alosetron
Trade name: lotronex
Approved
Feb 9, 2000
Alosetron, marketed under the brand name Lotronex, is a 5-HT3 antagonist used for the management of severe diarrhea-predominant irritable bowel syndrome (IBS) in women only. Alosetron is a potent and selective 5-HT3 receptor antagonist. 5-HT3 receptors are nonselective cation channels that are extensively distributed on enteric neurons in the human gastrointestinal tract, as well as other peripheral and central locations. Activation of these channels and the resulting neuronal depolarization affect the regulation of visceral pain, colonic transit and gastrointestinal secretions, processes that relate to the pathophysiology of irritable bowel syndrome (IBS). 5-HT3 receptor antagonists such as alosetron inhibit activation of non-selective cation channels which results in the modulation of the enteric nervous system. Alosetron is used for the treating women with severe irritable bowel syndrome (IBS) accompanied by severe diarrhea (usually lasting for 6 months or more). It is only prescribed to women who do not respond to other medicines and is not to be used by women whose main IBS problem is constipation. — NCATS
Clinical trial activity
6 trials · 5 clinical orgs · 15 marketing orgs
Earliest trial started Jun 1, 2003 (NCT00067561)
Timeline
2000s
- Feb 9, 2000
Earliest FDA Approval
- Feb 9, 2000
Sebela Pharmaceuticals — NDA Secondary Org
- Feb 9, 2000
LEGACY PHARMA — Marketing Organization
- Feb 11, 2000
Glaxo Wellcome — First NDA Organization
- Feb 11, 2000
Glaxo Wellcome — NDA Organization
- Jan 1, 2003
Earliest Phase 2 Sponsor(trial)
- Jan 1, 2003
Earliest Phase 3 Sponsor(trial)
2010s
- May 4, 2015
West-Ward Pharmaceutical — Marketing Organization
- May 4, 2015
Hikma — Marketing Organization
- Dec 22, 2016
Amneal Pharmaceuticals — Marketing Organization
- Feb 23, 2018
Par Pharmaceuticals — Marketing Organization
- Feb 23, 2018
Bristol-Myers Squibb — Marketing Organization
- Feb 23, 2018
Endo Pharmaceuticals — Marketing Organization
- Feb 23, 2018
PH HEALTH — Marketing Organization
- Jan 14, 2019
Rising Pharmaceuticals — Marketing Organization
- Sep 16, 2019
Eywa Pharma — Marketing Organization
- Sep 16, 2019
HIBROW HLTHCARE — Marketing Organization
2020s
- Sep 9, 2020
MannKind Corp — Marketing Organization
- Sep 9, 2020
Mankind Pharma — Marketing Organization
Indications
Approved for
Mechanism of action
- Serotonin 3a (5-HT3a) receptorANTAGONIST
HTR3A antagonist
Approval history
- approvedPriority reviewFeb 9, 2000
Chemistry & pharmacology
SMILES
Cc1[nH]cnc1CN1CCc2c(c3ccccc3n2C)C1=O- Mol. weight
- 294.36 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- Yes
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL1110 ↗
- WikipediaAlosetron ↗
- NCATS13Z9HTH115 ↗
- ChEMBLCHEMBL628 ↗
- ChEMBLCHEMBL1200885 ↗
Also known as
- 2,3,4,5-tetrahydro-5-methyl-2-((5-methyl-1h-imidazol-4-yl)methyl)-1h-pyrido(4,3-b)indol-1-one
- 2,3,4,5-tetrahydro-5-methyl-2-((5-methyl-1h-imidazol-4-yl)methyl)-1h-pyrido(4,3-b)indol-1-one
- 2,3,4,5-tetrahydro-5-methyl-2-((5-methylimidazol-4-yl)methyl)-1h-pyrido(4,3-b)indol-1-one monohydrochloride
- alosetron
- alosetron
- alosetron
- alosetron
- alosetron
- alosetron
- alosetron
- alosetron
- alosetron
- alosetron
- alosetron
- alosetron hcl
- alosetron hcl
- alosetron hcl
- alosetron hydrochloride
- alosetron hydrochloride
- alosetron hydrochloride
- alosetron hydrochloride
- alosetron hydrochloride
- alosetron hydrochloride
- alosetron monohydrochloride
- alosetron monohydrochloride
- glaxosmithkline brand of alosetron hydrochloride
- gr68755
- gr68755
- gr 68755
- gr-68755c
- gr-68755c
- lotronex
- lotronex
- lotronex
- lotronex
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05583266 | Phase 4 | Nov 1, 2022 | Capital Medical University, Yiling Pharmaceutical Inc. |
| NCT05284448 | Phase 3 | Feb 1, 2022 | Ain Shams University, Al Azhar University |
| NCT00370032 | Phase 4 | Dec 1, 2006 | GlaxoSmithKline |
| NCT01855711 | Phase 2 | Sep 18, 2003 | GlaxoSmithKline |
| NCT00067457 | Phase 3 | Jun 1, 2003 | GlaxoSmithKline |
| NCT00067561 | Phase 3 | Jun 1, 2003 | GlaxoSmithKline |
Organizations
Research & Development (5)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| GlaxoSmithKline | For profit | 4 | 4 | 3 | 2003 |
| Ain Shams University | Academic/Hospital | 1 | 0 | 1 | 2022 |
| Al Azhar University | Academic/Hospital | 1 | 1 | 1 | 2022 |
| Capital Medical University | Academic/Hospital | 1 | 1 | 1 | 2022 |
| Yiling Pharmaceutical Inc. | For profit | 1 | 0 | 1 | 2022 |
Marketing (17)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Amneal Pharmaceuticals | For profit | MKTG | Dec 22, 2016 |
| Bristol-Myers Squibb | For profit | MKTG | Feb 23, 2018 |
| Endo Pharmaceuticals | For profit | MKTG | Feb 23, 2018 |
| Eywa Pharma | For profit | MKTG | Sep 16, 2019 |
| Glaxo Wellcome | For profit | NDA | Feb 11, 2000 |
| HIBROW HLTHCARE | For profit | MKTG | Sep 16, 2019 |
| Hikma | For profit | MKTG | May 4, 2015 |
| Hikma | For profit | SYN | May 4, 2015 |
| LEGACY PHARMA | For profit | MKTG | Feb 9, 2000 |
| Mankind Pharma | For profit | MKTG | Sep 9, 2020 |
| MannKind Corp | For profit | MKTG | Sep 9, 2020 |
| PH HEALTH | For profit | MKTG | Feb 23, 2018 |
| Par Pharmaceuticals | For profit | MKTG | Feb 23, 2018 |
| Rising Pharmaceuticals | For profit | MKTG | Jan 14, 2019 |
| Rising Pharmaceuticals | For profit | SYN | Jan 14, 2019 |
| Sebela Pharmaceuticals | For profit | NDA2 | Feb 9, 2000 |
| West-Ward Pharmaceutical | For profit | MKTG | May 4, 2015 |