fenfluramine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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
14 mg O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 80.50 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK3,MAPK10,MAPK7,MET,NTRK2,PDK2,PDK4,PIK3CG,PRKDC,TEK,TGFBR1 24
kinase-selectivity-class AXL,EIF2AK3,EPHB4,PDK4 4
pfas-class PFAS structural alert (1 = True, 0 = False) 1
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1

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 493.64 65.26 162 1629 152467 90474189
Tricuspid valve incompetence 253.40 65.26 60 1731 16671 90609985
Petit mal epilepsy 189.00 65.26 38 1753 4920 90621736
Off label use 180.18 65.26 157 1634 1102095 89524561
Mitral valve incompetence 127.37 65.26 37 1754 22487 90604169
Epilepsy 109.98 65.26 46 1745 82160 90544496
Tonic convulsion 107.49 65.26 20 1771 1718 90624938
Pulmonary valve incompetence 101.77 65.26 19 1772 1662 90624994
Mitral valve thickening 99.54 65.26 12 1779 44 90626612
Generalised tonic-clonic seizure 99.53 65.26 34 1757 34869 90591787
Echocardiogram abnormal 83.74 65.26 16 1775 1583 90625073
Aortic valve incompetence 75.81 65.26 19 1772 6605 90620051
Decreased appetite 75.59 65.26 61 1730 376479 90250177
Somnolence 71.93 65.26 47 1744 209037 90417619
Seizure cluster 68.97 65.26 11 1780 378 90626278
Status epilepticus 68.20 65.26 22 1769 18852 90607804
Drug ineffective 68.12 65.26 107 1684 1384191 89242465
Atonic seizures 67.40 65.26 12 1779 804 90625852

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 335.78 69.20 137 1517 120424 42499257
Tricuspid valve incompetence 257.66 69.20 64 1590 11049 42608632
Pulmonary valve incompetence 171.83 69.20 31 1623 1132 42618549
Mitral valve incompetence 164.93 69.20 49 1605 16440 42603241
Off label use 133.23 69.20 141 1513 638194 41981487
Prescribed underdose 117.88 69.20 34 1620 10248 42609433
Aortic valve incompetence 113.66 69.20 30 1624 6518 42613163
Epilepsy 108.41 69.20 40 1614 26131 42593550
Tonic convulsion 100.73 69.20 21 1633 1638 42618043
Generalised tonic-clonic seizure 86.46 69.20 34 1620 26345 42593336
Seizure cluster 78.13 69.20 13 1641 291 42619390
Drug ineffective 75.99 69.20 106 1548 630091 41989590

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
Tricuspid valve incompetence 1974.31 65.69 408 5316 23465 110560110
Mitral valve incompetence 951.24 65.69 240 5484 33089 110550486
Seizure 834.06 65.69 340 5384 220845 110362730
Pulmonary valve incompetence 829.93 65.69 140 5584 2546 110581029
Mitral valve thickening 551.99 65.69 83 5641 686 110582889
Aortic valve incompetence 486.72 65.69 113 5611 10868 110572707
Prescribed underdose 375.41 65.69 137 5587 65037 110518538
Epilepsy 375.33 65.69 154 5570 100055 110483520
Aortic valve thickening 300.70 65.69 42 5682 191 110583384
Off label use 273.87 65.69 358 5366 1499827 109083748
Echocardiogram abnormal 209.83 65.69 44 5680 2630 110580945
Seizure cluster 206.34 65.69 36 5688 797 110582778
Petit mal epilepsy 202.97 65.69 52 5672 7495 110576080
Aortic dilatation 199.75 65.69 41 5683 2205 110581370
Somnolence 181.38 65.69 138 5586 297311 110286264
Vagal nerve stimulator implantation 164.23 65.69 25 5699 225 110583350
Generalised tonic-clonic seizure 161.02 65.69 71 5653 54609 110528966
Decreased appetite 148.86 65.69 151 5573 475695 110107880
Tonic convulsion 143.30 65.69 33 5691 3041 110580534
Status epilepticus 122.89 65.69 50 5674 31521 110552054
Atonic seizures 114.03 65.69 23 5701 1131 110582444
Mitral valve prolapse 102.72 65.69 24 5700 2354 110581221
Myoclonic epilepsy 99.77 65.69 24 5700 2667 110580908
Hospitalisation 86.32 65.69 66 5658 142427 110441148
Weight decreased 82.84 65.69 111 5613 467946 110115629
Behaviour disorder 81.30 65.69 27 5697 9620 110573955
Pericardial effusion 80.56 65.69 45 5679 57172 110526403
Cardiac valve disease 79.09 65.69 24 5700 6397 110577178
Aggression 76.44 65.69 44 5680 59166 110524409
Medical device battery replacement 73.59 65.69 9 5715 9 110583566
Multiple-drug resistance 72.95 65.69 27 5697 13208 110570367
Tricuspid valve thickening 71.47 65.69 10 5714 46 110583529

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
MeSH PA D014179 Neurotransmitter Uptake Inhibitors
MeSH PA D017367 Selective Serotonin Reuptake Inhibitors
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018490 Serotonin Agents
MeSH PA D049990 Membrane Transport Modulators
CHEBI has role CHEBI:35623 anticonvulsant
CHEBI has role CHEBI:35941 serotonergic agonist
CHEBI has role CHEBI:50507 appetite depressant
CHEBI has role CHEBI:50949 serotonin uptake inhibitor
CHEBI has role CHEBI:53784 antispasmodic drug
CHEBI has role CHEBI:74518 anti-obesity agent

Related Drugs by ATC class:

A08AA Centrally acting antiobesity products 15 drugs
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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 12097206 May 3, 2033 A METHOD OF ADJUNCTIVE TREATING, PREVENTING AND/OR AMELIORATING SEIZURES IN A PERSON WITH DRAVET SYNDROME COMPRISING ADMINISTERING FENFLURAMINE OR A SALT THEREOF IN A DOSE OF 0.2 MG/KG/DAY TO 0.5/MG/KG/DAY AND DOSES OF STIRIPENTOL AND CLOBAZAM
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 11759440 Aug. 2, 2037 METHOD OF REDUCING OR AMELIORATING SEIZURES IN A PATIENT BY ADMINISTERING A LIQUID FORMULATION OF FENFLURAMINE WITH STIRIPENTOL THEREBY MODULATING DOWN THE FORMATION OF NORFENFLURAMINE AND RESULTING IN HIGHER LEVELS OF FENFLURAMINE
EQ 2.2MG BASE/ML FINTEPLA UCB INC N212102 June 25, 2020 RX SOLUTION ORAL 11786487 Aug. 2, 2037 METHOD OF TREATING SEIZURES IN A PATIENT BY ADMINISTERING A LIQUID FORMULATION OF FENFLURAMINE OR ITS SALTS PLUS STIRIPENTOL THEREBY REDUCING NORFENFLURAMINE FORMATION WHILE INCREASING THE FENFLURAMINE LEVEL. PATIENTS CAN HAVE E.G. DRAVET OR LGS
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, 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
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
Muscarinic acetylcholine receptor M4 GPCR Ki 5.17 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
4018420 VANDF
4019754 VANDF
C0015827 UMLSCUI
CHEBI:5000 CHEBI
CHEMBL87493 ChEMBL_ID
DB00574 DRUGBANK_ID
CHEMBL2106217 ChEMBL_ID
D005277 MESH_DESCRIPTOR_UI
3337 PUBCHEM_CID
4613 IUPHAR_LIGAND_ID
1596 INN_ID
404-82-0 SECONDARY_CAS_RN
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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Fintepla HUMAN PRESCRIPTION DRUG LABEL 1 43376-322 SOLUTION 2.20 mg ORAL NDA 35 sections
Fintepla HUMAN PRESCRIPTION DRUG LABEL 1 43376-322 SOLUTION 2.20 mg ORAL NDA 35 sections