bepotastine
Trade name: bepreve
Approved
Sep 8, 2009
Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor. It belongs to the second-generation piperidine chemical class. It is a mast cell stabilizer and suppresses the migration of eosinophils into inflamed tissues. Bepotastine was approved in Japan for use in the treatment of allergic rhinitis and uriticaria/puritus in July 2000 and January 2002, respectively, and is marketed by Tanabe Seiyaku Co., Ltd. under the brand name Talion. It is available in oral and opthalmic dosage forms in Japan. The opthalmic solution is FDA approved since Sept 8, 2009 and is under the brand name Bepreve. — NCATS
Clinical trial activity
33 trials · 26 clinical orgs · 9 marketing orgs
Earliest trial started Feb 1, 2007 (NCT00424398)
Timeline
2000s
- Jan 1, 2007
Bausch & Lomb — Earliest Phase 2 Sponsor(trial)
- Jan 1, 2007
Bausch & Lomb — Earliest Phase 3 Sponsor(trial)
- Sep 8, 2009
ISTA Pharmaceuticals — Earliest FDA Approval
- Sep 8, 2009
ISTA Pharmaceuticals — NDA Organization
- Sep 8, 2009
Bausch & Lomb — NDA Secondary Org
2010s
- Jan 1, 2010
Bausch & Lomb — Earliest Phase 1 Sponsor(trial)
- Jun 7, 2017
Sandoz — Marketing Organization
- Jun 7, 2017
Novartis — Marketing Organization
- Mar 5, 2019
Apotex — Marketing Organization
- Mar 18, 2019
Micro Labs Ltd India — Marketing Organization
- Mar 18, 2019
Mylan — Marketing Organization
2020s
- Apr 5, 2023
Alembic — Marketing Organization
- Aug 14, 2024
Somerset Pharmaceuticals — Marketing Organization
Indications
Studied for
- Allergy and Immunology · Phase 4
- Blood Transfusion · Phase 4
- Colorectal Neoplasms · Phase 2
- Cough · Phase 4
- Dermatitis · Phase 3
- Healthy Volunteers · Phase 1
- Hemorrhoids · Phase 4
- Lung Diseases · Phase 1
- Pruritus · Phase 3
- Rhinitis, Allergic · Phase 4
- Rhinitis, Allergic, Perennial · Phase 3
- Rhinitis, Allergic, Seasonal · Phase 2
- Safety · Phase 1
- Urticaria · Phase 1
- Vision, Ocular · Phase 1
Mechanism of action
- Histamine H1 receptorANTAGONIST
HRH1 antagonist
Approval history
- approvedSep 8, 2009
Chemistry & pharmacology
SMILES
O=C(O)CCCN1CCC(O[C@@H](c2ccc(Cl)cc2)c2ccccn2)CC1- Mol. weight
- 388.9 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Topical
- Availability
- Prescription Only
Oral
No
Parenteral
No
Topical
Yes
Sources
- ChEMBLCHEMBL1201758 ↗
- WikipediaBepotastine ↗
- NCATSHYD2U48IAS ↗
- ChEMBLCHEMBL1201759 ↗
Also known as
- bb
- bb
- bepotastine
- bepotastine
- bepotastine
- bepotastine
- bepotastine
- bepotastine
- bepotastine
- bepotastine
- bepotastine
- bepotastine
- bepotastine besilate
- bepotastine besilate
- bepotastine besilate
- bepotastine besilate
- bepotastine besilate
- bepotastine besylate
- bepotastine besylate
- bepotastine besylate
- bepotastine salicylate
- bepreve
- bepreve
- bepreve
- bepreve
- betotastine
- betotastine besilate
- (s)-4-(4-((4-chlorophenyl)(2-pyridil)methoxy)piperidino)butylic acid monobenzenesulfonate
- tau 284
- tau-284
- tau-284
- tau-284
- tau-284
- tau-284ds
- tau-284ds
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06705777 | Phase 4 | Sep 1, 2024 | Federal University of Rio de Janeiro, Fluminense Federal University, Fundação Educacional Serra dos Órgãos |
| NCT06299670 | Phase 4 | Nov 1, 2023 | Bangladesh Medical University |
| NCT04877678 | Phase 4 | Oct 31, 2021 | University of Ulsan |
| NCT04776096 | Phase 4 | Mar 10, 2021 | Laboratorios Poen |
| NCT04693429 | Phase 1 | Sep 24, 2020 | Laboratorios Sophia S.A de C.V. |
| NCT04097951 | Phase 1 | Nov 8, 2019 | Hyundai, Inha University |
| NCT03932435 | N/A | Apr 23, 2019 | Dong-A Pharmaceutical |
| NCT05414461 | Phase 2 | Mar 10, 2019 | Zhejiang University |
| NCT03200496 | Phase 1 | May 29, 2017 | Dong-A Pharmaceutical |
| NCT03317301 | Phase 3 | May 17, 2017 | Hanlim Pharm. Co., Ltd. |
| NCT03655210 | Phase 3 | Feb 7, 2017 | Hanlim Pharm. Co., Ltd. |
| NCT02686294 | Phase 1 | Feb 1, 2016 | Hanlim Pharm. Co., Ltd., Korea University |
| NCT02682745 | Phase 1 | Jan 1, 2016 | Hanlim Pharm. Co., Ltd. |
| NCT02332044 | Phase 1 | Apr 1, 2014 | Daewoong Pharmaceutical Co. LTD. |
| NCT01900054 | Phase 3 | Jun 1, 2013 | Mitsubishi Tanabe, Nippon Medical School |
| NCT01861522 | Phase 3 | Apr 1, 2013 | Mitsubishi Tanabe, Nippon Medical School |
| NCT01840605 | Phase 3 | Mar 1, 2013 | Mitsubishi Tanabe, Tokyo Women's Medical University |
| NCT01753739 | Phase 2 | Jan 1, 2013 | Bausch & Lomb |
| NCT01925313 | Phase 1 | Dec 1, 2012 | CJ HealthCare Corp., Yonsei University |
| NCT01578278 | Phase 2 | Dec 1, 2011 | Bausch & Lomb, ISTA Pharmaceuticals |
Organizations
Research & Development (26)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Bausch & Lomb | For profit | 10 | 8 | 3 | 2007 |
| ISTA Pharmaceuticals | For profit | 7 | 0 | 2 | 2007 |
| Hanlim Pharm. Co., Ltd. | For profit | 5 | 4 | 2 | 2011 |
| Mitsubishi Tanabe | For profit | 4 | 4 | 1 | 2011 |
| Nippon Medical School | Academic/Hospital | 3 | 0 | 1 | 2011 |
| Dong-A Pharmaceutical | For profit | 2 | 2 | 2 | 2017 |
| Korea University | Academic/Hospital | 2 | 1 | 1 | 2011 |
| Bangladesh Medical University | Academic/Hospital | 1 | 1 | 1 | 2023 |
| CJ HealthCare Corp. | For profit | 1 | 1 | 1 | 2012 |
| Daewoong Pharmaceutical Co. LTD. | For profit | 1 | 1 | 1 | 2014 |
| Federal University of Rio de Janeiro | Academic/Hospital | 1 | 0 | 1 | 2024 |
| Fluminense Federal University | Academic/Hospital | 1 | 0 | 1 | 2024 |
| Fundação Educacional Serra dos Órgãos | Academic/Hospital | 1 | 1 | 1 | 2024 |
| Hom, Milton M., OD, FAAO | Academic/Hospital | 1 | 1 | 1 | 2011 |
| Hyundai | For profit | 1 | 1 | 1 | 2019 |
| Inha University | Academic/Hospital | 1 | 0 | 1 | 2019 |
| Laboratorios Poen | For profit | 1 | 1 | 1 | 2021 |
| Laboratorios Sophia S.A de C.V. | For profit | 1 | 1 | 1 | 2020 |
| McCabe Vision Center | Academic/Hospital | 1 | 1 | 1 | 2011 |
| Minnesota Eye Consultants | Academic/Hospital | 1 | 1 | 1 | 2011 |
Marketing (10)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Alembic | For profit | MKTG | Apr 5, 2023 |
| Apotex | For profit | SYN | Mar 5, 2019 |
| Apotex | For profit | MKTG | Mar 5, 2019 |
| Bausch & Lomb | For profit | NDA2 | Sep 8, 2009 |
| ISTA Pharmaceuticals | For profit | NDA | Sep 8, 2009 |
| Micro Labs Ltd India | For profit | MKTG | Mar 18, 2019 |
| Mylan | For profit | MKTG | Mar 18, 2019 |
| Novartis | For profit | MKTG | Jun 7, 2017 |
| Sandoz | For profit | MKTG | Jun 7, 2017 |
| Somerset Pharmaceuticals | For profit | MKTG | Aug 14, 2024 |