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deferiprone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 4188 | 30652-11-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 25, 1999 | EMA | APOTEX EUROPE BV | |
| Oct. 14, 2011 | FDA | APOPHARMA INC |
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 |
|---|---|---|---|---|---|---|
| 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 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 |
|---|---|---|---|---|---|---|
| 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 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 |
|---|---|---|---|---|---|---|
| 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:
| Source | Code | Description |
|---|---|---|
| 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|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.54 | acidic |
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |