betaxolol
Trade name: kerlone
Approved
Aug 30, 1985
Betaxolol or SL 75212, (± )-1-(isopropylamino)-3-(p-(cyclopropylmethoxyethyl-phenoxy)2-propranol, is a potent cardioselective beta1-adrenoceptor antagonist devoid of intrinsic sympathomimetic activity with very weak local anaesthetic properties. Oral betaxolol has been used for the treatment of essential hypertension. Betaxolol is used topically in glaucoma and ocular hypertension. — NCATS
Clinical trial activity
4 trials · 9 clinical orgs · 15 marketing orgs
Earliest trial started Oct 1, 1992 (NCT00000132)
Timeline
1980s
- Aug 30, 1985
Earliest FDA Approval
- Aug 30, 1985
Sandoz — NDA Secondary Org
- Aug 30, 1985
Sandoz — Marketing Organization
- Oct 27, 1989
Sanofi-Aventis — NDA Secondary Org
- Dec 29, 1989
Novartis — NDA Secondary Org
- Dec 29, 1989
Novartis — Marketing Organization
1990s
- Jan 1, 1992
Earliest Phase 3 Sponsor(trial)
- Apr 17, 1997
Alcon — Marketing Organization
- Apr 17, 1997
Nestle — NDA Secondary Org
- Oct 22, 1999
Epic Pharma Llc — Marketing Organization
2000s
- Jun 30, 2000
Akorn, Inc. — Marketing Organization
- Jun 30, 2000
Sciegen Pharmaceticals — Marketing Organization
- Jun 30, 2000
PHARMOBEDIENT — Marketing Organization
- Sep 28, 2000
Apotex — Marketing Organization
- Apr 12, 2001
Medimetriks — Marketing Organization
- Jun 27, 2008
Kvk Tech Inc — Marketing Organization
- Nov 16, 2009
Wockhardt — Marketing Organization
- Nov 16, 2009
Acella Pharmaceuticals — Marketing Organization
- Nov 16, 2009
Chartwell Pharmaceuticals — Marketing Organization
2010s
- Jan 1, 2011
Earliest Phase 1 Sponsor(trial)
Indications
Mechanism of action
- Beta-1 adrenergic receptorANTAGONIST
ADRB1 antagonist
Selective
Combination products
betoptic pilo
with pilocarpine
kerledex
with chlorthalidone
Approval history
- approvedPriority reviewAug 30, 1985
Chemistry & pharmacology
SMILES
CC(C)NCC(O)COc1ccc(CCOCC2CC2)cc1- Mol. weight
- 307.43 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral, Topical
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
Yes
Sources
- ChEMBLCHEMBL423 ↗
- WikipediaBetaxolol ↗
- NCATSO0ZR1R6RZ2 ↗
- ChEMBLCHEMBL1691 ↗
Also known as
- 1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl)amino)-2-propanol
- 1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl)amino)-2-propanol
- 1-(isopropylamino)-3-[p-(cyclopropylmethoxyethyl)phenoxy]-2-propanol
- 1-(isopropylamino)-3-[p-(cyclopropylmethoxyethyl)phenoxy]-2-propanol
- alo-1401-02
- alo-1401-02
- betaxolol
- betaxolol
- betaxolol
- betaxolol
- betaxolol
- betaxolol
- betaxolol
- betaxolol
- betaxolol
- betaxolol
- (+/-)-betaxolol
- betaxolol hcl
- betaxolol hcl
- betaxolol hcl
- betaxolol hydrochloride
- betaxolol hydrochloride
- betaxolol hydrochloride
- betaxolol hydrochloride
- betaxololum
- betaxololum
- betoptic
- betoptic
- betoptic
- betoptic s
- betoptic s
- betoptic susp
- kerledex
- kerledex
- kerlone
- kerlone
- sl 75.212-10
- sl 75.212-10
- sl-75212-10
- sl-75212-10
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02617459 | Phase 3 | Nov 1, 2015 | Lee's Pharmaceutical, Xiamen University |
| NCT01660620 | Phase 1 | Apr 1, 2011 | Ohio State University, Smith-Kettlewell Eye Research Institute, University of Minnesota, University of Oklahoma, University of Texas at Houston |
| NCT00061542 | Phase 3 | Jan 1, 2003 | Alcon |
| NCT00000132 | Phase 3 | Oct 1, 1992 | National Eye Institute (NEI) |
Organizations
Research & Development (9)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Alcon | For profit | 1 | 1 | 1 | 2003 |
| Lee's Pharmaceutical | For profit | 1 | 1 | 1 | 2015 |
| National Eye Institute (NEI) | Government | 1 | 1 | 1 | 1992 |
| Ohio State University | Academic/Hospital | 1 | 0 | 1 | 2011 |
| Smith-Kettlewell Eye Research Institute | Academic/Hospital | 1 | 1 | 1 | 2011 |
| University of Minnesota | Academic/Hospital | 1 | 0 | 1 | 2011 |
| University of Oklahoma | Academic/Hospital | 1 | 0 | 1 | 2011 |
| University of Texas at Houston | Academic/Hospital | 1 | 0 | 1 | 2011 |
| Xiamen University | Academic/Hospital | 1 | 0 | 1 | 2015 |
Marketing (18)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Acella Pharmaceuticals | For profit | MKTG | Nov 16, 2009 |
| Akorn, Inc. | For profit | MKTG | Jun 30, 2000 |
| Alcon | For profit | NDA | — |
| Alcon | For profit | MKTG | Apr 17, 1997 |
| Apotex | For profit | MKTG | Sep 28, 2000 |
| Chartwell Pharmaceuticals | For profit | MKTG | Nov 16, 2009 |
| Epic Pharma Llc | For profit | MKTG | Oct 22, 1999 |
| Kvk Tech Inc | For profit | MKTG | Jun 27, 2008 |
| Medimetriks | For profit | MKTG | Apr 12, 2001 |
| Nestle | For profit | NDA2 | Apr 17, 1997 |
| Novartis | For profit | NDA2 | Dec 29, 1989 |
| Novartis | For profit | MKTG | Dec 29, 1989 |
| PHARMOBEDIENT | For profit | MKTG | Jun 30, 2000 |
| Sandoz | For profit | NDA2 | Aug 30, 1985 |
| Sandoz | For profit | MKTG | Aug 30, 1985 |
| Sanofi-Aventis | For profit | NDA2 | Oct 27, 1989 |
| Sciegen Pharmaceticals | For profit | MKTG | Jun 30, 2000 |
| Wockhardt | For profit | MKTG | Nov 16, 2009 |