Identification

Name
Lorcaserin
Accession Number
DB04871
Type
Small Molecule
Groups
Approved
Description

Lorcaserin (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 IDs
APD-356
Product Ingredients
IngredientUNIICASInChI Key
Lorcaserin hydrochloride0QJF08GDPE846589-98-8ITIHHRMYZPNGRC-QRPNPIFTSA-N
Lorcaserin hydrochloride hemihydrateREV26SR2B4856681-05-5WRZCAWKMTLRWPR-VSODYHHCSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BelviqTablet10 mg/1OralEisai Limited2012-06-27Not applicableUs
Belviq XRTablet, film coated, extended release20 mg/1OralEisai Limited2016-07-15Not applicableUs
International/Other Brands
Lorqess
Categories
UNII
637E494O0Z
CAS number
616202-92-7
Weight
Average: 195.69
Monoisotopic: 195.0814772
Chemical Formula
C11H14ClN
InChI Key
XTTZERNUQAFMOF-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

Indication

For the treatment of obesity, as an adjunct to a reduced-calorie diet and increased physical activity.

Structured Indications
Pharmacodynamics

Lorcaserin produced a dose-dependent weight loss over a 12-week period by promoting satiety and decreasing food consumption.

Mechanism of action

Although 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.

TargetActionsOrganism
U5-hydroxytryptamine receptor 2CNot AvailableHuman
Absorption

Lorcaserin 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 binding

Lorcaserin 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.

Route of elimination

Lorcaserin is eliminated by hepatic metabolism, and the metabolites are eliminated mostly in the urine (92.3%) and some through feces (2.2%).

Half life

The plasma half life is approximately 11 hours.

Clearance

The clearance value was not determined.

Toxicity

Most 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
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not 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
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Lorcaserin.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, Investigational
AlmotriptanThe metabolism of Almotriptan can be decreased when 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
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Lorcaserin.Approved
AmoxapineThe metabolism of Amoxapine can be decreased when combined with Lorcaserin.Approved
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 Lorcaserin can be decreased when combined with Artemether.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
AvanafilThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Avanafil.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
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
BisoprololThe metabolism of Bisoprolol can be decreased when combined with Lorcaserin.Approved
BoceprevirThe metabolism of Lorcaserin can be decreased when combined with Boceprevir.Approved, Withdrawn
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
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 metabolism of Buspirone can be decreased when 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
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, Investigational
CitalopramThe metabolism of Lorcaserin can be decreased when combined with Citalopram.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 metabolism of Lorcaserin can be decreased when combined with Clomipramine.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
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 Conivaptan can be increased when it is combined with Lorcaserin.Approved, Investigational
CrizotinibThe metabolism of Lorcaserin can be decreased when combined with Crizotinib.Approved
CyclobenzaprineThe metabolism of Cyclobenzaprine can be decreased when 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
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, Investigational
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 metabolism of Lorcaserin can be decreased when combined with Desipramine.Approved
DeutetrabenazineThe metabolism of Deutetrabenazine can be decreased when combined with Lorcaserin.Approved, Investigational
Dexchlorpheniramine maleateThe metabolism of Dexchlorpheniramine maleate can be decreased when combined with Lorcaserin.Approved
DexfenfluramineThe metabolism of Dexfenfluramine can be decreased when combined with Lorcaserin.Approved, Illicit, Investigational, 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 metabolism of Dextromethorphan can be decreased when combined with Lorcaserin.Approved
DihydrocodeineThe metabolism of Dihydrocodeine can be decreased when combined with Lorcaserin.Approved, Illicit
DihydroergotamineThe metabolism of Lorcaserin can be decreased when 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
DolasetronThe metabolism of Dolasetron can be decreased when combined with 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
DosulepinThe metabolism of Lorcaserin can be decreased when combined with Dosulepin.Approved
DoxazosinThe metabolism of Doxazosin can be decreased when combined with Lorcaserin.Approved
DoxepinThe metabolism of Doxepin can be decreased when 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
DuloxetineThe metabolism of Lorcaserin can be decreased when combined with Duloxetine.Approved
EfavirenzThe metabolism of Lorcaserin can be decreased when combined with Efavirenz.Approved, Investigational
EletriptanThe metabolism of Eletriptan can be decreased when combined with Lorcaserin.Approved, Investigational
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Lorcaserin.Approved
EnasidenibThe metabolism of Enasidenib can be decreased when combined with Lorcaserin.Approved
EncainideThe metabolism of Encainide can be decreased when combined with Lorcaserin.Approved, Investigational, 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
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 metabolism of Escitalopram can be decreased when combined with Lorcaserin.Approved, Investigational
Eslicarbazepine acetateThe metabolism of Lorcaserin can be decreased when 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 metabolism of Lorcaserin can be decreased when combined with Etravirine.Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination 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
FluphenazineThe metabolism of Fluphenazine can be decreased when combined with Lorcaserin.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
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
GranisetronThe metabolism of Granisetron can be decreased when combined with 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 metabolism of Lorcaserin can be decreased when 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 metabolism of Lorcaserin can be decreased when combined with Imipramine.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
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
LetermovirThe metabolism of Letermovir can be decreased when combined with Lorcaserin.Approved
LevodopaThe metabolism of Levodopa can be decreased when combined with Lorcaserin.Approved
LevomilnacipranThe metabolism of Levomilnacipran can be decreased when combined with Lorcaserin.Approved
LidocaineThe metabolism of Lorcaserin can be decreased when combined with Lidocaine.Approved, Vet Approved
LisurideThe metabolism of Lisuride can be decreased when combined with Lorcaserin.Approved, Investigational
LobeglitazoneThe metabolism of Lorcaserin can be decreased when combined with Lobeglitazone.Approved, Investigational
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
LorpiprazoleThe serum concentration of Lorcaserin can be increased when it is combined with Lorpiprazole.Approved
LovastatinThe metabolism of Lorcaserin can be decreased when combined with Lovastatin.Approved, Investigational
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
ManidipineThe metabolism of Lorcaserin can be decreased when combined with Manidipine.Approved, Investigational
MaprotilineThe metabolism of Maprotiline can be decreased when combined with Lorcaserin.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, Investigational
MethadoneThe metabolism of Lorcaserin can be decreased when combined with Methadone.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, Investigational, Vet Approved
MethylergometrineThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Methylergometrine.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 metabolism of Metoclopramide can be decreased when combined with Lorcaserin.Approved, Investigational
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Lorcaserin.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, Investigational
MidostaurinThe metabolism of Lorcaserin can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Lorcaserin can be increased when it is combined with Mifepristone.Approved, Investigational
MinaprineThe metabolism of Minaprine can be decreased when combined with Lorcaserin.Approved
MirabegronThe metabolism of Mirabegron can be decreased when combined with Lorcaserin.Approved
MirodenafilThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Mirodenafil.Investigational
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Lorcaserin.Approved
MitotaneThe serum concentration of Lorcaserin can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Moclobemide can be decreased when combined with Lorcaserin.Approved
ModafinilThe metabolism of Lorcaserin can be decreased when combined with Modafinil.Approved, Investigational
MorphineThe metabolism of Morphine can be decreased when 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, Investigational
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, Investigational, Vet Approved
NortriptylineThe metabolism of Nortriptyline can be decreased when 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
OndansetronThe metabolism of Ondansetron can be decreased when combined with Lorcaserin.Approved
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
PalonosetronThe metabolism of Palonosetron can be decreased when combined with 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
PerhexilineThe metabolism of Perhexiline can be decreased when combined with Lorcaserin.Approved, Investigational
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Lorcaserin.Approved
PethidineThe metabolism of Pethidine can be decreased when combined with Lorcaserin.Approved
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Lorcaserin.Withdrawn
PhenforminThe metabolism of Phenformin can be decreased when combined with Lorcaserin.Approved, Investigational, 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
PindololThe metabolism of Pindolol can be decreased when combined with Lorcaserin.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, Investigational
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
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 metabolism of Promethazine can be decreased when combined with Lorcaserin.Approved
PropafenoneThe serum concentration of Lorcaserin can be increased when it is combined with Propafenone.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
ProtriptylineThe metabolism of Protriptyline can be decreased when 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
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
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
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
RitonavirThe metabolism of Lorcaserin can be decreased when combined with Ritonavir.Approved, Investigational
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
RucaparibThe metabolism of Rucaparib can be decreased when combined with Lorcaserin.Approved, Investigational
RupatadineThe metabolism of Rupatadine can be decreased when combined with Lorcaserin.Approved
SaquinavirThe metabolism of Lorcaserin can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Lorcaserin can be decreased when used in combination with Sarilumab.Approved
SertindoleThe metabolism of Sertindole can be decreased when combined with Lorcaserin.Approved, Investigational, Withdrawn
SertralineThe metabolism of Lorcaserin can be decreased when combined with Sertraline.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.Investigational, 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
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 metabolism of Tapentadol can be decreased when combined with 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, Withdrawn
TelithromycinThe metabolism of Lorcaserin can be decreased when combined with Telithromycin.Approved
Tenofovir disoproxilThe metabolism of Lorcaserin can be decreased when combined with Tenofovir disoproxil.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
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Lorcaserin.Approved, Withdrawn
ThiotepaThe metabolism of Lorcaserin can be decreased when combined with Thiotepa.Approved
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 metabolism of Lorcaserin can be decreased when combined with Tranylcypromine.Approved
TrazodoneThe metabolism of Trazodone can be decreased when combined with Lorcaserin.Approved, Investigational
TrimipramineThe metabolism of Trimipramine can be decreased when combined with Lorcaserin.Approved
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
ValbenazineThe metabolism of Valbenazine can be decreased when combined with Lorcaserin.Approved, Investigational
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 metabolism of Lorcaserin can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Lorcaserin can be decreased when combined with Verapamil.Approved
VernakalantThe metabolism of Vernakalant can be decreased when combined with Lorcaserin.Approved, Investigational
VilazodoneThe metabolism of Vilazodone can be decreased when combined with Lorcaserin.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 metabolism of Vortioxetine can be decreased when combined with Lorcaserin.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, Investigational
ZiprasidoneThe metabolism of Lorcaserin can be decreased when combined with Ziprasidone.Approved
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Lorcaserin.Approved
ZucapsaicinThe metabolism of Lorcaserin can be decreased when combined with Zucapsaicin.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
KEGG Drug
D06613
PubChem Compound
11658860
PubChem Substance
310264855
ChemSpider
9833595
BindingDB
50161646
ChEBI
65353
ChEMBL
CHEMBL360328
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Lorcaserin
ATC Codes
A08AA11 — Lorcaserin
FDA label
Download (401 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableBMI >30 kg/m22
1CompletedNot AvailableHepatic Impairment1
1CompletedNot AvailableImpaired Renal Function1
1CompletedNot AvailablePharmacokinetics in Obese Adolescents1
1CompletedDiagnosticCocaine Abuse1
1CompletedTreatmentBMI >30 kg/m21
1CompletedTreatmentHealthy Volunteers2
1Not Yet RecruitingBasic ScienceDependence, Cocaine1
1Not Yet RecruitingPreventionCardiovascular Disease (CVD)1
1RecruitingBasic ScienceCocaine Use Disorders1
1RecruitingTreatmentCannabis Use Disorders1
1RecruitingTreatmentCocaine-Related Disorders / Opioid-Related Disorders1
1, 2CompletedTreatmentTobacco Use Disorders / Weight gain therapy1
1, 2Enrolling by InvitationTreatmentMuscle Weakness / Sepsis1
1, 2RecruitingBasic ScienceCannabis Use1
1, 2RecruitingTreatmentCocaine Use Disorders1
2CompletedTreatmentBMI >30 kg/m22
2CompletedTreatmentCessation, Smoking1
2Not Yet RecruitingTreatmentCocaine Use Disorders1
2RecruitingTreatmentCocaine-Related Disorders1
2RecruitingTreatmentNicotine Dependence1
2, 3RecruitingTreatmentBMI >30 kg/m2 / Cessation, Smoking1
3CompletedTreatmentBMI >27 kg/m2 / Obese1
3CompletedTreatmentBMI >30 kg/m23
4Active Not RecruitingTreatmentBMI >27 kg/m2 / BMI >30 kg/m2 / Cardiovascular Disease (CVD) / High Cardiovascular Risk / Type 2 Diabetes Mellitus1
4Active Not RecruitingTreatmentBMI >30 kg/m2 / Obese experiencing rapid weight loss1
4CompletedTreatmentChronic Weight Management1
4Not Yet RecruitingOtherOverweight and Obesity1
4RecruitingTreatmentBMI >27 kg/m2 / Schizoaffective Disorders / Schizophrenic Disorders1
4RecruitingTreatmentBMI >30 kg/m21
4Unknown StatusTreatmentWeight gain therapy1
Not AvailableCompletedTreatmentBMI >30 kg/m21

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
TabletOral10 mg/1
Tablet, film coated, extended releaseOral20 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6953787No2003-04-102023-04-10Us
US7514422No2003-04-102023-04-10Us
US7977329No2003-04-102023-04-10Us
US8207158No2003-04-102023-04-10Us
US8273734No2003-04-102023-04-10Us
US8546379No2003-04-102023-04-10Us
US8367657No2003-04-102023-04-10Us
US8575149No2003-04-102023-04-10Us
US9169213No2012-12-062032-12-06Us
US8999970No2013-02-072033-02-07Us
US8980881No2005-12-202025-12-20Us
US8946207No2004-06-162024-06-16Us
US8168624No2009-04-182029-04-18Us
US8697686No2005-12-202025-12-20Us
US7169401No2003-07-182023-07-18Us
US9770455No2011-08-312031-08-31Us

Properties

State
Solid
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 RuleNoChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This 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).
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzazepines
Sub Class
Not Available
Direct Parent
Benzazepines
Alternative Parents
Azepines / Aralkylamines / Benzenoids / Aryl chlorides / Dialkylamines / Azacyclic compounds / Organopnictogen compounds / Organochlorides / Hydrocarbon derivatives
Substituents
Benzazepine / Azepine / Aralkylamine / Benzenoid / Aryl halide / Aryl chloride / Azacycle / Secondary amine / Secondary aliphatic amine / Organonitrogen compound
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
organochlorine compound, benzazepine (CHEBI:65353)

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-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
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. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
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 un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
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 im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
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
Inhibitor
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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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
Uniprot Name
Dimethylaniline monooxygenase [N-oxide-forming] 1
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 un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
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]

Drug created on October 20, 2007 04:39 / Updated on January 20, 2018 03:52