lorcaserin
Trade name: belviq
Approved
Jun 27, 2012
Lorcaserin, currently marketed under the trade name Belviq and previously Lorqess during development, is a weight-loss drug developed by Arena Pharmaceuticals. Lorcaserin is a selective 5-HT2C receptor agonist, and in vitro testing of the drug showed reasonable selectivity for 5-HT2C over other related targets. 5-HT2C receptors are located almost exclusively in the brain, and can be found in the choroid plexus, cortex, hippocampus, cerebellum, amygdala, thalamus, and hypothalamus. The activation of 5-HT2C receptors in the hypothalamus is supposed to activate proopiomelanocortin (POMC) production and consequently promote weight loss through satiety. This hypothesis is supported by clinical trials and other studies. While it is generally thought that 5-HT2C receptors help to regulate appetite as well as mood, and endocrine secretion, the exact mechanism of appetite regulation is not yet known. Lorcaserin has shown 100x selectivity for 5-HT2C versus the closely related 5-HT2B receptor, and 17x selectivity over the 5-HT2A receptor — NCATS
Clinical trial activity
51 trials · 30 clinical orgs · 4 marketing orgs
Earliest trial started Dec 1, 2004 (NCT00104507)
Timeline
2000s
- Jan 1, 2004
Arena Pharmaceuticals — Earliest Phase 2 Sponsor(trial)
- Jan 1, 2006
Arena Pharmaceuticals — Earliest Phase 3 Sponsor(trial)
- Jan 1, 2008
Arena Pharmaceuticals — Earliest Phase 1 Sponsor(trial)
2010s
- Jun 27, 2012
Arena Pharmaceuticals — Earliest FDA Approval
- Jun 27, 2012
Arena Pharmaceuticals — NDA Organization
- Jun 27, 2012
Eisai — NDA Secondary Org
- Jul 15, 2016
Sarepta Therapeutics — NDA Secondary Org
- Dec 2, 2019
Zydus Discovery DMCC — Marketing Organization
Indications
Approved for
Studied for
- Alcoholism · Phase 2
- Analgesics, Opioid · Phase 1
- Body Weight · Phase 4
- Breast Neoplasms · Phase 1
- Cannabis · Phase 1/Phase 2
- Cardiovascular Diseases · Phase 4
- Cocaine-Related Disorders · Phase 2
- Diabetes Mellitus, Type 2 · Phase 4
- Digestive System Neoplasms · Phase 1
- Drug-Related Side Effects and Adverse Reactions · Phase 2
- Epilepsies, Myoclonic · Phase 3
- Healthy Volunteers · Phase 1
- Kidney Failure, Chronic · Phase 1
- Liver Diseases · Phase 1
- Muscle Weakness · Phase 1/Phase 2
- Opioid-Related Disorders · Phase 2/Phase 3
- Overweight · Phase 4
- Psychotic Disorders · Phase 4
- Schizophrenia · Phase 4
- Sepsis · Phase 1/Phase 2
- Smoking Cessation · Phase 2/Phase 3
- Substance-Related Disorders · Phase 1
- Tobacco Smoking · Phase 2
- Tobacco Use Disorder · Phase 2
- Weight Gain · Phase 4
- Weight Loss · Phase 4
Mechanism of action
HTR2C agonist
Approval history
- approvedJun 27, 2012
Chemistry & pharmacology
SMILES
C[C@H]1CNCCc2ccc(Cl)cc21- Mol. weight
- 195.69 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- Yes
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL360328 ↗
- WikipediaLorcaserin ↗
- NCATS637E494O0Z ↗
- ChEMBLCHEMBL2095211 ↗
Also known as
- (1r)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine
- 8-chloro-2,3,4,5-tetrahydro-1-methyl-1h-3-benzazepine
- apd356
- apd356
- apd356
- apd356
- apd 356
- apd 356
- apd-356
- apd-356
- apd-356
- apd-356
- ar-10a
- belviq
- belviq
- belviq
- belviq
- belviq
- belviq
- lorcaserin
- lorcaserin
- lorcaserin
- lorcaserin
- lorcaserin
- lorcaserin
- lorcaserin
- lorcaserin
- lorcaserin
- lorcaserin hcl
- lorcaserin hcl
- lorcaserin hcl
- lorcaserin hydrochloride
- lorcaserin hydrochloride
- lorcaserin hydrochloride
- lorcaserin hydrochloride
- lorcaserin hydrochloride hemihydrate
- lorcaserin hydrochloride hemihydrate
- lorcaserin hydrochloride hemihydrate
- lorcaserin hydrochloride hemihydrate
- lorcaserin hydrochloride hemihydrate
- lorqess
- lorqess
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04572243 | Phase 3 | Sep 23, 2020 | Eisai |
| NCT04205071 | Phase 1 | Jan 31, 2020 | National Cancer Institute (NCI), Ohio State University |
| NCT04396834 | Phase 2 | Dec 4, 2019 | The Mind Research Network |
| NCT04396847 | Phase 2 | Oct 25, 2019 | The Mind Research Network |
| NCT03812523 | Phase 2 | Jun 30, 2019 | Southeastern Regional Medical Center |
| NCT03799198 | Phase 4 | Jan 7, 2019 | Novo Nordisk |
| NCT03720574 | Phase 3 | Dec 6, 2018 | Jiangsu Kanion Pharmaceutical Co., Ltd, Peking University |
| NCT03637842 | Early Phase 1 (Phase 1) | Oct 1, 2018 | Columbia University, National Institute on Drug Abuse (NIDA) |
| NCT03266939 | Phase 1 | Sep 30, 2018 | Mclean Hospital |
| NCT03627936 | Phase 1 | Aug 7, 2018 | Eisai |
| NCT03353220 | Phase 4 | Jan 3, 2018 | Columbia University, National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) |
| NCT03011645 | Phase 1 | Jan 1, 2018 | Duke University, National Heart, Lung, and Blood Institute (NHLBI) |
| NCT03338296 | Phase 4 | Sep 28, 2017 | Eisai |
| NCT03253926 | Phase 1/Phase 2 (Phase 2) | Sep 5, 2017 | Columbia University, National Institute on Drug Abuse (NIDA) |
| NCT03192995 | Phase 2 | Aug 1, 2017 | National Institute on Drug Abuse (NIDA), University of California, San Francisco |
| NCT03007394 | Phase 2 | Jun 1, 2017 | National Institute on Drug Abuse (NIDA) |
| NCT03169816 | Phase 2/Phase 3 (Phase 3) | May 25, 2017 | Columbia University |
| NCT03143855 | Phase 1 | Jan 30, 2017 | National Institute on Drug Abuse (NIDA), Virginia Commonwealth University |
| NCT02906644 | Phase 2 | Nov 8, 2016 | Duke University, National Institute on Drug Abuse (NIDA) |
| NCT02932215 | Phase 1 | Oct 1, 2016 | Columbia University |
Organizations
Research & Development (30)
Marketing (4)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Arena Pharmaceuticals | For profit | NDA | Jun 27, 2012 |
| Eisai | For profit | NDA2 | Jun 27, 2012 |
| Sarepta Therapeutics | For profit | NDA2 | Jul 15, 2016 |
| Zydus Discovery DMCC | For profit | MKTG | Dec 2, 2019 |