Lorcaserin

Summary

Lorcaserin (CHEMBL360328) is an approved small-molecule appetite depressant (ATC A08AA11) targeting HTR2A, HTR2B, and HTR2C; indicated across 11 conditions including obesity disorder and cocaine dependence.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A08AA11
• Targets: 3 (HTR2A, HTR2B, HTR2C)
• Indications: 11 conditions
• Clinical trials: 34
• Chemistry: 195.69 Da · C11H14ClN

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL360328
Name	Lorcaserin
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	11658860
ChEBI	CHEBI:65353
ATC	A08AA11
Molecular formula	C11H14ClN
Molecular weight	195.69
InChIKey	XTTZERNUQAFMOF-QMMMGPOBSA-N

SMILES: C[C@H]1CNCCC2=C1C=C(C=C2)Cl

IUPAC name: (5R)-7-chloro-5-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine

ChEBI definition: A benzazepine that is 2,3,4,5-tetrahydro-3-benzazepine substituted at position 1 by a methyl group and a t position 6 by a chloro group.

Pharmacological roles (ChEBI): appetite depressant, anti-obesity agent.

Also known as: ADP-356, ADP356, Lorcaserin, Lorcaserina, Lorcaserine, lorcaserin, SID170466882, SID144206569, LORCASERIN, Locarserin, Lorcaserin; Belviq

Parent form; salt/anhydrous children: CHEMBL2095211, CHEMBL3527027

Patent coverage: 790 distinct patent families (2,132 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,620 (76%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
HTR2A	5-HT2A receptor	Full agonist	6.8	0%	P28223
HTR2B	5-HT2B receptor	Full agonist	6	0.4%	P41595
HTR2C	5-HT2C receptor	Agonist	8.24	0%	P28335

Broader ChEMBL bioactivity targets: 15 (assay-derived). Sample: 5-hydroxytryptamine receptor 2C, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, Serotonin 2 receptors; 5-HT2a & 5-HT2c, Beta-1 adrenergic receptor, 5-hydroxytryptamine receptor 1A, Cannabinoid receptor 1, Sodium-dependent noradrenaline transporter.

Bioactivity

ChEMBL activities: 80 potent at pChembl ≥ 5 of 84 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HTR2A	8.89	Ki	1.3	nM	CHEMBL_ACT_12688743
HTR2B	8.89	Ki	1.3	nM	CHEMBL_ACT_12688746
HTR2C	8.74	EC50	1.82	nM	CHEMBL_ACT_16484024
HTR2C	8.68	EC50	2.1	nM	CHEMBL_ACT_18063621
HTR2C	8.58	EC50	2.63	nM	CHEMBL_ACT_18063682
HTR2C	8.58	EC50	2.63	nM	CHEMBL_ACT_22450768
HTR2C	8.58	EC50	2.64	nM	CHEMBL_ACT_22450769
HTR2C	8.57	EC50	2.7	nM	CHEMBL_ACT_16482379
HTR2C	8.57	EC50	2.7	nM	CHEMBL_ACT_2283282
HTR2C	8.47	EC50	3.4	nM	CHEMBL_ACT_22451261
HTR2C	8.46	EC50	3.47	nM	CHEMBL_ACT_22451260
HTR2C	8.44	EC50	3.6	nM	CHEMBL_ACT_15225453
HTR2C	8.32	EC50	4.79	nM	CHEMBL_ACT_19077839
HTR2C	8.32	EC50	4.77	nM	CHEMBL_ACT_19077941
HTR2A	8.12	Ki	7.5	nM	CHEMBL_ACT_19121009
HTR2C	8.12	EC50	7.6	nM	CHEMBL_ACT_20656878
HTR2C	8.1	EC50	7.94	nM	CHEMBL_ACT_2065698
HTR2C	8.05	EC50	9	nM	CHEMBL_ACT_12688749
HTR2C	8.05	EC50	9	nM	CHEMBL_ACT_6179752
HTR2C	7.96	EC50	11	nM	CHEMBL_ACT_1423380
HTR2C	7.82	Ki	15	nM	CHEMBL_ACT_13515548
HTR2C	7.82	Ki	15	nM	CHEMBL_ACT_18862364
HTR2C	7.82	Ki	15	nM	CHEMBL_ACT_19121010
HTR2C	7.82	Ki	15	nM	CHEMBL_ACT_20656875
HTR2C	7.82	Ki	15	nM	CHEMBL_ACT_29316873
HTR2C	7.82	Ki	15	nM	CHEMBL_ACT_6179754
Q60F97	7.79	EC50	16.2	nM	CHEMBL_ACT_6179755
HTR2A	7.49	EC50	32.36	nM	CHEMBL_ACT_19077907
HTR2A	7.48	EC50	33	nM	CHEMBL_ACT_19077967
HTR2C	7.4	EC50	39.81	nM	CHEMBL_ACT_18063723

Target pathways

Aggregated over 3 target gene(s): HTR2A, HTR2B, HTR2C.

Top Reactome pathways

8 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	3	HTR2A, HTR2B, HTR2C
Signaling by GPCR	3	HTR2A, HTR2B, HTR2C
Class A/1 (Rhodopsin-like receptors)	3	HTR2A, HTR2B, HTR2C
Amine ligand-binding receptors	3	HTR2A, HTR2B, HTR2C
GPCR downstream signalling	3	HTR2A, HTR2B, HTR2C
Serotonin receptors	3	HTR2A, HTR2B, HTR2C
G alpha (q) signalling events	3	HTR2A, HTR2B, HTR2C
GPCR ligand binding	3	HTR2A, HTR2B, HTR2C

Dominant GO biological processes

GO term	Targets
intracellular calcium ion homeostasis	3
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	3
phospholipase C-activating serotonin receptor signaling pathway	3
serotonin receptor signaling pathway	3
chemical synaptic transmission	3
positive regulation of phosphatidylinositol biosynthetic process	3
release of sequestered calcium ion into cytosol	3
positive regulation of ERK1 and ERK2 cascade	3
G protein-coupled serotonin receptor signaling pathway	3
signal transduction	3
G protein-coupled receptor signaling pathway	3
positive regulation of cell population proliferation	2
response to xenobiotic stimulus	2
positive regulation of fat cell differentiation	2
obsolete cGMP-mediated signaling	2

Indications & clinical

Indications

11 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
obesity disorder	4	MONDO:0011122	EFO:0001073
cocaine dependence	2	MONDO:0005186	EFO:0002610
nicotine dependence	2	MONDO:0008575	EFO:0003768
opiate dependence	2	MONDO:0005530	EFO:0005611
peripheral neuropathy	2	MONDO:0005244	EFO:0003100
cardiovascular disorder	1	MONDO:0004995	EFO:0000319
liver disorder	1	MONDO:0005154	EFO:0001421
drug dependence	1	MONDO:0005303	EFO:0003890
cannabis dependence	1	MONDO:0005689	EFO:0007191
kidney disorder	1	MONDO:0005240	EFO:0003086

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 34.

Phase distribution

Phase	Trials
PHASE1	12
PHASE2	6
PHASE4	4
PHASE1/PHASE2	4
Not specified	3
PHASE3	2
PHASE2/PHASE3	2
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01962402	PHASE4	UNKNOWN	Lorcaserin for Weight Loss Management in Patients on Antipsychotics: A Pilot Study
NCT01987427	PHASE4	COMPLETED	A Multicenter, Double-blind, Randomized, Parallel-group, Pilot Study of 12-week Duration to Assess the Short-term Safety and Tolerability of Lorcaserin Plus Two Doses of Immediate-Release Phentermine-HCl Compared With Lorcaserin Alone in Overweight and Obese Adults
NCT02796144	PHASE4	TERMINATED	MEtformin and Lorcaserin for WeighT Loss in Schizophrenia
NCT03338296	PHASE4	TERMINATED	Study to Evaluate the Efficacy and Safety of Belviq XR® in Conjunction With Lifestyle Modification for Weight Loss in Obese Adolescents, Age 12 to 17 Years
NCT02129608	PHASE3	COMPLETED	Low Level Laser Treatment (LLLT) and Lorcaserin for Weight Management
NCT02412631	PHASE2/PHASE3	TERMINATED	Addressing Post Cessation Weight Gain
NCT03169816	PHASE2/PHASE3	COMPLETED	Lorcaserin in Combination With XR-Naltrexone for Relapse Prevention in Opioid Use Disorder
NCT04572243	PHASE3	TERMINATED	A Study of Lorcaserin as Adjunctive Treatment in Participants With Dravet Syndrome
NCT02393547	PHASE1/PHASE2	COMPLETED	Lorcaserin for Preventing Weight Gain Among Smokers
NCT02523690	PHASE1/PHASE2	TERMINATED	Evaluating Muscle Weakness Improvement With Lorcaserin in ICU
NCT02680288	PHASE1/PHASE2	UNKNOWN	Lorcaserin Intra Venous Cocaine Effects
NCT02906644	PHASE2	COMPLETED	Combination Nicotine Patch / Lorcaserin for Smoking Cessation
NCT03007394	PHASE2	COMPLETED	Lorcaserin in the Treatment of Cocaine Use Disorder
NCT03192995	PHASE2	TERMINATED	Treatment With Lorcaserin for Cocaine Use: The TLC Study
NCT03253926	PHASE1/PHASE2	COMPLETED	Effect of Lorcaserin on Cannabis Withdrawal and Self-administration
NCT03812523	PHASE2	UNKNOWN	Comparing Lorcaserin Versus Duloxetine for the Treatment of Chemotherapy-Induced Peripheral Neuropathy
NCT04396834	PHASE2	TERMINATED	Mechanisms of Lorcaserin for Smoking Cessation
NCT04396847	PHASE2	TERMINATED	Laboratory Screening of Lorcaserin for Alcohol Use Disorder
NCT00828438	PHASE1	COMPLETED	Pharmacokinetic Properties of Lorcaserin in Subjects With Renal Impairment
NCT00828581	PHASE1	COMPLETED	Pharmacokinetic Properties of Lorcaserin in Obese or Overweight Elderly Subjects
NCT00828724	PHASE1	COMPLETED	Pharmacokinetic Properties of Lorcaserin in the Fed and Fasted State
NCT00828932	PHASE1	COMPLETED	Pharmacokinetic Properties of Lorcaserin in Subjects With Hepatic Impairment
NCT02022956	PHASE1	COMPLETED	Single Dose Study to Determine the Safety, Tolerability, and Pharmacokinetic Properties of Lorcaserin Hydrochloride (BELVIQ) in Obese Adolescents From 12 to 17 Years of Age
NCT02393599	PHASE1	COMPLETED	Study to Assess Potential Interactions Between Intravenous Cocaine and Oral Lorcaserin
NCT02537873	PHASE1	COMPLETED	Drug Interaction and Self Administration Studies of Compounds for Cocaine Use Disorder
NCT02932215	PHASE1	COMPLETED	Use of a Mobile Health Sensor in an Open Label Trial of Lorcaserin for the Treatment of Cannabis Use Disorder
NCT03011645	PHASE1	TERMINATED	Gene-by-Stress Interactions in Intervention Studies Significance
NCT03143855	PHASE1	COMPLETED	Drug Interaction and Subjective Effects of Compounds for Opioid Use Disorder
NCT03266939	PHASE1	WITHDRAWN	Rebalancing the Serotonergic System in Cocaine Dependence
NCT04205071	PHASE1	WITHDRAWN	Lorcaserin in Treating Chemotherapy-Induced Peripheral Neuropathy in Patients With Stage I-IV Gastrointestinal or Breast Cancer
NCT03637842	EARLY_PHASE1	TERMINATED	Lorcaserin for Cannabis Use Disorder
NCT04457687	Not specified	AVAILABLE	Extended Access Program With Lorcaserin For The Treatment of Dravet Syndrome and Other Refractory Epilepsies
NCT02388568	Not specified	COMPLETED	Lifestyle Modification and Lorcaserin for Weight Loss Maintenance
NCT03552107	Not specified	COMPLETED	Lorcaserin: Real World Experience in an Insurance-Based Weight Management Clinic

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

562 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
FIDAXOMICIN	ChEMBL + PubChem	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
PIMAVANSERIN	ChEMBL + PubChem	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
PROPOXYPHENE	ChEMBL + PubChem	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
ALOSETRON	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
AMIODARONE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
AMLODIPINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
AMOXAPINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
APOMORPHINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
ASENAPINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
ATOMOXETINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
AZATADINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
AZELASTINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
BENFLUOREX	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
BENPERIDOL	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
BENZQUINAMIDE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
BENZTROPINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
BUSPIRONE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CANNABIDIOL	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CARIPRAZINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CARVEDILOL	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CINACALCET	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CISAPRIDE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CITALOPRAM	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CLEMASTINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CLOZAPINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CYCLIZINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CYCLOBENZAPRINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DAPIPRAZOLE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DASATINIB	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DESIPRAMINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DESLORATADINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DICYCLOMINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DIMENHYDRINATE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DIPHENHYDRAMINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DOMPERIDONE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DOTHIEPIN	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DOXAZOSIN	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DOXEPIN	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DROPERIDOL	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
DULOXETINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
EBASTINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
ECONAZOLE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
ENCAINIDE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
ERGOTAMINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
FLUOXETINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
FLUSPIRILENE	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C
GUANABENZ	ChEMBL	Phase 4 (approved)	HTR2A, HTR2B, HTR2C