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lorcaserin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 4374 | 616202-92-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a serotonin 2C receptor agonist for oral administration used for chronic weight management
|
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 |
| BA (Bioavailability) | 93 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK12,MAPK7,MAPK9,MAPKAPK2,NTRK2,PDK2,PDK4,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1 | 43 | |||
| kinase-selectivity-class | AKT1,AKT2,AKT3,AXL,BRAF,EIF2AK3,MELK,PAK4,PDK1,PDK4,PRKACA,PRKG1,STK33 | 13 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
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 | 122.71 | 35.89 | 96 | 1106 | 862650 | 89764595 |
| Dizziness | 73.36 | 35.89 | 61 | 1141 | 589223 | 90038022 |
| Fatigue | 69.41 | 35.89 | 80 | 1122 | 1153943 | 89473302 |
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 | 68.56 | 32.03 | 61 | 1014 | 882316 | 109705908 |
| Dizziness | 47.60 | 32.03 | 45 | 1030 | 698148 | 109890076 |
| Intentional underdose | 38.26 | 32.03 | 8 | 1067 | 2544 | 110585680 |
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:35941 | serotonergic agonist |
| CHEBI has role | CHEBI:50507 | appetite depressant |
| CHEBI has role | CHEBI:74518 | anti-obesity agent |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:231911 | renoprotective agent |
Related Drugs by ATC class:
A08AA Centrally acting antiobesity products 15 drugs
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 | AGONIST | Ki | 7.89 | DRUG LABEL | DRUG LABEL | |||
| Sodium-dependent serotonin transporter | Transporter | Ki | 5.58 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 7.04 | DRUG LABEL | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | 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 |
| 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 |
| 8765 | INN_ID |
| 11658860 | PUBCHEM_CID |
| 637E494O0Z | INXIGHT DRUGS |
Pharmaceutical products:
None