcademic/Hospital2212011
Department of DefenseGovernment2022013
Medical University of South CarolinaAcademic/Hospital2012016
National Institute on Alcohol Abuse and Alcoholism (NIAAA)Government2012011
Northern California Institute of Research and EducationAcademic/Hospital2022013
The University of Texas, DallasAcademic/Hospital2011993
Tzu Chi UniversityAcademic/Hospital2222012
University of ColoradoAcademic/Hospital2021995
University of VigoAcademic/Hospital2212000
Yale UniversityAcademic/Hospital2121995
Aarhus UniversityAcademic/Hospital1112007
AstraZenecaFor profit1012000
Atrium Medical CenterAcademic/Hospital1012011
Boehringer IngelheimFor profit1112005
92 organizations
Page 1 / 5

Marketing (31)

OrganizationOrg typeRelationshipDate
Accord ResearchFor profitMKTGJun 11, 2014
ActavisFor profitMKTGOct 18, 2000
Ani PharmaceuticalsFor profitMKTGOct 18, 2000
Ani PharmaceuticalsFor profitSYNOct 18, 2000
ApotexFor profitMKTGOct 18, 2000
Appco PharmaFor profitMKTGApr 17, 2018
Aurobindo PharmaFor profitMKTGOct 19, 2000
Chartwell PharmaceuticalsFor profitMKTGOct 18, 2000
DAVA PharmaceuticalsFor profitMKTGJun 10, 2004
EmcureFor profitMKTGFeb 13, 2018
FosunFor profitMKTGOct 18, 2000
GenpharmFor profitMKTGOct 18, 2000
Heritage PharmaFor profitMKTGFeb 13, 2018
MedarexFor profitMKTGOct 18, 2000
MylanFor profitMKTGOct 19, 2000
MylanFor profitSYNMar 15, 2022
Nesher PharmsFor profitMKTGOct 18, 2000
PfizerFor profitNDANov 2, 1990
PharmgenFor profitMKTGMar 15, 2022
PlivaFor profitMKTGJun 8, 2001
Rising PharmaceuticalsFor profitMKTGMar 15, 2022
Strides Pharma ScienceFor profitMKTGJun 10, 2004
TevaFor profitMKTGOct 18, 2000
TevaFor profitSYNOct 18, 2000
UnichemFor profitMKTGJan 10, 2024
UpjohnFor profitMKTGNov 2, 1990
Upsher-Smith LaboratoriesFor profitMKTGApr 17, 2018
ViatrisFor profitMKTGNov 2, 1990
ViatrisFor profitNDA2Nov 2, 1990
Watson PharmaceuticalsFor profitMKTGOct 18, 2000
Zydus Discovery DMCCFor profitMKTGJul 7, 2017