lorcaserin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	4374	616202-92-7

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

lorcaserin hydrochloride hemihydrate
lorcaserin hydrochloride
belviq
lorcaserin
lorcaserin HCl
APD356
APD 356
APD-356

a serotonin 2C receptor agonist for oral administration used for chronic weight management

Molecular weight: 195.69
Formula: C11H14ClN
CLOGP: 3.24
LIPINSKI: 0
HAC: 1
HDO: 1
TPSA: 12.03
ALOGS: -3.44
ROTB: 0

Drug dosage:

None

ADMET properties:

Property	Value	Reference
fu (Fraction unbound in plasma)	0.06 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Approvals:

Date	Agency	Company	Orphan
June 27, 2012	FDA	EISAI INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Headache	120.38	34.76	95	1056	633146	62854725
Dizziness	73.56	34.76	61	1090	429864	63058007
Fatigue	64.54	34.76	79	1072	887949	62599922

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Headache	67.18	30.92	59	937	653713	79089679
Dizziness	46.93	30.92	44	952	526397	79216995
Intentional underdose	36.91	30.92	8	988	2346	79741046

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	A08AA11	ALIMENTARY TRACT AND METABOLISM ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS Centrally acting antiobesity products
FDA MoA	N0000182137	Cytochrome P450 2D6 Inhibitors
FDA MoA	N0000185009	Serotonin 2c Receptor Agonists
FDA EPC	N0000185010	Serotonin-2c Receptor Agonist
CHEBI has role	CHEBI:74518	anti-obestic agents
CHEBI has role	CHEBI:35941	serotonin agonists

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Obesity	indication	414916001	DOID:9970
Pregnancy, function	contraindication	289908002

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.63	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	AGONIST	Ki	7.89		DRUG LABEL	DRUG LABEL
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.58		CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	7.04		DRUG LABEL
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	6.83		DRUG LABEL

External reference:

ID	Source
D06613	KEGG_DRUG
4032466	VUID
N0000187068	NUI
856681-05-5	SECONDARY_CAS_RN
4032466	VANDF
4032467	VANDF
CHEBI:65353	CHEBI
T4U	PDB_CHEM_ID
CHEMBL360328	ChEMBL_ID
CHEMBL2095211	ChEMBL_ID
C506658	MESH_SUPPLEMENTAL_RECORD_UI
2941	IUPHAR_LIGAND_ID
8765	INN_ID
DB04871	DRUGBANK_ID
637E494O0Z	UNII
1300700	RXNORM
191544	MMSL
244047	MMSL
28610	MMSL
d07875	MMSL
015054	NDDF
015055	NDDF
716226007	SNOMEDCT_US
716227003	SNOMEDCT_US
C2350948	UMLSCUI
11658860	PUBCHEM_CID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Belviq	HUMAN PRESCRIPTION DRUG LABEL	1	62856-529	TABLET	10 mg	ORAL	NDA	32 sections
BELVIQ XR Extended ReleaseExtended Release	HUMAN PRESCRIPTION DRUG LABEL	1	62856-535	TABLET, FILM COATED, EXTENDED RELEASE	20 mg	ORAL	NDA	31 sections