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Identification
NameLorcaserin
Accession NumberDB04871
TypeSmall Molecule
GroupsApproved
DescriptionLorcaserin (previously APD-356), a highly selective 5HT2C receptor agonist, is used for the treatment of obesity. It has been shown to reduce body weight and food intake in animal models of obesity, and it is thought that targeting the 5HT2C receptor may alter body weight by regulating satiety. Lorcaserin is marketed as a salt form called Belviq, which is lorcaserin hydrochloride.
Structure
Thumb
Synonyms
Lorqess
External Identifiers
  • APD-356
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BelviqTablet10 mg/1OralEisai Inc.2012-06-27Not applicableUs
Belviq XR Extended Release Extended ReleaseTablet, film coated, extended release20 mg/1OralEisai Inc.2016-07-15Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
LorqessNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Lorcaserin hydrochloride
846589-98-8
Thumb
  • InChI Key: ITIHHRMYZPNGRC-QRPNPIFTSA-N
  • Monoisotopic Mass: 231.058154899
  • Average Mass: 232.15
DBSALT000111
Lorcaserin hydrochloride hemihydrate
856681-05-5
Thumb
  • InChI Key: WRZCAWKMTLRWPR-VSODYHHCSA-N
  • Monoisotopic Mass: 480.1268745
  • Average Mass: 482.31
DBSALT001583
Categories
UNII637E494O0Z
CAS number616202-92-7
WeightAverage: 195.69
Monoisotopic: 195.0814772
Chemical FormulaC11H14ClN
InChI KeyXTTZERNUQAFMOF-QMMMGPOBSA-N
InChI
InChI=1S/C11H14ClN/c1-8-7-13-5-4-9-2-3-10(12)6-11(8)9/h2-3,6,8,13H,4-5,7H2,1H3/t8-/m0/s1
IUPAC Name
(1R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine
SMILES
C[[email protected]]1CNCCC2=CC=C(Cl)C=C12
Pharmacology
IndicationFor the treatment of obesity, as an adjunct to a reduced-calorie diet and increased physical activity.
Structured Indications
PharmacodynamicsLorcaserin produced a dose-dependent weight loss over a 12-week period by promoting satiety and decreasing food consumption.
Mechanism of actionAlthough the exact mechanism is unknown, it is believed to involve the selective activation of 5-HT2C receptors in the anorexigenic pro-opiomelanocortin neurons in the arcuate nucleus of the hypothalamus. This results in decreased food intake and satiety by promoting the release of alpha-melanocortin stimulating hormone, which acts on melanocortin-4 receptors.
TargetKindPharmacological actionActionsOrganismUniProt ID
5-hydroxytryptamine receptor 2CProteinunknownNot AvailableHumanP28335 details
Related Articles
AbsorptionLorcaserin has a peak plasma concentration of about 1.5 - 2 hours, but the bioavailability was not determined.
Volume of distribution

The volume of distribution was not determined, but lorcaserin distributes to the central nervous system and cerebrospinal fluid.

Protein bindingLorcaserin hydrochloride has a plasma protein binding of approximately 70%.
Metabolism

Lorcaserin has extensive hepatic metabolism producing inactive compounds. Lorcaserin sulfamate (M1) is the major metabolite circulating in the plasma, and N-carbamoyl glucuronide lorcaserin (M5) is the major metabolite in urine. Other minor metabolites that are both excreted in urine are glucuronide or sulfate conjugates.

SubstrateEnzymesProduct
Lorcaserin
Not Available
Lorcaserin sulfamateDetails
Lorcaserin
Not Available
N-carbamoyl glucuronide lorcaserinDetails
Route of eliminationLorcaserin is eliminated by hepatic metabolism, and the metabolites are eliminated mostly in the urine (92.3%) and some through feces (2.2%).
Half lifeThe plasma half life is approximately 11 hours.
Clearance

The clearance value was not determined.

ToxicityMost common adverse reactions include hypoglycemia (diabetic patients), headache, back pain,fatigue, decrease in lymphocytes,upper respiratory tract infection, and nasopharyngitis. Moreover, the safety and efficacy of coadministration with other weight loss products has not been established, and cardiovascular effects on mortality and morbidity have not been established.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be decreased when combined with Lorcaserin.Experimental, Illicit
AbirateroneThe serum concentration of Lorcaserin can be increased when it is combined with Abiraterone.Approved
AcepromazineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Aceprometazine.Approved
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Lorcaserin.Approved
AcetophenazineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Acetophenazine.Approved
AcetylcholineThe metabolism of Acetylcholine can be decreased when combined with Lorcaserin.Approved
AjmalineThe metabolism of Ajmaline can be decreased when combined with Lorcaserin.Approved
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Lorcaserin.Approved, Investigational
AlogliptinThe metabolism of Alogliptin can be decreased when combined with Lorcaserin.Approved
AlprenololThe metabolism of Alprenolol can be decreased when combined with Lorcaserin.Approved, Withdrawn
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Lorcaserin.Approved, Withdrawn
AmiodaroneThe metabolism of Lorcaserin can be decreased when combined with Amiodarone.Approved, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Amisulpride.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Lorcaserin.Approved
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Lorcaserin.Approved
AmperozideThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Amperozide.Experimental
AmphetamineThe metabolism of Amphetamine can be decreased when combined with Lorcaserin.Approved, Illicit
AmprenavirThe metabolism of Amprenavir can be decreased when combined with Lorcaserin.Approved
AmsacrineThe metabolism of Amsacrine can be decreased when combined with Lorcaserin.Approved
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Lorcaserin.Approved
AprepitantThe serum concentration of Lorcaserin can be increased when it is combined with Aprepitant.Approved, Investigational
AprindineThe metabolism of Aprindine can be decreased when combined with Lorcaserin.Approved
ArformoterolThe metabolism of Arformoterol can be decreased when combined with Lorcaserin.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Lorcaserin.Approved, Investigational
ArmodafinilThe metabolism of Lorcaserin can be decreased when combined with Armodafinil.Approved, Investigational
ArtemetherThe metabolism of Artemether can be decreased when combined with Lorcaserin.Approved
AsenapineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Asenapine.Approved
AstemizoleThe metabolism of Astemizole can be decreased when combined with Lorcaserin.Approved, Withdrawn
AtazanavirThe metabolism of Lorcaserin can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Lorcaserin can be decreased when combined with Atomoxetine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Azaperone.Vet Approved
AzelastineThe metabolism of Azelastine can be decreased when combined with Lorcaserin.Approved
AzithromycinThe metabolism of Lorcaserin can be decreased when combined with Azithromycin.Approved
BenperidolThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Benperidol.Investigational
BenzatropineThe metabolism of Benzatropine can be decreased when combined with Lorcaserin.Approved
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Lorcaserin.Approved
BepridilThe metabolism of Bepridil can be decreased when combined with Lorcaserin.Approved, Withdrawn
BetaxololThe metabolism of Lorcaserin can be decreased when combined with Betaxolol.Approved
BexaroteneThe serum concentration of Lorcaserin can be decreased when it is combined with Bexarotene.Approved, Investigational
BifeprunoxThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Bifeprunox.Investigational
BisoprololThe metabolism of Bisoprolol can be decreased when combined with Lorcaserin.Approved
BoceprevirThe metabolism of Lorcaserin can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Lorcaserin can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Lorcaserin can be decreased when it is combined with Bosentan.Approved, Investigational
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Lorcaserin.Approved
BromocriptineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Bromocriptine.Approved, Investigational
BromperidolThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Bromperidol.Investigational
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Lorcaserin.Approved
BufuralolThe metabolism of Bufuralol can be decreased when combined with Lorcaserin.Experimental, Investigational
BupivacaineThe metabolism of Bupivacaine can be decreased when combined with Lorcaserin.Approved, Investigational
BuprenorphineThe metabolism of Buprenorphine can be decreased when combined with Lorcaserin.Approved, Illicit, Investigational, Vet Approved
BupropionBupropion may increase the serotonergic activities of Lorcaserin.Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Lorcaserin.Approved, Investigational
CabergolineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Cabergoline.Approved
CaffeineThe metabolism of Lorcaserin can be decreased when combined with Caffeine.Approved
CaptoprilThe metabolism of Captopril can be decreased when combined with Lorcaserin.Approved
CarbamazepineThe metabolism of Lorcaserin can be increased when combined with Carbamazepine.Approved, Investigational
CariprazineThe metabolism of Cariprazine can be decreased when combined with Lorcaserin.Approved
CarteololThe metabolism of Carteolol can be decreased when combined with Lorcaserin.Approved
CarvedilolThe metabolism of Carvedilol can be decreased when combined with Lorcaserin.Approved, Investigational
CelecoxibThe metabolism of Lorcaserin can be decreased when combined with Celecoxib.Approved, Investigational
CephalexinThe metabolism of Cephalexin can be decreased when combined with Lorcaserin.Approved, Vet Approved
CeritinibThe serum concentration of Lorcaserin can be increased when it is combined with Ceritinib.Approved
CevimelineThe metabolism of Cevimeline can be decreased when combined with Lorcaserin.Approved
ChloramphenicolThe metabolism of Lorcaserin can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChlordiazepoxideThe metabolism of Chlordiazepoxide can be decreased when combined with Lorcaserin.Approved, Illicit
ChloroquineThe metabolism of Lorcaserin can be decreased when combined with Chloroquine.Approved, Vet Approved
ChlorphenamineThe metabolism of Chlorphenamine can be decreased when combined with Lorcaserin.Approved
ChlorpromazineThe metabolism of Lorcaserin can be decreased when combined with Chlorpromazine.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Chlorprothixene.Approved, Withdrawn
ChlorzoxazoneThe metabolism of Chlorzoxazone can be decreased when combined with Lorcaserin.Approved
CholecalciferolThe metabolism of Lorcaserin can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CilostazolThe metabolism of Cilostazol can be decreased when combined with Lorcaserin.Approved
CimetidineThe metabolism of Lorcaserin can be decreased when combined with Cimetidine.Approved
CinacalcetThe metabolism of Lorcaserin can be decreased when combined with Cinacalcet.Approved
CinnarizineThe metabolism of Cinnarizine can be decreased when combined with Lorcaserin.Approved
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Lorcaserin.Approved
ClarithromycinThe metabolism of Lorcaserin can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Lorcaserin can be decreased when combined with Clemastine.Approved
ClevidipineThe metabolism of Clevidipine can be decreased when combined with Lorcaserin.Approved
ClobazamThe metabolism of Lorcaserin can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Lorcaserin.Approved, Vet Approved
ClonidineThe metabolism of Clonidine can be decreased when combined with Lorcaserin.Approved
ClopidogrelThe metabolism of Lorcaserin can be decreased when combined with Clopidogrel.Approved, Nutraceutical
ClotrimazoleThe metabolism of Lorcaserin can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Lorcaserin can be decreased when combined with Clozapine.Approved
CobicistatThe serum concentration of Lorcaserin can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Lorcaserin can be decreased when combined with Cocaine.Approved, Illicit
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Lorcaserin.Approved, Illicit
ConivaptanThe serum concentration of Lorcaserin can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Lorcaserin can be decreased when combined with Crizotinib.Approved
CyamemazineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Cyamemazine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Lorcaserin.Approved
CyclophosphamideThe metabolism of Cyclophosphamide can be decreased when combined with Lorcaserin.Approved, Investigational
CyclosporineThe metabolism of Lorcaserin can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Lorcaserin can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Lorcaserin can be decreased when it is combined with Dabrafenib.Approved
DapagliflozinThe metabolism of Dapagliflozin can be decreased when combined with Lorcaserin.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Dapiprazole.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Lorcaserin.Investigational
DarifenacinThe metabolism of Lorcaserin can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Lorcaserin can be increased when it is combined with Darunavir.Approved
DasabuvirThe metabolism of Dasabuvir can be decreased when combined with Lorcaserin.Approved
DasatinibThe serum concentration of Lorcaserin can be increased when it is combined with Dasatinib.Approved, Investigational
DebrisoquinThe metabolism of Debrisoquin can be decreased when combined with Lorcaserin.Approved
DeferasiroxThe serum concentration of Lorcaserin can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Lorcaserin can be decreased when combined with Delavirdine.Approved
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Lorcaserin.Approved
DesvenlafaxineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Desvenlafaxine.Approved
DexamethasoneThe serum concentration of Lorcaserin can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexfenfluramineThe metabolism of Dexfenfluramine can be decreased when combined with Lorcaserin.Approved, Illicit, Withdrawn
DexmethylphenidateThe metabolism of Dexmethylphenidate can be decreased when combined with Lorcaserin.Approved
DextroamphetamineThe metabolism of Dextroamphetamine can be decreased when combined with Lorcaserin.Approved, Illicit
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Lorcaserin.Approved
DihydrocodeineThe metabolism of Dihydrocodeine can be decreased when combined with Lorcaserin.Approved, Illicit
DihydroergotamineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Lorcaserin can be decreased when combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Lorcaserin can be decreased when combined with Diphenhydramine.Approved
DolasetronDolasetron may increase the serotonergic activities of Lorcaserin.Approved
DomperidoneThe metabolism of Domperidone can be decreased when combined with Lorcaserin.Approved, Investigational, Vet Approved
DonepezilThe metabolism of Donepezil can be decreased when combined with Lorcaserin.Approved
DopamineThe metabolism of Dopamine can be decreased when combined with Lorcaserin.Approved
DoxazosinThe metabolism of Doxazosin can be decreased when combined with Lorcaserin.Approved
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Lorcaserin.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Lorcaserin.Approved, Investigational
DoxorubicinThe metabolism of Doxorubicin can be decreased when combined with Lorcaserin.Approved, Investigational
DoxycyclineThe metabolism of Lorcaserin can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Lorcaserin can be decreased when combined with Dronedarone.Approved
DroperidolThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Droperidol.Approved, Vet Approved
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Lorcaserin.Approved
EcopipamThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Ecopipam.Investigational
EfavirenzThe serum concentration of Lorcaserin can be decreased when it is combined with Efavirenz.Approved, Investigational
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Lorcaserin.Approved, Investigational
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Lorcaserin.Approved
EncainideThe metabolism of Encainide can be decreased when combined with Lorcaserin.Approved, Withdrawn
EnclomipheneThe metabolism of Enclomiphene can be decreased when combined with Lorcaserin.Investigational
EnzalutamideThe serum concentration of Lorcaserin can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe metabolism of Epinastine can be decreased when combined with Lorcaserin.Approved, Investigational
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Ergoloid mesylate.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Ergonovine.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Ergotamine.Approved
ErlotinibThe metabolism of Erlotinib can be decreased when combined with Lorcaserin.Approved, Investigational
ErythromycinThe metabolism of Lorcaserin can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramThe risk or severity of adverse effects can be increased when Escitalopram is combined with Lorcaserin.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Lorcaserin can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsmirtazapineThe metabolism of Esmirtazapine can be decreased when combined with Lorcaserin.Investigational
EsomeprazoleThe metabolism of Lorcaserin can be decreased when combined with Esomeprazole.Approved, Investigational
EthylmorphineThe metabolism of Ethylmorphine can be decreased when combined with Lorcaserin.Approved, Illicit
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Lorcaserin.Approved, Investigational
EtravirineThe serum concentration of Lorcaserin can be decreased when it is combined with Etravirine.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Fencamfamine.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Lorcaserin.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe metabolism of Fesoterodine can be decreased when combined with Lorcaserin.Approved
FingolimodThe metabolism of Fingolimod can be decreased when combined with Lorcaserin.Approved, Investigational
FlecainideThe metabolism of Flecainide can be decreased when combined with Lorcaserin.Approved, Withdrawn
FluconazoleThe metabolism of Lorcaserin can be decreased when combined with Fluconazole.Approved
FlunarizineThe metabolism of Flunarizine can be decreased when combined with Lorcaserin.Approved
FluoxetineThe metabolism of Lorcaserin can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe metabolism of Fluphenazine can be decreased when combined with Lorcaserin.Approved
FluspirileneThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Fluspirilene.Approved
FluvastatinThe metabolism of Fluvastatin can be decreased when combined with Lorcaserin.Approved
FluvoxamineThe metabolism of Lorcaserin can be decreased when combined with Fluvoxamine.Approved, Investigational
FormoterolThe metabolism of Formoterol can be decreased when combined with Lorcaserin.Approved, Investigational
FosamprenavirThe metabolism of Lorcaserin can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Lorcaserin can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Lorcaserin can be increased when combined with Fosphenytoin.Approved
FrovatriptanThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Lorcaserin.Approved, Investigational
Fusidic AcidThe serum concentration of Lorcaserin can be increased when it is combined with Fusidic Acid.Approved
GalantamineThe metabolism of Galantamine can be decreased when combined with Lorcaserin.Approved
GefitinibThe metabolism of Gefitinib can be decreased when combined with Lorcaserin.Approved, Investigational
GemfibrozilThe metabolism of Lorcaserin can be decreased when combined with Gemfibrozil.Approved
GranisetronGranisetron may increase the serotonergic activities of Lorcaserin.Approved, Investigational
HalofantrineThe metabolism of Halofantrine can be decreased when combined with Lorcaserin.Approved
HaloperidolThe metabolism of Lorcaserin can be decreased when combined with Haloperidol.Approved
HalothaneThe metabolism of Halothane can be decreased when combined with Lorcaserin.Approved, Vet Approved
HydrocodoneThe metabolism of Hydrocodone can be decreased when combined with Lorcaserin.Approved, Illicit
HydromorphoneThe metabolism of Hydromorphone can be decreased when combined with Lorcaserin.Approved, Illicit
IbrutinibThe metabolism of Ibrutinib can be decreased when combined with Lorcaserin.Approved
IdarubicinThe metabolism of Idarubicin can be decreased when combined with Lorcaserin.Approved
IdelalisibThe serum concentration of Lorcaserin can be increased when it is combined with Idelalisib.Approved
IloperidoneThe metabolism of Iloperidone can be decreased when combined with Lorcaserin.Approved
ImatinibThe metabolism of Lorcaserin can be decreased when combined with Imatinib.Approved
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Lorcaserin.Approved
IndinavirThe metabolism of Lorcaserin can be decreased when combined with Indinavir.Approved
Ipratropium bromideThe metabolism of Ipratropium bromide can be decreased when combined with Lorcaserin.Approved
IsavuconazoniumThe metabolism of Lorcaserin can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Lorcaserin.Approved
IsoniazidThe metabolism of Lorcaserin can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Lorcaserin can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Lorcaserin can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Lorcaserin can be increased when it is combined with Ivacaftor.Approved
IxazomibThe metabolism of Ixazomib can be decreased when combined with Lorcaserin.Approved
KetoconazoleThe metabolism of Lorcaserin can be decreased when combined with Ketoconazole.Approved, Investigational
LabetalolThe metabolism of Labetalol can be decreased when combined with Lorcaserin.Approved
LevodopaThe metabolism of Levodopa can be decreased when combined with Lorcaserin.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Levomilnacipran.Approved
LidocaineThe metabolism of Lorcaserin can be decreased when combined with Lidocaine.Approved, Vet Approved
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Lorcaserin.Approved, Investigational
LisurideThe metabolism of Lisuride can be decreased when combined with Lorcaserin.Approved
LithiumThe risk or severity of adverse effects can be increased when Lithium is combined with Lorcaserin.Approved
LomustineThe metabolism of Lomustine can be decreased when combined with Lorcaserin.Approved
LoperamideThe metabolism of Loperamide can be decreased when combined with Lorcaserin.Approved
LopinavirThe metabolism of Lorcaserin can be decreased when combined with Lopinavir.Approved
LoratadineThe metabolism of Loratadine can be decreased when combined with Lorcaserin.Approved
LovastatinThe metabolism of Lorcaserin can be decreased when combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Loxapine.Approved
LuliconazoleThe serum concentration of Lorcaserin can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Lorcaserin can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Lorcaserin can be decreased when combined with Lumefantrine.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Lurasidone.Approved
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Lorcaserin.Approved
MelperoneThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Melperone.Approved
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Lorcaserin.Investigational, Withdrawn
MequitazineThe metabolism of Mequitazine can be decreased when combined with Lorcaserin.Approved
MesoridazineThe metabolism of Mesoridazine can be decreased when combined with Lorcaserin.Approved
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Lorcaserin.Approved
MethamphetamineThe metabolism of Methamphetamine can be decreased when combined with Lorcaserin.Approved, Illicit
MethotrimeprazineThe metabolism of Lorcaserin can be decreased when combined with Methotrimeprazine.Approved
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Lorcaserin.Approved, Vet Approved
MethylphenidateThe metabolism of Methylphenidate can be decreased when combined with Lorcaserin.Approved, Investigational
MethyprylonThe metabolism of Methyprylon can be decreased when combined with Lorcaserin.Approved, Illicit, Withdrawn
MetoclopramideThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Metoclopramide.Approved, Investigational
MetoprololThe metabolism of Lorcaserin can be decreased when combined with Metoprolol.Approved, Investigational
MexiletineThe metabolism of Lorcaserin can be decreased when combined with Mexiletine.Approved
MianserinThe metabolism of Mianserin can be decreased when combined with Lorcaserin.Approved
MifepristoneThe serum concentration of Lorcaserin can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Milnacipran.Approved
MinaprineThe metabolism of Minaprine can be decreased when combined with Lorcaserin.Approved
MirabegronThe metabolism of Mirabegron can be decreased when combined with Lorcaserin.Approved
MirtazapineThe risk or severity of adverse effects can be increased when Mirtazapine is combined with Lorcaserin.Approved
MitotaneThe serum concentration of Lorcaserin can be decreased when it is combined with Mitotane.Approved
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Lorcaserin.Approved
ModafinilThe serum concentration of Lorcaserin can be decreased when it is combined with Modafinil.Approved, Investigational
MolindoneThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Molindone.Approved
MorphineThe metabolism of Morphine can be decreased when combined with Lorcaserin.Approved, Investigational
NafcillinThe serum concentration of Lorcaserin can be decreased when it is combined with Nafcillin.Approved
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Lorcaserin.Approved, Investigational
NateglinideThe metabolism of Nateglinide can be decreased when combined with Lorcaserin.Approved, Investigational
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Lorcaserin.Approved, Investigational
NefazodoneThe metabolism of Lorcaserin can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Lorcaserin can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Lorcaserin can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Lorcaserin can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Lorcaserin can be decreased when combined with Nicardipine.Approved
NicergolineThe metabolism of Nicergoline can be decreased when combined with Lorcaserin.Approved
NicotineThe metabolism of Nicotine can be decreased when combined with Lorcaserin.Approved
NifedipineThe metabolism of Nifedipine can be decreased when combined with Lorcaserin.Approved
NilotinibThe metabolism of Lorcaserin can be decreased when combined with Nilotinib.Approved, Investigational
NitrofuralThe metabolism of Nitrofural can be decreased when combined with Lorcaserin.Approved, Vet Approved
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Lorcaserin.Approved
OlanzapineThe metabolism of Olanzapine can be decreased when combined with Lorcaserin.Approved, Investigational
OlaparibThe metabolism of Lorcaserin can be decreased when combined with Olaparib.Approved
OmeprazoleThe metabolism of Lorcaserin can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronOndansetron may increase the serotonergic activities of Lorcaserin.Approved
OsanetantThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Osanetant.Investigational
OsimertinibThe serum concentration of Lorcaserin can be increased when it is combined with Osimertinib.Approved
OxycodoneThe metabolism of Oxycodone can be decreased when combined with Lorcaserin.Approved, Illicit, Investigational
OxymorphoneThe metabolism of Oxymorphone can be decreased when combined with Lorcaserin.Approved, Investigational, Vet Approved
PalbociclibThe serum concentration of Lorcaserin can be increased when it is combined with Palbociclib.Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Paliperidone.Approved
PalonosetronPalonosetron may increase the serotonergic activities of Lorcaserin.Approved, Investigational
PanobinostatThe serum concentration of Lorcaserin can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe metabolism of Lorcaserin can be decreased when combined with Pantoprazole.Approved
ParoxetineThe metabolism of Lorcaserin can be decreased when combined with Paroxetine.Approved, Investigational
PazopanibThe metabolism of Pazopanib can be decreased when combined with Lorcaserin.Approved
Peginterferon alfa-2bThe serum concentration of Lorcaserin can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentamidineThe metabolism of Pentamidine can be decreased when combined with Lorcaserin.Approved
PentobarbitalThe metabolism of Lorcaserin can be increased when combined with Pentobarbital.Approved, Vet Approved
PerazineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Perazine.Investigational
PerhexilineThe metabolism of Perhexiline can be decreased when combined with Lorcaserin.Approved
PerospironeThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Perospirone.Approved
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Lorcaserin.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Lorcaserin.Approved
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Lorcaserin.Withdrawn
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Lorcaserin.Approved
PhenforminThe metabolism of Phenformin can be decreased when combined with Lorcaserin.Approved, Withdrawn
PhenobarbitalThe metabolism of Lorcaserin can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Lorcaserin can be increased when combined with Phenytoin.Approved, Vet Approved
PimozideThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Pimozide.Approved
PindololThe metabolism of Pindolol can be decreased when combined with Lorcaserin.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Pipamperone.Approved
PiperazineThe metabolism of Piperazine can be decreased when combined with Lorcaserin.Approved, Vet Approved
PipotiazineThe metabolism of Pipotiazine can be decreased when combined with Lorcaserin.Approved
PonatinibThe metabolism of Ponatinib can be decreased when combined with Lorcaserin.Approved
PosaconazoleThe metabolism of Lorcaserin can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Lorcaserin can be increased when combined with Primidone.Approved, Vet Approved
ProcainamideThe metabolism of Procainamide can be decreased when combined with Lorcaserin.Approved
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Lorcaserin.Approved
ProchlorperazineThe metabolism of Prochlorperazine can be decreased when combined with Lorcaserin.Approved, Vet Approved
ProgesteroneThe metabolism of Progesterone can be decreased when combined with Lorcaserin.Approved, Vet Approved
PromazineThe metabolism of Lorcaserin can be decreased when combined with Promazine.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Lorcaserin.Approved
PropafenoneThe serum concentration of Lorcaserin can be increased when it is combined with Propafenone.Approved
PropericiazineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Propericiazine.Approved
PropofolThe metabolism of Propofol can be decreased when combined with Lorcaserin.Approved, Investigational, Vet Approved
PropranololThe metabolism of Propranolol can be decreased when combined with Lorcaserin.Approved, Investigational
ProthipendylThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Prothipendyl.Investigational
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Lorcaserin.Approved
PseudoephedrineThe metabolism of Pseudoephedrine can be decreased when combined with Lorcaserin.Approved
QuazepamThe serum concentration of Lorcaserin can be increased when it is combined with Quazepam.Approved, Illicit
QuetiapineThe metabolism of Quetiapine can be decreased when combined with Lorcaserin.Approved
QuinidineThe metabolism of Lorcaserin can be decreased when combined with Quinidine.Approved
QuinineThe metabolism of Lorcaserin can be decreased when combined with Quinine.Approved
RacloprideThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Raclopride.Investigational
RanitidineThe metabolism of Ranitidine can be decreased when combined with Lorcaserin.Approved
RanolazineThe metabolism of Lorcaserin can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Lorcaserin.Approved
RemoxiprideThe metabolism of Remoxipride can be decreased when combined with Lorcaserin.Approved, Withdrawn
repinotanThe metabolism of repinotan can be decreased when combined with Lorcaserin.Investigational
ReserpineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Reserpine.Approved
RifabutinThe metabolism of Lorcaserin can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Lorcaserin can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Lorcaserin can be increased when combined with Rifapentine.Approved
RisperidoneThe metabolism of Risperidone can be decreased when combined with Lorcaserin.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Ritanserin.Investigational
RitonavirThe metabolism of Lorcaserin can be decreased when combined with Ritonavir.Approved, Investigational
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Lorcaserin.Approved
RolapitantThe metabolism of Lorcaserin can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Lorcaserin can be decreased when combined with Ropinirole.Approved, Investigational
RopivacaineThe metabolism of Ropivacaine can be decreased when combined with Lorcaserin.Approved
RotigotineThe metabolism of Rotigotine can be decreased when combined with Lorcaserin.Approved
SaquinavirThe metabolism of Lorcaserin can be decreased when combined with Saquinavir.Approved, Investigational
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Lorcaserin.Approved, Investigational, Vet Approved
SertindoleThe metabolism of Sertindole can be decreased when combined with Lorcaserin.Approved, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Lorcaserin.Approved
SildenafilThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Lorcaserin can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Lorcaserin can be increased when it is combined with Simeprevir.Approved
SimvastatinThe metabolism of Simvastatin can be decreased when combined with Lorcaserin.Approved
SorafenibThe metabolism of Lorcaserin can be decreased when combined with Sorafenib.Approved, Investigational
SparteineThe metabolism of Sparteine can be decreased when combined with Lorcaserin.Experimental
St. John's WortThe serum concentration of Lorcaserin can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Lorcaserin can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Lorcaserin can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulpirideThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Sulpiride.Approved
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Lorcaserin.Approved, Investigational
TadalafilThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Tadalafil.Approved, Investigational
TamoxifenThe serum concentration of the active metabolites of Tamoxifen can be reduced when Tamoxifen is used in combination with Lorcaserin resulting in a loss in efficacy.Approved
TamsulosinThe metabolism of Tamsulosin can be decreased when combined with Lorcaserin.Approved, Investigational
TapentadolThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Tapentadol.Approved
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Lorcaserin.Approved
TegaserodThe metabolism of Tegaserod can be decreased when combined with Lorcaserin.Investigational, Withdrawn
TelaprevirThe metabolism of Lorcaserin can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Lorcaserin can be decreased when combined with Telithromycin.Approved
TenofovirThe metabolism of Lorcaserin can be decreased when combined with Tenofovir.Approved, Investigational
TerbinafineThe metabolism of Lorcaserin can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerfenadineThe metabolism of Terfenadine can be decreased when combined with Lorcaserin.Withdrawn
TeriflunomideThe serum concentration of Lorcaserin can be decreased when it is combined with Teriflunomide.Approved
TesmilifeneThe metabolism of Tesmilifene can be decreased when combined with Lorcaserin.Investigational
TetrabenazineThe metabolism of Tetrabenazine can be decreased when combined with Lorcaserin.Approved
TheophyllineThe metabolism of Lorcaserin can be decreased when combined with Theophylline.Approved
ThioproperazineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Thioproperazine.Approved
ThioridazineThe metabolism of Lorcaserin can be decreased when combined with Thioridazine.Approved
ThiotepaThe metabolism of Lorcaserin can be decreased when combined with Thiotepa.Approved
ThiothixeneThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Thiothixene.Approved
TiaprideThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Tiapride.Investigational
TiclopidineThe metabolism of Lorcaserin can be decreased when combined with Ticlopidine.Approved
TimololThe metabolism of Timolol can be decreased when combined with Lorcaserin.Approved
TiotropiumThe metabolism of Tiotropium can be decreased when combined with Lorcaserin.Approved
TipranavirThe metabolism of Lorcaserin can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Lorcaserin can be decreased when it is combined with Tocilizumab.Approved
TolterodineThe metabolism of Tolterodine can be decreased when combined with Lorcaserin.Approved, Investigational
TopiramateThe metabolism of Lorcaserin can be decreased when combined with Topiramate.Approved
TrabectedinThe metabolism of Trabectedin can be decreased when combined with Lorcaserin.Approved, Investigational
TramadolThe therapeutic efficacy of Tramadol can be decreased when used in combination with Lorcaserin.Approved, Investigational
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Lorcaserin.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Lorcaserin.Approved, Investigational
TrifluoperazineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Trifluoperazine.Approved
TriflupromazineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Triflupromazine.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Lorcaserin.Approved
TropisetronTropisetron may increase the serotonergic activities of Lorcaserin.Investigational
UdenafilThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Udenafil.Approved, Investigational
UmeclidiniumThe metabolism of Umeclidinium can be decreased when combined with Lorcaserin.Approved
VardenafilThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Vardenafil.Approved
VemurafenibThe serum concentration of Lorcaserin can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Lorcaserin.Approved
VerapamilThe metabolism of Lorcaserin can be decreased when combined with Verapamil.Approved
VilazodoneThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Vilazodone.Approved
VinblastineThe metabolism of Vinblastine can be decreased when combined with Lorcaserin.Approved
VinorelbineThe metabolism of Vinorelbine can be decreased when combined with Lorcaserin.Approved, Investigational
VoriconazoleThe metabolism of Lorcaserin can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Vortioxetine.Approved
YohimbineThe metabolism of Yohimbine can be decreased when combined with Lorcaserin.Approved, Vet Approved
ZalcitabineThe metabolism of Zalcitabine can be decreased when combined with Lorcaserin.Approved
ZiprasidoneThe metabolism of Lorcaserin can be decreased when combined with Ziprasidone.Approved
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Lorcaserin.Approved, Investigational
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Lorcaserin.Approved
ZotepineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Zotepine.Approved
ZuclopenthixolThe metabolism of Zuclopenthixol can be decreased when combined with Lorcaserin.Approved, Investigational
Food Interactions
  • Administration with or without food has no effect.
References
Synthesis Reference

Jandacek RJ: APD-356 (Arena). Curr Opin Investig Drugs. 2005 Oct;6(10):1051-6.

General References
  1. Halford JC: Obesity drugs in clinical development. Curr Opin Investig Drugs. 2006 Apr;7(4):312-8. [PubMed:16625817 ]
  2. Smith BM, Smith JM, Tsai JH, Schultz JA, Gilson CA, Estrada SA, Chen RR, Park DM, Prieto EB, Gallardo CS, Sengupta D, Dosa PI, Covel JA, Ren A, Webb RR, Beeley NR, Martin M, Morgan M, Espitia S, Saldana HR, Bjenning C, Whelan KT, Grottick AJ, Menzaghi F, Thomsen WJ: Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity. J Med Chem. 2008 Jan 24;51(2):305-13. Epub 2007 Dec 21. [PubMed:18095642 ]
External Links
ATC CodesA08AA11
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (401 KB)
MSDSNot Available
ADMET
Predicted ADMET featuresNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
TabletOral10 mg/1
Tablet, film coated, extended releaseOral20 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6953787 No2003-04-102023-04-10Us
US7514422 No2003-04-102023-04-10Us
US7977329 No2003-04-102023-04-10Us
US8168624 No2009-04-182029-04-18Us
US8207158 No2003-04-102023-04-10Us
US8273734 No2003-04-102023-04-10Us
US8367657 No2003-04-102023-04-10Us
US8546379 No2003-04-102023-04-10Us
US8575149 No2003-04-102023-04-10Us
US8697686 No2005-12-202025-12-20Us
US8946207 No2004-06-162024-06-16Us
US8980881 No2005-12-202025-12-20Us
US8999970 No2013-02-072033-02-07Us
US9169213 No2012-12-062032-12-06Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityWater solubility is greater than 400 mg/mL.From FDA label.
Predicted Properties
PropertyValueSource
Water Solubility0.0709 mg/mLALOGPS
logP3ALOGPS
logP2.83ChemAxon
logS-3.4ALOGPS
pKa (Strongest Basic)10.12ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area12.03 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity56.65 m3·mol-1ChemAxon
Polarizability21.51 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzazepines. These are organic compounds containing a benzene ring fused to an azepine ring (unsaturated seven-membered heterocycle with one nitrogen atom replacing a carbon atom).
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzazepines
Sub ClassNot Available
Direct ParentBenzazepines
Alternative Parents
Substituents
  • Benzazepine
  • Azepine
  • Aralkylamine
  • Benzenoid
  • Aryl halide
  • Aryl chloride
  • Secondary amine
  • Secondary aliphatic amine
  • Azacycle
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Organic nitrogen compound
  • Amine
  • Hydrocarbon derivative
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modul...
Gene Name:
HTR2C
Uniprot ID:
P28335
Molecular Weight:
51820.705 Da
References
  1. Halford JC: Obesity drugs in clinical development. Curr Opin Investig Drugs. 2006 Apr;7(4):312-8. [PubMed:16625817 ]
  2. Jandacek RJ: APD-356 (Arena). Curr Opin Investig Drugs. 2005 Oct;6(10):1051-6. [PubMed:16259227 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Usmani KA, Chen WG, Sadeque AJ: Identification of human cytochrome P450 and flavin-containing monooxygenase enzymes involved in the metabolism of lorcaserin, a novel selective human 5-hydroxytryptamine 2C agonist. Drug Metab Dispos. 2012 Apr;40(4):761-71. doi: 10.1124/dmd.111.043414. Epub 2012 Jan 20. [PubMed:22266842 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 Da
References
  1. Usmani KA, Chen WG, Sadeque AJ: Identification of human cytochrome P450 and flavin-containing monooxygenase enzymes involved in the metabolism of lorcaserin, a novel selective human 5-hydroxytryptamine 2C agonist. Drug Metab Dispos. 2012 Apr;40(4):761-71. doi: 10.1124/dmd.111.043414. Epub 2012 Jan 20. [PubMed:22266842 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Usmani KA, Chen WG, Sadeque AJ: Identification of human cytochrome P450 and flavin-containing monooxygenase enzymes involved in the metabolism of lorcaserin, a novel selective human 5-hydroxytryptamine 2C agonist. Drug Metab Dispos. 2012 Apr;40(4):761-71. doi: 10.1124/dmd.111.043414. Epub 2012 Jan 20. [PubMed:22266842 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Usmani KA, Chen WG, Sadeque AJ: Identification of human cytochrome P450 and flavin-containing monooxygenase enzymes involved in the metabolism of lorcaserin, a novel selective human 5-hydroxytryptamine 2C agonist. Drug Metab Dispos. 2012 Apr;40(4):761-71. doi: 10.1124/dmd.111.043414. Epub 2012 Jan 20. [PubMed:22266842 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Usmani KA, Chen WG, Sadeque AJ: Identification of human cytochrome P450 and flavin-containing monooxygenase enzymes involved in the metabolism of lorcaserin, a novel selective human 5-hydroxytryptamine 2C agonist. Drug Metab Dispos. 2012 Apr;40(4):761-71. doi: 10.1124/dmd.111.043414. Epub 2012 Jan 20. [PubMed:22266842 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Usmani KA, Chen WG, Sadeque AJ: Identification of human cytochrome P450 and flavin-containing monooxygenase enzymes involved in the metabolism of lorcaserin, a novel selective human 5-hydroxytryptamine 2C agonist. Drug Metab Dispos. 2012 Apr;40(4):761-71. doi: 10.1124/dmd.111.043414. Epub 2012 Jan 20. [PubMed:22266842 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Nadp binding
Specific Function:
This protein is involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. Form I catalyzes the N-oxygenation of secondary and tertiary amines.
Gene Name:
FMO1
Uniprot ID:
Q01740
Molecular Weight:
60310.285 Da
References
  1. Usmani KA, Chen WG, Sadeque AJ: Identification of human cytochrome P450 and flavin-containing monooxygenase enzymes involved in the metabolism of lorcaserin, a novel selective human 5-hydroxytryptamine 2C agonist. Drug Metab Dispos. 2012 Apr;40(4):761-71. doi: 10.1124/dmd.111.043414. Epub 2012 Jan 20. [PubMed:22266842 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Vitamin d 24-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. Usmani KA, Chen WG, Sadeque AJ: Identification of human cytochrome P450 and flavin-containing monooxygenase enzymes involved in the metabolism of lorcaserin, a novel selective human 5-hydroxytryptamine 2C agonist. Drug Metab Dispos. 2012 Apr;40(4):761-71. doi: 10.1124/dmd.111.043414. Epub 2012 Jan 20. [PubMed:22266842 ]
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Drug created on October 20, 2007 04:39 / Updated on December 05, 2016 02:43