All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Stem definition	Drug id	CAS RN
anorexics	1150	458-24-2

Description:

Molecule

Description

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:

Dose	Unit	Route
0.12	g	O
14	mg	O

ADMET properties:

Property	Value	Reference
BA (Bioavailability)	80.50 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
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:

Date	Agency	Company	Orphan
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 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
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 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
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 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
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:

Source	Code	Description
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:

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

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (acidic/basic)
pKa1	9.22	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN		Ki	6.00		PDSP
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Ki	5.11		PDSP
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.43		PDSP
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	6.18		PDSP
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	6.17		PDSP
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	5.85		PDSP
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	6.40		PDSP
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	5.79		PDSP
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	5.04		PDSP
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	5.38		PDSP
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	6.57		PDSP
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.72		PDSP
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	6.02		PDSP
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	5.73		PDSP
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	5.49		PDSP
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	5.17		PDSP
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN		Ki	5.74		PDSP
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN		Ki	6.20		PDSP
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	6.74		PDSP
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		Ki	6.85		PDSP
Sodium-dependent serotonin transporter	Transporter		SC6A4_RAT		EC50	6.97		CHEMBL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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