fenfluramine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
anorexics 1150 458-24-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fenfluramine
  • DL-Fenfluramine
  • fenfluramine hydrochloride
  • fenfluramine HCl
  • pondimin
A centrally active drug that apparently both blocks serotonin uptake and provokes transport-mediated serotonin release.
  • Molecular weight: 231.26
  • Formula: C12H16F3N
  • CLOGP: 3.30
  • LIPINSKI: 0
  • HAC: 1
  • HDO: 1
  • TPSA: 12.03
  • ALOGS: -4.03
  • ROTB: 5

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.12 g O

ADMET properties:

None

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC A08AA02 ALIMENTARY TRACT AND METABOLISM
ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS
ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS
Centrally acting antiobesity products
ATC N03AX26 NERVOUS SYSTEM
ANTIEPILEPTICS
ANTIEPILEPTICS
Other antiepileptics
CHEBI has role CHEBI:35941 serotonergic agonists
CHEBI has role CHEBI:50949 serotonin reuptake inhibitor
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D014179 Neurotransmitter Uptake Inhibitors
MeSH PA D018490 Serotonin Agents
MeSH PA D017367 Serotonin Uptake Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Obesity indication 414916001 DOID:9970
Alcoholism contraindication 7200002
Glaucoma contraindication 23986001 DOID:1686
Hypertensive disorder contraindication 38341003 DOID:10763
Diabetes mellitus type 2 contraindication 44054006 DOID:9352
Diabetes mellitus type 1 contraindication 46635009 DOID:9744
Pulmonary hypertension contraindication 70995007 DOID:6432

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.22 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 2.2MG BASE/ML FINTEPLA ZOGENIX INC N212102 June 25, 2020 RX SOLUTION ORAL June 25, 2023 NEW PRODUCT
EQ 2.2MG BASE/ML FINTEPLA ZOGENIX INC N212102 June 25, 2020 RX SOLUTION ORAL June 25, 2027 INDICATED FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME IN PATIENTS 2 YEARS OF AGE AND OLDER

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Alpha-1B adrenergic receptor GPCR Ki 6.85 PDSP
Alpha-2C adrenergic receptor GPCR Ki 6.74 PDSP
Alpha-2B adrenergic receptor GPCR Ki 6.72 PDSP
Alpha-1A adrenergic receptor GPCR Ki 6.57 PDSP
Alpha-2A adrenergic receptor GPCR Ki 6.43 PDSP
5-hydroxytryptamine receptor 2B GPCR Ki 6.40 PDSP
5-hydroxytryptamine receptor 1D GPCR Ki 6.20 PDSP
Sodium-dependent serotonin transporter Transporter Ki 6.18 PDSP
5-hydroxytryptamine receptor 1A GPCR Ki 6.17 PDSP
Muscarinic acetylcholine receptor M1 GPCR Ki 6.02 PDSP
Beta-1 adrenergic receptor GPCR Ki 6.00 PDSP
5-hydroxytryptamine receptor 2A GPCR Ki 5.84 PDSP
5-hydroxytryptamine receptor 2C GPCR Ki 5.79 PDSP
5-hydroxytryptamine receptor 1B GPCR Ki 5.74 PDSP
Muscarinic acetylcholine receptor M2 GPCR Ki 5.73 PDSP
Muscarinic acetylcholine receptor M3 GPCR Ki 5.49 PDSP
5-hydroxytryptamine receptor 7 GPCR Ki 5.38 PDSP
Muscarinic acetylcholine receptor M4 GPCR Ki 5.17 PDSP
Beta-2 adrenergic receptor GPCR Ki 5.11 PDSP
5-hydroxytryptamine receptor 6 GPCR Ki 5.04 PDSP

External reference:

IDSource
4019754 VUID
N0000147845 NUI
D04148 KEGG_DRUG
404-82-0 SECONDARY_CAS_RN
4018420 VANDF
4019754 VANDF
C0015827 UMLSCUI
CHEBI:5000 CHEBI
CHEMBL87493 ChEMBL_ID
CHEMBL2106217 ChEMBL_ID
DB00574 DRUGBANK_ID
D005277 MESH_DESCRIPTOR_UI
3337 PUBCHEM_CID
4613 IUPHAR_LIGAND_ID
1596 INN_ID
2DS058H2CF UNII
202366 RXNORM
1756 MMSL
38581 MMSL
4717 MMSL
d00812 MMSL
001873 NDDF
004776 NDDF
387262004 SNOMEDCT_US
387451002 SNOMEDCT_US
78700004 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
FINTEPLA HUMAN PRESCRIPTION DRUG LABEL 1 43376-322 SOLUTION 2.20 mg ORAL NDA 31 sections