fenfluramine 🐶 Veterinary Use | 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
  • fintepla
A centrally active drug that apparently both blocks serotonin uptake and provokes transport-mediated serotonin release. The mechanisms by which fenfluramine exerts its therapeutic effects in the treatment of seizures associated with Dravet syndrome are unknown. Fenfluramine and the metabolite, norfenfluramine, increase extracellular levels of serotonin through interaction with serotonin transporter proteins, and exhibit agonist activity at serotonin 5HT-2 receptors.
  • 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
8 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
June 25, 2020 FDA UCB INC
Sept. 26, 2022 PMDA UCB JAPAN CO., LTD.
Dec. 18, 2020 EMA UCB PHARMA S.A.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Seizure 133.20 76.18 42 294 132592 63356094

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Seizure 131.76 71.38 43 229 104814 34851845
Echocardiogram abnormal 83.00 71.38 13 259 1050 34955609

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Seizure 214.24 66.63 69 454 188765 79555100
Echocardiogram abnormal 117.60 66.63 19 504 2209 79741656

FDA Adverse Event Reporting System (Pediatric)

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 serotonin agonists
CHEBI has role CHEBI:50949 SSRI
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D014179 Neurotransmitter Uptake Inhibitors
MeSH PA D017367 Selective Serotonin Reuptake Inhibitors
MeSH PA D018490 Serotonin Agents

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

DiseaseRelationSNOMED_IDDOID
Seizures associated with Dravet syndrome indication 230437002
Dravet syndrome indication 230437002
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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL 10478441 May 3, 2033 USE IN COMBINATION WITH STIRIPENTOL FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL 10478442 May 3, 2033 USE IN COMBINATION WITH STIRIPENTOL FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL 9549909 May 3, 2033 USE IN COMBINATION WITH STIRIPENTOL, VALPROATE, AND CLOBAZAM FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL 9603814 May 3, 2033 USE IN COMBINATION WITH STIRIPENTOL, VALPROATE, AND CLOBAZAM FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL 9603815 May 3, 2033 USE IN COMBINATION WITH STIRIPENTOL, VALPROATE, AND CLOBAZAM FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL 9610260 May 3, 2033 USE IN COMBINATION WITH STIRIPENTOL, VALPROATE, AND CLOBAZAM FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL 10603290 Aug. 2, 2037 USE IN COMBINATION WITH CANNABIDIOL FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL 10603290 Aug. 2, 2037 USE IN COMBINATION WITH CANNABIDIOL FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH LENNOX-GASTAUT SYNDROME
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL 11040018 Aug. 2, 2037 USE IN COMBINATION WITH CANNABIDIOL FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL 11040018 Aug. 2, 2037 USE IN COMBINATION WITH CANNABIDIOL FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH LENNOX-GASTAUT SYNDROME
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL 11406606 Aug. 2, 2037 USE OF FENFLURAMINE AT REDUCED AMOUNTS WITH STIRIPENTOL FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL 11406606 Aug. 2, 2037 USE OF FENFLURAMINE AT REDUCED AMOUNTS WITH STIRIPENTOL FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH LENNOX GASTAUT SYNDROME
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL 10452815 June 29, 2038 USE OF CARDIAC MONITORING AND RESTRICTED DISTRIBUTION OF FENFLURAMINE TO MITIGATE RISK OF CARDIOVASCULAR TOXICITY IN THE TREATMENT OF SEIZURES ASSOCIATED WITH DRAVET SYNDROME

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL June 25, 2023 NEW PRODUCT
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL Dec. 25, 2023 PEDIATRIC EXCLUSIVITY
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL March 25, 2025 INDICATION FOR THE TREATMENT OF SEIZURES ASSOCIATED WITH LENNOX-GASTAUT SYNDROME (LGS) IN PATIENTS WHO ARE 2 YEARS OF AGE AND OLDER
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL Sept. 25, 2025 PEDIATRIC EXCLUSIVITY
EQ 2.2MG BASE/ML FINTEPLA UCB 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
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL Dec. 25, 2027 PEDIATRIC EXCLUSIVITY
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL March 25, 2029 TREATMENT OF SEIZURES ASSOCIATED WITH LENNOX-GASTAUT SYNDROME (LGS) IN PATIENTS 2 YEARS OF AGE AND OLDER
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL Sept. 25, 2029 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Muscarinic acetylcholine receptor M4 GPCR Ki 5.17 PDSP
Beta-1 adrenergic receptor GPCR Ki 6.00 PDSP
Beta-2 adrenergic receptor GPCR Ki 5.11 PDSP
Alpha-2A adrenergic receptor GPCR Ki 6.43 PDSP
Sodium-dependent serotonin transporter Transporter Ki 6.18 PDSP
5-hydroxytryptamine receptor 1A GPCR Ki 6.17 PDSP
5-hydroxytryptamine receptor 2A GPCR Ki 5.85 PDSP
5-hydroxytryptamine receptor 2B GPCR Ki 6.40 PDSP
5-hydroxytryptamine receptor 2C GPCR Ki 5.79 PDSP
5-hydroxytryptamine receptor 6 GPCR Ki 5.04 PDSP
5-hydroxytryptamine receptor 7 GPCR Ki 5.38 PDSP
Alpha-1A adrenergic receptor GPCR Ki 6.57 PDSP
Alpha-2B adrenergic receptor GPCR Ki 6.72 PDSP
Muscarinic acetylcholine receptor M1 GPCR Ki 6.02 PDSP
Muscarinic acetylcholine receptor M2 GPCR Ki 5.73 PDSP
Muscarinic acetylcholine receptor M3 GPCR Ki 5.49 PDSP
5-hydroxytryptamine receptor 1B GPCR Ki 5.74 PDSP
5-hydroxytryptamine receptor 1D GPCR Ki 6.20 PDSP
Alpha-2C adrenergic receptor GPCR Ki 6.74 PDSP
Alpha-1B adrenergic receptor GPCR Ki 6.85 PDSP
Sodium-dependent serotonin transporter Transporter EC50 6.97 CHEMBL

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
DB00574 DRUGBANK_ID
D005277 MESH_DESCRIPTOR_UI
3337 PUBCHEM_CID
4613 IUPHAR_LIGAND_ID
1596 INN_ID
2DS058H2CF UNII
202366 RXNORM
1756 MMSL
335891 MMSL
38581 MMSL
4717 MMSL
d00812 MMSL
001873 NDDF
004776 NDDF
387262004 SNOMEDCT_US
387451002 SNOMEDCT_US
78700004 SNOMEDCT_US
CHEMBL2106217 ChEMBL_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
FINTEPLA HUMAN PRESCRIPTION DRUG LABEL 1 43376-322 SOLUTION 2.20 mg ORAL NDA 36 sections
FINTEPLA HUMAN PRESCRIPTION DRUG LABEL 1 43376-322 SOLUTION 2.20 mg ORAL NDA 36 sections
FINTEPLA HUMAN PRESCRIPTION DRUG LABEL 1 43376-322 SOLUTION 2.20 mg ORAL NDA 36 sections
FINTEPLA HUMAN PRESCRIPTION DRUG LABEL 1 43376-322 SOLUTION 2.20 mg ORAL NDA 36 sections