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

Stem definitionDrug idCAS RN
4188 30652-11-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • deferiprone
  • deferione
  • ferriprox
a chelating agent with an affinity for ferric ion (iron III) indicated for the treatment of patients with transfusional iron overload due to thalassemia syndromes
  • Molecular weight: 139.15
  • Formula: C7H9NO2
  • CLOGP: -0.90
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 40.54
  • ALOGS: 0.29
  • ROTB: 0

  • Status: OFP

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

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,ITK,JAK1,JAK2,KIT,MAP3K21,MAP3K7,MAPK12,MAPK7,MAPK9,MARK4,MTOR,NTRK2,PDK1,PDK2,PDPK1,PIK3CB,PIK3CD,PIM2,PLK1,PLK2,PLK3,PLK4,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 52
kinase-selectivity-class ACVR2B,AXL,BRAF,CDK9,DDR1,EIF2AK3,ERBB2,GRK2,MAP2K6,MAPK7,MARK4,SIK2,STK33,TEK 14
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Aug. 25, 1999 EMA APOTEX EUROPE BV
Oct. 14, 2011 FDA APOPHARMA INC

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
Agranulocytosis 264.44 36.85 70 1503 34932 90591942
Sickle cell anaemia with crisis 202.46 36.85 42 1531 7255 90619619
Off label use 111.56 36.85 114 1459 1102138 89524736
Neutropenia 87.30 36.85 52 1521 224852 90402022
Serum ferritin increased 76.23 36.85 19 1554 7362 90619512
Treatment noncompliance 62.61 36.85 26 1547 51701 90575173
Death 60.20 36.85 55 1518 456496 90170378
Neuroleptic malignant syndrome 54.29 36.85 17 1556 15079 90611795

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
Agranulocytosis 164.30 31.83 53 1217 30559 42589506
Death 64.49 31.83 74 1196 471111 42148954
Neutropenia 50.61 31.83 44 1226 199387 42420678
Sickle cell anaemia with crisis 45.60 31.83 13 1257 4877 42615188
Off label use 38.62 31.83 68 1202 638267 41981798
Serum ferritin increased 36.53 31.83 12 1258 7207 42612858

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
Agranulocytosis 391.03 30.77 113 2309 61647 110525230
Sickle cell anaemia with crisis 155.01 30.77 37 2385 9508 110577369
Neutropenia 130.33 30.77 88 2334 374532 110212345
Off label use 126.33 30.77 158 2264 1500027 109086850
Death 122.13 30.77 109 2313 698760 109888117
Serum ferritin increased 76.04 30.77 22 2400 11825 110575052
Treatment noncompliance 71.76 30.77 34 2388 72956 110513921
Neuroleptic malignant syndrome 36.95 30.77 17 2405 34042 110552835
Endocrine disorder 32.59 30.77 7 2415 1117 110585760
Prescribed overdose 31.25 30.77 21 2401 87560 110499317

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC V03AC02 VARIOUS
ALL OTHER THERAPEUTIC PRODUCTS
ALL OTHER THERAPEUTIC PRODUCTS
Iron chelating agents
FDA MoA N0000000144 Iron Chelating Activity
FDA EPC N0000175522 Iron Chelator
MeSH PA D002614 Chelating Agents
MeSH PA D007502 Iron Chelating Agents
MeSH PA D064449 Sequestering Agents
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:38157 iron chelator
CHEBI has role CHEBI:48407 antiparkinson drug
CHEBI has role CHEBI:50267 protective agent
CHEBI has role CHEBI:64946 anti-HIV agent
CHEBI has role CHEBI:75835 anti-anaemic agent
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

V03AC Iron chelating agents 2 drugs

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

DiseaseRelationSNOMED_IDDOID
Iron overload indication 60737008
beta Thalassemia indication 65959000 DOID:12241




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.54 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
100MG/ML FERRIPROX CHIESI N208030 Sept. 9, 2015 RX SOLUTION ORAL 8703156 Oct. 26, 2029 METHOD OF TREATING TRANSFUSIONAL IRON OVERLOAD
80MG/ML FERRIPROX CHIESI N208030 April 20, 2018 DISCN SOLUTION ORAL 8703156 Oct. 26, 2029 METHOD OF TREATING TRANSFUSIONAL IRON OVERLOAD
1GM FERRIPROX CHIESI N212269 May 19, 2020 RX TABLET ORAL 10780055 Oct. 25, 2038 METHOD OF TREATING TRANSFUSIONAL IRON OVERLOAD
1GM FERRIPROX CHIESI N212269 May 19, 2020 RX TABLET ORAL 10940115 Oct. 25, 2038 METHOD OF TREATING TRANSFUSIONAL IRON OVERLOAD
1GM FERRIPROX CHIESI N212269 May 19, 2020 RX TABLET ORAL 11357731 Oct. 25, 2038 METHOD OF TREATING TRANSFUSIONAL IRON OVERLOAD
1GM FERRIPROX CHIESI N212269 May 19, 2020 RX TABLET ORAL 11723874 Oct. 25, 2038 METHOD OF TREATING TRANSFUSIONAL IRON OVERLOAD

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
1GM FERRIPROX CHIESI N021825 July 25, 2019 RX TABLET ORAL April 30, 2028 TREATMENT OF TRANSFUSIONAL IRON OVERLOAD IN ADULT AND PEDIATRIC PATIENTS 8 YEARS OF AGE AND OLDER WITH SICKLE CELL DISEASE OR OTHER ANEMIAS
1GM FERRIPROX CHIESI N021825 July 25, 2019 RX TABLET ORAL April 30, 2028 TREATMENT OF TRANSFUSIONAL IRON OVERLOAD IN ADULT PATIENTS WITH THALASSEMIA SYNDROMES EXCLUDING ADULT PATIENTS COVERED BY THE INDICATION FOR THALASSEMIA SYNDROMES APPROVED ON OCTOBER 14, 2011
1GM FERRIPROX CHIESI N021825 July 25, 2019 RX TABLET ORAL April 30, 2028 TREATMENT OF TRANSFUSIONAL IRON OVERLOAD IN PEDIATRIC PATIENTS 8 YEARS OF AGE AND OLDER WITH THALASSEMIA SYNDROMES
500MG FERRIPROX CHIESI N021825 Oct. 14, 2011 DISCN TABLET ORAL April 30, 2028 TREATMENT OF TRANSFUSIONAL IRON OVERLOAD IN ADULT AND PEDIATRIC PATIENTS 8 YEARS OF AGE AND OLDER WITH SICKLE CELL DISEASE OR OTHER ANEMIAS
500MG FERRIPROX CHIESI N021825 Oct. 14, 2011 DISCN TABLET ORAL April 30, 2028 TREATMENT OF TRANSFUSIONAL IRON OVERLOAD IN ADULT PATIENTS WITH THALASSEMIA SYNDROMES EXCLUDING ADULT PATIENTS COVERED BY THE INDICATION FOR THALASSEMIA SYNDROMES APPROVED ON OCTOBER 14, 2011
500MG FERRIPROX CHIESI N021825 Oct. 14, 2011 DISCN TABLET ORAL April 30, 2028 TREATMENT OF TRANSFUSIONAL IRON OVERLOAD IN PEDIATRIC PATIENTS 8 YEARS OF AGE AND OLDER WITH THALASSEMIA SYNDROMES
100MG/ML FERRIPROX CHIESI N208030 Sept. 9, 2015 RX SOLUTION ORAL April 30, 2028 TREATMENT OF TRANSFUSIONAL IRON OVERLOAD IN ADULT AND PEDIATRIC PATIENTS 3 YEARS OF AGE AND OLDER WITH SICKLE CELL DISEASE OR OTHER ANEMIAS
100MG/ML FERRIPROX CHIESI N208030 Sept. 9, 2015 RX SOLUTION ORAL April 30, 2028 TREATMENT OF TRANSFUSIONAL IRON OVERLOAD IN ADULT PATIENTS WITH THALASSEMIA SYNDROMES EXCLUDING ADULT PATIENTS COVERED BY THE INDICATION FOR THALASSEMIA SYNDROMES APPROVED ON OCTOBER 14, 2011
100MG/ML FERRIPROX CHIESI N208030 Sept. 9, 2015 RX SOLUTION ORAL April 30, 2028 TREATMENT OF TRANSFUSIONAL IRON OVERLOAD IN PEDIATRIC PATIENTS 3 YEARS OF AGE AND OLDER WITH THALASSEMIA SYNDROMES
80MG/ML FERRIPROX CHIESI N208030 April 20, 2018 DISCN SOLUTION ORAL April 30, 2028 TREATMENT OF TRANSFUSIONAL IRON OVERLOAD IN ADULT AND PEDIATRIC PATIENTS 3 YEARS OF AGE AND OLDER WITH SICKLE CELL DISEASE OR OTHER ANEMIAS
80MG/ML FERRIPROX CHIESI N208030 April 20, 2018 DISCN SOLUTION ORAL April 30, 2028 TREATMENT OF TRANSFUSIONAL IRON OVERLOAD IN ADULT PATIENTS WITH THALASSEMIA SYNDROMES EXCLUDING ADULT PATIENTS COVERED BY THE INDICATION FOR THALASSEMIA SYNDROMES APPROVED ON OCTOBER 14, 2011
80MG/ML FERRIPROX CHIESI N208030 April 20, 2018 DISCN SOLUTION ORAL April 30, 2028 TREATMENT OF TRANSFUSIONAL IRON OVERLOAD IN PEDIATRIC PATIENTS 3 YEARS OF AGE AND OLDER WITH THALASSEMIA SYNDROMES
1GM FERRIPROX CHIESI N212269 May 19, 2020 RX TABLET ORAL April 30, 2028 TREATMENT OF TRANSFUSIONAL IRON OVERLOAD IN ADULT AND PEDIATRIC PATIENTS 8 YEARS OF AGE AND OLDER WITH SICKLE CELL DISEASE OR OTHER ANEMIAS
1GM FERRIPROX CHIESI N212269 May 19, 2020 RX TABLET ORAL April 30, 2028 TREATMENT OF TRANSFUSIONAL IRON OVERLOAD IN ADULT PATIENTS WITH THALASSEMIA SYNDROMES EXCLUDING ADULT PATIENTS COVERED BY THE INDICATION FOR THALASSEMIA SYNDROMES APPROVED ON OCTOBER 14, 2011
1GM FERRIPROX CHIESI N212269 May 19, 2020 RX TABLET ORAL April 30, 2028 TREATMENT OF TRANSFUSIONAL IRON OVERLOAD IN PEDIATRIC PATIENTS 8 YEARS OF AGE AND OLDER WITH THALASSEMIA SYNDROMES

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Deoxyhypusine hydroxylase Enzyme IC50 5.30 CHEMBL
Lysine-specific demethylase 6A Enzyme IC50 5.38 CHEMBL
Lysine-specific demethylase 4A Enzyme IC50 5.49 CHEMBL
Lysine-specific demethylase 5C Enzyme IC50 5.25 CHEMBL
Lysine-specific demethylase 2B Enzyme IC50 5.09 CHEMBL
Lysine-specific demethylase 2A Enzyme IC50 5.17 CHEMBL

External reference:

IDSource
4031179 VUID
N0000183921 NUI
D07416 KEGG_DRUG
4031179 VANDF
C0043832 UMLSCUI
CHEBI:68554 CHEBI
CHEMBL70927 ChEMBL_ID
D000077543 MESH_DESCRIPTOR_UI
DB08826 DRUGBANK_ID
7456 IUPHAR_LIGAND_ID
6958 INN_ID
2BTY8KH53L UNII
2972 PUBCHEM_CID
11645 RXNORM
117386 MMSL
18035 MMSL
399943 MMSL
51626 MMSL
d04976 MMSL
007561 NDDF
329482000 SNOMEDCT_US
396011004 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Deferiprone HUMAN PRESCRIPTION DRUG LABEL 1 0054-0576 TABLET, COATED 500 mg ORAL ANDA 28 sections
Deferiprone HUMAN PRESCRIPTION DRUG LABEL 1 0054-0711 TABLET, COATED 1000 mg ORAL ANDA 28 sections
FERRIPROX HUMAN PRESCRIPTION DRUG LABEL 1 10122-100 TABLET, FILM COATED 500 mg ORAL NDA 28 sections
FERRIPROX HUMAN PRESCRIPTION DRUG LABEL 1 10122-100 TABLET, FILM COATED 500 mg ORAL NDA 28 sections
FERRIPROX HUMAN PRESCRIPTION DRUG LABEL 1 10122-101 SOLUTION 100 mg ORAL NDA 29 sections
FERRIPROX HUMAN PRESCRIPTION DRUG LABEL 1 10122-103 TABLET, FILM COATED 1000 mg ORAL NDA 29 sections
FERRIPROX HUMAN PRESCRIPTION DRUG LABEL 1 10122-104 TABLET 1000 mg ORAL NDA 29 sections
Deferiprone HUMAN PRESCRIPTION DRUG LABEL 1 51672-4196 TABLET 500 mg ORAL ANDA 32 sections
Deferiprone HUMAN PRESCRIPTION DRUG LABEL 1 51672-4237 TABLET 1000 mg ORAL ANDA 32 sections
FERRIPROX HUMAN PRESCRIPTION DRUG LABEL 1 52609-0006 TABLET, FILM COATED 500 mg ORAL NDA 28 sections
FERRIPROX HUMAN PRESCRIPTION DRUG LABEL 1 52609-0007 TABLET, FILM COATED 1000 mg ORAL NDA 29 sections
DEFERIPRONE HUMAN PRESCRIPTION DRUG LABEL 1 75907-348 TABLET, COATED 1000 mg ORAL ANDA 25 sections
DEFERIPRONE HUMAN PRESCRIPTION DRUG LABEL 1 75907-349 TABLET, COATED 500 mg ORAL ANDA 25 sections