terazosin
Trade name: hytrin
Approved
Aug 7, 1987
Terazosin (marketed as Hytrin or Zayasel) is a selective alpha1-antagonist used for treatment of symptoms of benign prostatic hyperplasia (BPH). It also acts to lower blood pressure, so it is a drug of choice for men with hypertension and prostate enlargement. All three receptor subtypes appear to be involved in maintaining vascular tone. The α1A-receptor maintains basal vascular tone while the α1B-receptor mediates the vasocontrictory effects of exogenous α1-agonists. Activation of α1-receptors activates Gq-proteins, which results in intracellular stimulation of phospholipases C, A2, and D. This results in mobilization of Ca2+ from intracellular stores, activation of mitogen-activated kinase and PI3 kinase pathways and subsequent vasoconstriction. — NCATS
Clinical trial activity
24 trials · 39 clinical orgs · 18 marketing orgs
Earliest trial started Aug 1, 1998 (NCT02244255)
Timeline
1990s
- Mar 30, 1998
Sandoz — Marketing Organization
- Mar 30, 1998
Apnar Pharma — Marketing Organization
- Mar 30, 1998
Senores Pharms — Marketing Organization
- Dec 31, 1998
Novartis — Marketing Organization
- Jan 1, 1999
Earliest Phase 3 Sponsor(trial)
2000s
- Feb 11, 2000
Mylan — Marketing Organization
- Feb 11, 2000
PHARMOBEDIENT — Marketing Organization
- Apr 21, 2000
Teva — Marketing Organization
- Apr 28, 2000
Chartwell Pharmaceuticals — Marketing Organization
- Jul 28, 2000
Beximco — Marketing Organization
- Jul 28, 2000
Bionpharma Inc — Marketing Organization
- Jan 30, 2001
Heritage Pharma — Marketing Organization
- Apr 12, 2001
Apotex — Marketing Organization
- Apr 12, 2001
Hikma — Marketing Organization
- Aug 22, 2002
Ranbaxy — Marketing Organization
- Dec 20, 2004
Jubilant Innovation Ltd. — Marketing Organization
2020s
- Jul 29, 2024
Novitium Pharma — Marketing Organization
- May 12, 2025
Ajanta Pharma Ltd — Marketing Organization
Indications
Studied for
- Amyotrophic Lateral Sclerosis · Early Phase 1
- Atherosclerosis · Phase 3
- Atrial Fibrillation · Phase 4
- Cardiovascular Diseases · Phase 3
- Carotid Stenosis · Phase 2
- Coronary Disease · Phase 3
- Diabetes Mellitus · Phase 3
- Diabetes Mellitus, Type 2 · Phase 4
- Directly Observed Therapy · Phase 4
- Ejaculation · Phase 1
- Gait Analysis · Phase 4
- Healthy Volunteers · Phase 1
- Hypercholesterolemia · Phase 3
- Hyperhidrosis · Phase 4
- Hypertension · Phase 4
- Lewy Body Disease · Phase 1/Phase 2
- Metabolic Diseases · Phase 4
- Parkinson Disease · Phase 4
- Parkinson Disease, Secondary · Phase 2
- Prostatic Hyperplasia · Phase 4
- REM Sleep Behavior Disorder · Phase 2
- Stents · Phase 3
- Urination Disorders · Phase 2/Phase 3
Mechanism of action
- Adrenergic receptor alpha-1ANTAGONIST
Adrenergic receptor alpha-1 antagonist
Approval history
- approvedAug 7, 1987
Chemistry & pharmacology
SMILES
COc1cc2nc(N3CCN(C(=O)C4CCCO4)CC3)nc(N)c2cc1OC.Cl.O.O- Mol. weight
- 459.93 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
- ChEMBLCHEMBL3989562 ↗
- WikipediaTerazosin ↗
- NCATS8L5014XET7 ↗
- ChEMBLCHEMBL611 ↗
- ChEMBLCHEMBL1256665 ↗
- ChEMBLCHEMBL1201091 ↗
Also known as
- 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-((tetrahydro-2-furanyl)carbonyl)piperazine
- 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-((tetrahydro-2-furanyl)carbonyl)piperazine
- a 45975
- abbott-45975
- abbott-45975
- adecur
- apo-terazosin
- benph
- deflox
- dysalfa
- flotrin
- heitrin
- hexal brand of terazosin hydrochloride
- hytrin
- hytrin
- hytrin
- hytrin
- hytrin
- hytrin bph
- hytrin bph
- hytrin bph
- hytrine
- magnurol
- novo-terazosin
- nu-terazosin
- pms-terazosin
- ratio-terazosin
- sutif
- tazusin
- terazoflo
- terazosin
- terazosin
- terazosin
- terazosin
- terazosin
- terazosin
- terazosin
- terazosin
- terazosin
- terazosin
- terazosina
- terazosina
- terazosina alter
- terazosina kern
- terazosina qualix
- terazosin azu
- terazosine
- terazosine
- terazosine
- terazosine
- térazosine
- térazosine
- terazosin hcl
- terazosin hcl
- terazosin hcl
- terazosin hexal
- terazosin hydrochloride
- terazosin hydrochloride
- terazosin hydrochloride
- terazosin hydrochloride anhydrous
- terazosin hydrochloride anhydrous
- terazosin hydrochloride hydrate
- terazosin hydrochloride hydrate
- terazosin hydrochloride hydrate
- terazosin, monohydrochloride, dihydrate
- terazosinum
- terazosinum
- zayasel
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07288450 | Phase 1/Phase 2 (Phase 2) | Sep 1, 2026 | University of Iowa |
| NCT07224269 | Early Phase 1 (Phase 1) | Nov 17, 2025 | University of Iowa |
| NCT07207057 | Phase 3 | Sep 12, 2025 | Cure Parkinson's Trust, Medical Research Council, Michael J. Fox Foundation for Parkinson's Research, National Institute for Health Research, United Kingdom, Newcastle University, University of London, Van Andel Research Institute |
| NCT06966804 | Phase 3 | Jun 1, 2025 | Penang Medical College |
| NCT05855577 | Phase 4 | Dec 31, 2023 | I.R.C.C.S. Fondazione Santa Lucia |
| NCT05109364 | Phase 2 | Nov 1, 2021 | Cedars-Sinai Medical Center |
| NCT04760860 | Phase 1/Phase 2 (Phase 2) | Oct 31, 2021 | University of Iowa |
| NCT04551040 | Phase 1 | Nov 1, 2020 | Michael J. Fox Foundation for Parkinson's Research, University of Iowa |
| NCT04386317 | Phase 2 | Jul 1, 2020 | Cedars-Sinai Medical Center |
| NCT03905811 | Phase 1/Phase 2 (Phase 2) | May 31, 2019 | University of Iowa |
| NCT03195673 | Phase 2 | Mar 2, 2018 | Capital Medical University |
| NCT01508637 | N/A | Jan 1, 2012 | Environmental Protection Agency, National Institute of Environmental Health Sciences (NIEHS), University of Washington |
| NCT01530243 | Phase 2/Phase 3 (Phase 3) | Jan 1, 2012 | Urmia University of Medical Sciences |
| NCT02046395 | Phase 4 | Jan 1, 2012 | Tulane University |
| NCT01366664 | Phase 1 | Apr 1, 2011 | Johnson and Johnson |
| NCT00438113 | Phase 4 | Dec 1, 2009 | Dalhousie University, Government of Canada, Nova Scotia Health Research Foundation |
| NCT00687388 | Phase 4 | May 1, 2008 | Sungkyunkwan University, The Korean Urological Association |
| NCT00700583 | N/A | May 1, 2008 | Seoul National University |
| NCT00449683 | Phase 4 | Mar 1, 2007 | Brain & Behavior Research Foundation, Thomas Jefferson University |
| NCT00693199 | N/A | Jul 1, 2006 | Anhui Medical University, Peking University, University of Science and Technology of China |
Organizations
Research & Development (39)
Marketing (22)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Abbott | For profit | NDA | Aug 7, 1987 |
| Ajanta Pharma Ltd | For profit | MKTG | May 12, 2025 |
| Apnar Pharma | For profit | MKTG | Mar 30, 1998 |
| Apotex | For profit | MKTG | Apr 12, 2001 |
| Beximco | For profit | MKTG | Jul 28, 2000 |
| Bionpharma Inc | For profit | MKTG | Jul 28, 2000 |
| Chartwell Pharmaceuticals | For profit | MKTG | Apr 28, 2000 |
| Heritage Pharma | For profit | SYN | Jan 30, 2001 |
| Heritage Pharma | For profit | MKTG | Jan 30, 2001 |
| Hikma | For profit | MKTG | Apr 12, 2001 |
| Jubilant Innovation Ltd. | For profit | MKTG | Dec 20, 2004 |
| Mylan | For profit | MKTG | Feb 11, 2000 |
| Mylan | For profit | SYN | Dec 1, 2000 |
| Mylan | For profit | SYN | Feb 11, 2000 |
| Novartis | For profit | MKTG | Dec 31, 1998 |
| Novitium Pharma | For profit | MKTG | Jul 29, 2024 |
| PHARMOBEDIENT | For profit | MKTG | Feb 11, 2000 |
| Ranbaxy | For profit | MKTG | Aug 22, 2002 |
| Sandoz | For profit | MKTG | Mar 30, 1998 |
| Senores Pharms | For profit | MKTG | Mar 30, 1998 |
| Teva | For profit | MKTG | Apr 21, 2000 |
| Teva | For profit | SYN | May 18, 2000 |