lorcaserin

Trade name: belviq

Small moleculeapproved

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

Phase 1
24
Phase 2
19
Phase 3
8
Phase 4
8

Earliest trial started Dec 1, 2004 (NCT00104507)

Timeline

2000s

  1. Jan 1, 2004

    Arena Pharmaceuticals — Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2006

    Arena Pharmaceuticals — Earliest Phase 3 Sponsor(trial)

  3. Jan 1, 2008

    Arena Pharmaceuticals — Earliest Phase 1 Sponsor(trial)

2010s

  1. Jun 27, 2012

    Arena Pharmaceuticals — Earliest FDA Approval

  2. Jun 27, 2012

    Arena Pharmaceuticals — NDA Organization

  3. Jun 27, 2012

    Eisai — NDA Secondary Org

  4. Jul 15, 2016

    Sarepta Therapeutics — NDA Secondary Org

  5. Dec 2, 2019

    Zydus Discovery DMCC — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedJun 27, 2012

Chemistry & pharmacology

Loading structure…

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

First in class

Sources

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 IDPhaseStart dateSponsor(s)
NCT04572243Phase 3Sep 23, 2020Eisai
NCT04205071Phase 1Jan 31, 2020National Cancer Institute (NCI), Ohio State University
NCT04396834Phase 2Dec 4, 2019The Mind Research Network
NCT04396847Phase 2Oct 25, 2019The Mind Research Network
NCT03812523Phase 2Jun 30, 2019Southeastern Regional Medical Center
NCT03799198Phase 4Jan 7, 2019Novo Nordisk
NCT03720574Phase 3Dec 6, 2018Jiangsu Kanion Pharmaceutical Co., Ltd, Peking University
NCT03637842Early Phase 1 (Phase 1)Oct 1, 2018Columbia University, National Institute on Drug Abuse (NIDA)
NCT03266939Phase 1Sep 30, 2018Mclean Hospital
NCT03627936Phase 1Aug 7, 2018Eisai
NCT03353220Phase 4Jan 3, 2018Columbia University, National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)
NCT03011645Phase 1Jan 1, 2018Duke University, National Heart, Lung, and Blood Institute (NHLBI)
NCT03338296Phase 4Sep 28, 2017Eisai
NCT03253926Phase 1/Phase 2 (Phase 2)Sep 5, 2017Columbia University, National Institute on Drug Abuse (NIDA)
NCT03192995Phase 2Aug 1, 2017National Institute on Drug Abuse (NIDA), University of California, San Francisco
NCT03007394Phase 2Jun 1, 2017National Institute on Drug Abuse (NIDA)
NCT03169816Phase 2/Phase 3 (Phase 3)May 25, 2017Columbia University
NCT03143855Phase 1Jan 30, 2017National Institute on Drug Abuse (NIDA), Virginia Commonwealth University
NCT02906644Phase 2Nov 8, 2016Duke University, National Institute on Drug Abuse (NIDA)
NCT02932215Phase 1Oct 1, 2016Columbia University
Showing 20 of 51 trials
Page 1 / 3

Organizations

Research & Development (30)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Arena PharmaceuticalsFor profit131332004
EisaiFor profit9842013
National Institute on Drug Abuse (NIDA)Government9232015
Columbia UniversityAcademic/Hospital6542016
University of VermontAcademic/Hospital4022006
Mayo ClinicAcademic/Hospital3322013
Virginia Commonwealth UniversityAcademic/Hospital3312015
Duke UniversityAcademic/Hospital2222016
National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)Government2012016
The Mind Research NetworkAcademic/Hospital2212019
Department of Veteran AffairsGovernment1112014
Georgetown UniversityAcademic/Hospital1012006
Harvard UniversityAcademic/Hospital1112014
IlDong Pharmaceutical Co LtdFor profit1112013
Jiangsu Kanion Pharmaceutical Co., LtdFor profit1112018
Johns Hopkins UniversityAcademic/Hospital1112015
Mclean HospitalAcademic/Hospital1112018
Midwest Biomedical Research FoundationAcademic/Hospital1112015
National Cancer Institute (NCI)Government1012020
National Heart, Lung, and Blood Institute (NHLBI)Government1012018
30 organizations
Page 1 / 2

Marketing (4)

OrganizationOrg typeRelationshipDate
Arena PharmaceuticalsFor profitNDAJun 27, 2012
EisaiFor profitNDA2Jun 27, 2012
Sarepta TherapeuticsFor profitNDA2Jul 15, 2016
Zydus Discovery DMCCFor profitMKTGDec 2, 2019