Details of the Drug

General Information of Drug (ID: DMG6OYJ)

• Drug Name: Lorcaserin
• Synonyms: APD 356; APD356; AR-10A; (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine; 10-chloro-2-methyl-4-azabicyclo[5.4.0]undeca-8,10,12-triene

Indication

Disease Entry	ICD 11	Status	REF
Obesity	5B81	Approved	[1]
Drug abuse	6C4G.1Z	Phase 1	[1]

• Affected Organisms: Humans and other mammals
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 195.69
  Logarithm of the Partition Coefficient (xlogp); 2.7
  Rotatable Bond Count (rotbonds); 0
  Hydrogen Bond Donor Count (hbonddonor); 1
  Hydrogen Bond Acceptor Count (hbondacc); 1
• ADMET Property:
  Half-life: The concentration or amount of drug in body reduced by one-half in 11 hours [2]
  Metabolism: The drug is metabolized via the hepatic []
• Chemical Identifiers:
  Formula: C11H14ClN
  IUPAC Name: (5R)-7-chloro-5-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine
  Canonical SMILES: C[C@H]1CNCCC2=C1C=C(C=C2)Cl
  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
  InChIKey: XTTZERNUQAFMOF-QMMMGPOBSA-N
• Cross-matching ID:
  PubChem CID: 11658860
  ChEBI ID: CHEMBL360328
  CAS Number: 616202-92-7
  UNII: 637E494O0Z
  DrugBank ID: DB04871
  TTD ID: D01JMC
  INTEDE ID: DR0979
  ACDINA ID: D00376
• Drug-Molecule Activity Atlas (DMA)NEW: Click to Jump to the Detailed DMA Information of This Drug
• Drug Pharmacogenomic Perturbation (DPP)NEW: Click to Jump to the Detailed DPP Information of This Drug
• Drug ADMET Endpoint Profile (DAE)NEW: Click to Jump to the Detailed DAE Information of This Drug
• Repurposed Drugs (RPD): Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 2C receptor (HTR2C)	TTWJBZ5	5HT2C_HUMAN	Agonist	[3]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Substrate	[4]
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Substrate	[4]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Substrate	[4]
Cytochrome P450 2A6 (CYP2A6)	DEJVYAZ	CP2A6_HUMAN	Substrate	[4]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Substrate	[4]
Cytochrome P450 2B6 (CYP2B6)	DEPKLMQ	CP2B6_HUMAN	Substrate	[4]

Molecular Expression Atlas of This Drug

• The Studied Disease: Obesity
• ICD Disease Classification: 5B81

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
5-HT 2C receptor (HTR2C)	DTT	HTR2C	1.02E-02	-0.45	-0.37
5-HT 2C receptor (HTR2C)	DTT	HTR2C	2.27E-01	0.27	0.6
Cytochrome P450 2B6 (CYP2B6)	DME	CYP2B6	9.90E-01	3.10E-03	1.75E-02
Cytochrome P450 2B6 (CYP2B6)	DME	CYP2B6	5.35E-01	1.10E-02	1.19E-01
Cytochrome P450 2A6 (CYP2A6)	DME	CYP2A6	6.24E-01	6.79E-02	2.28E-01
Cytochrome P450 2A6 (CYP2A6)	DME	CYP2A6	2.82E-01	-4.18E-02	-2.80E-01
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	6.73E-02	6.49E-02	3.07E-01
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	6.45E-01	2.07E-02	1.74E-01
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	7.39E-01	1.54E-02	4.74E-02
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	4.64E-02	-8.21E-02	-7.11E-01
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	2.59E-01	6.29E-02	3.14E-01
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	4.84E-01	-8.38E-02	-8.46E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	4.66E-01	4.25E-02	1.20E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	4.75E-01	5.15E-02	3.64E-01

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Lorcaserin (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Methylene blue	DMJAPE7	Major	Additive serotonergic effects by the combination of Lorcaserin and Methylene blue.	Acquired methaemoglobinaemia [3A93]	[5]
Levomilnacipran	DMV26S8	Major	Additive serotonergic effects by the combination of Lorcaserin and Levomilnacipran.	Chronic pain [MG30]	[5]
Vilazodone	DM4LECQ	Major	Additive serotonergic effects by the combination of Lorcaserin and Vilazodone.	Depression [6A70-6A7Z]	[5]
Vortioxetine	DM6F1PU	Major	Additive serotonergic effects by the combination of Lorcaserin and Vortioxetine.	Depression [6A70-6A7Z]	[5]
Milnacipran	DMBFE74	Major	Additive serotonergic effects by the combination of Lorcaserin and Milnacipran.	Depression [6A70-6A7Z]	[5]
Desvenlafaxine	DMHD4PE	Major	Additive serotonergic effects by the combination of Lorcaserin and Desvenlafaxine.	Depression [6A70-6A7Z]	[5]
OPC-34712	DMHG57U	Major	Decreased metabolism of Lorcaserin caused by OPC-34712 mediated inhibition of CYP450 enzyme.	Depression [6A70-6A7Z]	[6]
Mirabegron	DMS1GYT	Moderate	Decreased metabolism of Lorcaserin caused by Mirabegron mediated inhibition of CYP450 enzyme.	Functional bladder disorder [GC50]	[5]
Lasmiditan	DMXLVDT	Major	Additive serotonergic effects by the combination of Lorcaserin and Lasmiditan.	Migraine [8A80]	[5]
Ozanimod	DMT6AM2	Major	Additive serotonergic effects by the combination of Lorcaserin and Ozanimod.	Multiple sclerosis [8A40]	[7]
Iloperidone	DM6AUFY	Moderate	Increased risk of hyperprolactinemic effects by the combination of Lorcaserin and Iloperidone.	Schizophrenia [6A20]	[5]
Asenapine	DMSQZE2	Moderate	Increased risk of hyperprolactinemic effects by the combination of Lorcaserin and Asenapine.	Schizophrenia [6A20]	[5]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
FD&C blue no. 2	E00446	2723854	Colorant
Mannitol	E00103	6251	Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Sunset yellow FCF	E00255	17730	Colorant
Carmellose sodium	E00625	Not Available	Disintegrant
Eisenoxyd	E00585	56841934	Colorant
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Hydroxypropyl cellulose	E00632	Not Available	Binding agent; Coating agent; Emulsifying agent; Film/Membrane-forming agent; Modified-release agent; Suspending agent; Viscosity-controlling agent
Hypromellose	E00634	Not Available	Coating agent
Magnesium stearate	E00208	11177	lubricant
Polyethylene glycol 4000	E00654	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyvinyl alcohol	E00666	Not Available	Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Certolake sunset yellow	E00351	61817	Colorant
Colcothar yellow	E00436	518696	Colorant
Haematite red	E00236	14833	Colorant
Hydrophobic colloidal silica	E00285	24261	Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
Cellulose microcrystalline	E00698	Not Available	Adsorbent; Suspending agent; Diluent
Ethyl cellulose	E00699	Not Available	Coating agent; Microencapsulating agent; Binding agent; Diluent; Viscosity-controlling agent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Lorcaserin 20 mg tablet	20 mg	24 HR Extended Release Oral Tablet	Oral
Lorcaserin 10 mg tablet	10 mg	Oral Tablet	Oral
Lorcaserin Hydrochloride 10mg tablet	10mg	Tablet	Oral
Lorcaserin Hydrochloride 20mg tablet	20mg	Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2941).
• [2] Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
• [3] Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
• [4] 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.
• [5] Product Information. Belviq (lorcaserin). Eisai Inc, Teaneck, NJ.
• [6] Product Information. Rexulti (brexpiprazole). Otsuka American Pharmaceuticals Inc, Rockville, MD.
• [7] Gilman AG, Rall TW, Nies AS, Taylor P, eds. "Goodman and Gilman's the Pharmacological Basis of Therapeutics. 8th ed." New York, NY: Pergamon Press Inc. (1990):.