Details
Stereochemistry | ACHIRAL |
Molecular Formula | C7H9NO2 |
Molecular Weight | 139.1519 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C=CC(=O)C(O)=C1C
InChI
InChIKey=TZXKOCQBRNJULO-UHFFFAOYSA-N
InChI=1S/C7H9NO2/c1-5-7(10)6(9)3-4-8(5)2/h3-4,10H,1-2H3
Molecular Formula | C7H9NO2 |
Molecular Weight | 139.1519 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including https://pubchem.ncbi.nlm.nih.gov/compound/deferiprone#section=Top; http://www.ncbi.nlm.nih.gov/pubmed/12825969
Curator's Comment: description was created based on several sources, including https://pubchem.ncbi.nlm.nih.gov/compound/deferiprone#section=Top; http://www.ncbi.nlm.nih.gov/pubmed/12825969
Deferiprone (trade name Ferriprox) is an iron chelator indicated for the treatment of patients with transfusional iron overload due to thalassemia syndromes when current chelation therapy is inadequate. Deferiprone is an orally bioavailable bidentate ligand with iron chelating activity. Deferiprone binds to iron in a 3:1 (ligand:iron) molar ratio. By binding to iron, deferiprone is able to remove excess iron from the body. All the adverse effects of deferiprone are considered reversible, controllable and manageable. These include agranulocytosis with frequency of about 0.6%, neutropenia 6%, musculoskeletal and joint pains 15%, gastrointestinal complains 6% and zinc deficiency 1%.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2363058 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Secondary | FERRIPROX Approved UseIndicated for the treatment of patients with transfusional iron overload due to thalassemia syndromes when current chelation therapy is inadequate. Approval is based on a reduction in serum ferritin levels. There are no controlled trials demonstrating a direct treatment benefit, such as improvement in disease-related symptoms, functioning, or increased survival Launch Date2011 |
|||
Primary | FERRIPROX Approved UseIndicated for the treatment of patients with transfusional iron overload due to thalassemia syndromes when current chelation therapy is inadequate. Approval is based on a reduction in serum ferritin levels. There are no controlled trials demonstrating a direct treatment benefit, such as improvement in disease-related symptoms, functioning, or increased survival. Safety and effectiveness have not been established for the treatment of transfusional iron overload in patients with other chronic anemias. Launch Date2011 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
33.4 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01770652 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE serum | Homo sapiens |
|
43.3 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01770652 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE serum | Homo sapiens |
|
30.6 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01770652 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE serum | Homo sapiens |
|
60.8 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01770652 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE 3-O-BETA-D-GLUCURONIDE serum | Homo sapiens |
|
118.8 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01770652 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE 3-O-BETA-D-GLUCURONIDE serum | Homo sapiens |
|
150.8 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01770652 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE 3-O-BETA-D-GLUCURONIDE serum | Homo sapiens |
|
34.1 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01860703 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE plasma | Homo sapiens population: healthy age: sex: food status: |
|
35.2 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01860703 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE 3-O-BETA-D-GLUCURONIDE plasma | Homo sapiens population: healthy age: sex: food status: |
|
54.4 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01860703 |
50 mg/kg single, oral dose: 50 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE plasma | Homo sapiens population: healthy age: sex: food status: |
|
51.4 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01860703 |
50 mg/kg single, oral dose: 50 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE 3-O-BETA-D-GLUCURONIDE plasma | Homo sapiens population: healthy age: sex: food status: |
|
64.8 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27975237/ |
25 mg/kg single, oral dose: 25 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
DEFERIPRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
95.4 ug*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01860703 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE plasma | Homo sapiens population: healthy age: sex: food status: |
|
205.5 ug*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01860703 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE 3-O-BETA-D-GLUCURONIDE plasma | Homo sapiens population: healthy age: sex: food status: |
|
152.1 ug*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01860703 |
50 mg/kg single, oral dose: 50 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE plasma | Homo sapiens population: healthy age: sex: food status: |
|
331.2 ug*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01860703 |
50 mg/kg single, oral dose: 50 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE 3-O-BETA-D-GLUCURONIDE plasma | Homo sapiens population: healthy age: sex: food status: |
|
15001 μM × min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27975237/ |
25 mg/kg single, oral dose: 25 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
DEFERIPRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.77 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01770652 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE serum | Homo sapiens |
|
2.03 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01770652 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE serum | Homo sapiens |
|
2.2 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01770652 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE serum | Homo sapiens |
|
2.58 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01770652 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE 3-O-BETA-D-GLUCURONIDE serum | Homo sapiens |
|
2.58 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01770652 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE 3-O-BETA-D-GLUCURONIDE serum | Homo sapiens |
|
3.35 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01770652 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE 3-O-BETA-D-GLUCURONIDE serum | Homo sapiens |
|
1.8 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01860703 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE plasma | Homo sapiens population: healthy age: sex: food status: |
|
2.5 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01860703 |
33 mg/kg single, oral dose: 33 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE 3-O-BETA-D-GLUCURONIDE plasma | Homo sapiens population: healthy age: sex: food status: |
|
1.8 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01860703 |
50 mg/kg single, oral dose: 50 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE plasma | Homo sapiens population: healthy age: sex: food status: |
|
2.6 h Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01860703 |
50 mg/kg single, oral dose: 50 mg/kg route of administration: oral experiment type: single co-administered: |
DEFERIPRONE 3-O-BETA-D-GLUCURONIDE plasma | Homo sapiens population: healthy age: sex: food status: |
|
168 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27975237/ |
25 mg/kg single, oral dose: 25 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
DEFERIPRONE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
30 mg/kg 2 times / day multiple, oral Recommended Dose: 30 mg/kg, 2 times / day Route: oral Route: multiple Dose: 30 mg/kg, 2 times / day Sources: |
unhealthy, 29–71 |
Disc. AE: Neutropenic sepsis, Fatigue... AEs leading to discontinuation/dose reduction: Neutropenic sepsis (30%) Sources: Fatigue (10%) |
100 mg/kg multiple, oral Recommended Dose: 100 mg/kg Route: oral Route: multiple Dose: 100 mg/kg Sources: |
unhealthy |
Disc. AE: Arthralgia, Joint effusion... AEs leading to discontinuation/dose reduction: Arthralgia (non-serious) Sources: Joint effusion (non-serious) Nausea (non-serious) Abdominal discomfort (non-serious) Fatigue (non-serious) Joint swelling (non-serious) Epistaxis (non-serious) Upper respiratory tract infections (non-serious) Upper abdominal pain (non-serious) Vomiting (non-serious) Palpitation (non-serious) |
33 mg/kg 3 times / day multiple, oral Recommended Dose: 33 mg/kg, 3 times / day Route: oral Route: multiple Dose: 33 mg/kg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Disc. AE: Agranulocytosis, Fetal damage... AEs leading to discontinuation/dose reduction: Agranulocytosis (grade 3-5) Sources: Fetal damage |
33 mg/kg 3 times / day multiple, oral Recommended Dose: 33 mg/kg, 3 times / day Route: oral Route: multiple Dose: 33 mg/kg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Disc. AE: Aspartate aminotransferase increased, Alanine aminotransferase increased... AEs leading to discontinuation/dose reduction: Aspartate aminotransferase increased (0.78%) Sources: Alanine aminotransferase increased (0.16%) |
33 mg/kg 3 times / day multiple, oral Recommended Dose: 33 mg/kg, 3 times / day Route: oral Route: multiple Dose: 33 mg/kg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Disc. AE: Nausea, Vomiting... AEs leading to discontinuation/dose reduction: Nausea (1.6%) Sources: Vomiting (1.6%) Abdominal pain (1.6%) |
15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Other AEs: Neutropenia, Intestinal dilatation... Other AEs: Neutropenia (serious, 5 patients) Sources: Intestinal dilatation (serious, 1 patient) Intestinal obstruction (serious, 1 patient) Volvulus (serious, 1 patient) Obstruction (serious, 1 patient) Pyrexia (serious, 1 patient) Bacterial disease carrier (serious, 1 patient) Bronchitis (serious, 2 patients) Device related infection (serious, 1 patient) Pneumonia (serious, 2 patients) Wound infection (serious, 1 patient) Chemical eye injury (serious, 1 patient) Postoperative ileus (serious, 1 patient) Toxicity to various agents (serious, 1 patient) Unintentional medical device removal (serious, 1 patient) Oromandibular dystonia (serious, 1 patient) Device malfunction (serious, 1 patient) Urinary bladder rupture (serious, 1 patient) Choking (serious, 1 patient) Cough (serious, 1 patient) Respiratory disorder (serious, 1 patient) Colectomy (serious, 1 patient) Intestinal anastomosis (serious, 1 patient) Intrathecal pump insertion (serious, 1 patient) Laparotomy (serious, 1 patient) Medical device battery replacement (serious, 2 patients) Tracheostomy (serious, 1 patient) Tracheostomy tube removal (serious, 1 patient) Wound treatment (serious, 1 patient) Thrombosis (serious, 1 patient) Anaemia (below serious, 12 patients) Influenza (below serious, 3 patients) Pain (below serious, 4 patients) Bronchitis (below serious, 7 patients) Nasopharyngitis (below serious, 11 patient) Rhinitis (below serious, 4 patients) Upper respiratory tract infection (below serious, 8 patients) Viral infection (below serious, 4 patients) Laceration (below serious, 6 patients) Body temperature increased (below serious, 3 patients) Neutrophil count decreased (below serious, 10 patients) Serum ferritin decreased (below serious, 19 patients) Iron deficiency (below serious, 9 patients) Arthralgia (below serious, 8 patients) Muscle spasms (below serious, 3 patients) Pain in extremity (below serious, 10 patients) Dystonia (below serious, 25 patients) Migraine (below serious, 3 patients) Urinary incontinence (below serious, 3 patients) Cough (below serious, 10 patients) Oropharyngeal pain (below serious, 9 patients) Rhinorrhoea (below serious, 4 patients) Hyperhidrosis (below serious, 3 patients) Rash (below serious, 4 patients) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Fatigue | 10% Disc. AE |
30 mg/kg 2 times / day multiple, oral Recommended Dose: 30 mg/kg, 2 times / day Route: oral Route: multiple Dose: 30 mg/kg, 2 times / day Sources: |
unhealthy, 29–71 |
Neutropenic sepsis | 30% Disc. AE |
30 mg/kg 2 times / day multiple, oral Recommended Dose: 30 mg/kg, 2 times / day Route: oral Route: multiple Dose: 30 mg/kg, 2 times / day Sources: |
unhealthy, 29–71 |
Abdominal discomfort | non-serious Disc. AE |
100 mg/kg multiple, oral Recommended Dose: 100 mg/kg Route: oral Route: multiple Dose: 100 mg/kg Sources: |
unhealthy |
Arthralgia | non-serious Disc. AE |
100 mg/kg multiple, oral Recommended Dose: 100 mg/kg Route: oral Route: multiple Dose: 100 mg/kg Sources: |
unhealthy |
Epistaxis | non-serious Disc. AE |
100 mg/kg multiple, oral Recommended Dose: 100 mg/kg Route: oral Route: multiple Dose: 100 mg/kg Sources: |
unhealthy |
Fatigue | non-serious Disc. AE |
100 mg/kg multiple, oral Recommended Dose: 100 mg/kg Route: oral Route: multiple Dose: 100 mg/kg Sources: |
unhealthy |
Joint effusion | non-serious Disc. AE |
100 mg/kg multiple, oral Recommended Dose: 100 mg/kg Route: oral Route: multiple Dose: 100 mg/kg Sources: |
unhealthy |
Joint swelling | non-serious Disc. AE |
100 mg/kg multiple, oral Recommended Dose: 100 mg/kg Route: oral Route: multiple Dose: 100 mg/kg Sources: |
unhealthy |
Nausea | non-serious Disc. AE |
100 mg/kg multiple, oral Recommended Dose: 100 mg/kg Route: oral Route: multiple Dose: 100 mg/kg Sources: |
unhealthy |
Palpitation | non-serious Disc. AE |
100 mg/kg multiple, oral Recommended Dose: 100 mg/kg Route: oral Route: multiple Dose: 100 mg/kg Sources: |
unhealthy |
Upper abdominal pain | non-serious Disc. AE |
100 mg/kg multiple, oral Recommended Dose: 100 mg/kg Route: oral Route: multiple Dose: 100 mg/kg Sources: |
unhealthy |
Upper respiratory tract infections | non-serious Disc. AE |
100 mg/kg multiple, oral Recommended Dose: 100 mg/kg Route: oral Route: multiple Dose: 100 mg/kg Sources: |
unhealthy |
Vomiting | non-serious Disc. AE |
100 mg/kg multiple, oral Recommended Dose: 100 mg/kg Route: oral Route: multiple Dose: 100 mg/kg Sources: |
unhealthy |
Fetal damage | Disc. AE | 33 mg/kg 3 times / day multiple, oral Recommended Dose: 33 mg/kg, 3 times / day Route: oral Route: multiple Dose: 33 mg/kg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Agranulocytosis | grade 3-5 Disc. AE |
33 mg/kg 3 times / day multiple, oral Recommended Dose: 33 mg/kg, 3 times / day Route: oral Route: multiple Dose: 33 mg/kg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Alanine aminotransferase increased | 0.16% Disc. AE |
33 mg/kg 3 times / day multiple, oral Recommended Dose: 33 mg/kg, 3 times / day Route: oral Route: multiple Dose: 33 mg/kg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Aspartate aminotransferase increased | 0.78% Disc. AE |
33 mg/kg 3 times / day multiple, oral Recommended Dose: 33 mg/kg, 3 times / day Route: oral Route: multiple Dose: 33 mg/kg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Abdominal pain | 1.6% Disc. AE |
33 mg/kg 3 times / day multiple, oral Recommended Dose: 33 mg/kg, 3 times / day Route: oral Route: multiple Dose: 33 mg/kg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Nausea | 1.6% Disc. AE |
33 mg/kg 3 times / day multiple, oral Recommended Dose: 33 mg/kg, 3 times / day Route: oral Route: multiple Dose: 33 mg/kg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Vomiting | 1.6% Disc. AE |
33 mg/kg 3 times / day multiple, oral Recommended Dose: 33 mg/kg, 3 times / day Route: oral Route: multiple Dose: 33 mg/kg, 3 times / day Sources: |
unhealthy Health Status: unhealthy Sources: |
Cough | below serious, 10 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Neutrophil count decreased | below serious, 10 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Pain in extremity | below serious, 10 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Nasopharyngitis | below serious, 11 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Anaemia | below serious, 12 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Serum ferritin decreased | below serious, 19 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Dystonia | below serious, 25 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Body temperature increased | below serious, 3 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Hyperhidrosis | below serious, 3 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Influenza | below serious, 3 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Migraine | below serious, 3 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Muscle spasms | below serious, 3 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Urinary incontinence | below serious, 3 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Pain | below serious, 4 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Rash | below serious, 4 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Rhinitis | below serious, 4 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Rhinorrhoea | below serious, 4 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Viral infection | below serious, 4 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Laceration | below serious, 6 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Bronchitis | below serious, 7 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Arthralgia | below serious, 8 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Upper respiratory tract infection | below serious, 8 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Iron deficiency | below serious, 9 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Oropharyngeal pain | below serious, 9 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Bacterial disease carrier | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Chemical eye injury | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Choking | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Colectomy | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Cough | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Device malfunction | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Device related infection | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Intestinal anastomosis | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Intestinal dilatation | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Intestinal obstruction | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Intrathecal pump insertion | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Laparotomy | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Obstruction | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Oromandibular dystonia | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Postoperative ileus | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Pyrexia | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Respiratory disorder | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Thrombosis | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Toxicity to various agents | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Tracheostomy tube removal | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Tracheostomy | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Unintentional medical device removal | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Urinary bladder rupture | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Volvulus | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Wound infection | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Wound treatment | serious, 1 patient | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Bronchitis | serious, 2 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Medical device battery replacement | serious, 2 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Pneumonia | serious, 2 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Neutropenia | serious, 5 patients | 15 mg/kg 2 times / day steady, oral Dose: 15 mg/kg, 2 times / day Route: oral Route: steady Dose: 15 mg/kg, 2 times / day Sources: |
unhealthy |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/021825Orig1s000ClinPharmR.pdf#page=68 Page: 68.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/021825Orig1s000ClinPharmR.pdf#page=68 Page: 68.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/021825Orig1s000ClinPharmR.pdf#page=68 Page: 68.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/021825Orig1s000ClinPharmR.pdf#page=68 Page: 68.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/021825Orig1s000ClinPharmR.pdf#page=68 Page: 68.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/021825Orig1s000ClinPharmR.pdf#page=68 Page: 68.0 |
no |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 18, 26, 27-28, 31, 33, 41 |
major | |||
minor | ||||
minor | ||||
minor | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes | ||||
yes | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/021825Orig1s000ClinPharmR.pdf#page=73 Page: 73.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Exploring the "iron shuttle" hypothesis in chelation therapy: effects of combined deferoxamine and deferiprone treatment in hypertransfused rats with labeled iron stores and in iron-loaded rat heart cells in culture. | 2001 Aug |
|
Desferrioxamine-chelatable iron, a component of serum non-transferrin-bound iron, used for assessing chelation therapy. | 2001 Feb 1 |
|
Olivieri to testify against Apotex in Europe. | 2001 Jun |
|
[Therapeuetic management of patients with thalassemia major]. | 2001 May |
|
Determination of a new oral iron chelator, ICL670, and its iron complex in plasma by high-performance liquid chromatography and ultraviolet detection. | 2001 May 5 |
|
The Olivieri dispute: no end in sight? | 2002 Feb 19 |
|
I beg to differ. | 2002 Jul 9 |
|
Orally active iron chelators. | 2002 Jun |
|
Deferiprone versus deferoxamine in patients with thalassemia major: a randomized clinical trial. | 2002 Mar-Apr |
|
Iron toxicity and chelation therapy. | 2002 Oct |
|
Iron chelating agents for treating malaria. | 2003 |
|
Synthesis and antiviral evaluation of 3-hydroxy-2-methylpyridin-4-one dideoxynucleoside derivatives. | 2003 Dec 15 |
|
The Olivieri case. | 2003 Feb 27 |
|
The Olivieri case. | 2003 Feb 27 |
|
Patients' health or company profits? The commercialisation of academic research. | 2003 Jan |
|
Deferiprone versus desferrioxamine in thalassaemia, and T2* validation and utility. | 2003 Jan 11 |
|
Iron withdrawal strategies fail to prevent the growth of SiHa-induced tumors in mice. | 2003 Jul |
|
Role of deferiprone in chelation therapy for transfusional iron overload. | 2003 Jul 1 |
|
Pulmonary dysfunction in transfusion-dependent patients with thalassemia major. | 2003 Jul 15 |
|
Potential myocardial iron content evaluation by magnetic resonance imaging in thalassemia major patients treated with Deferoxamine or Deferiprone during a randomized multicenter prospective clinical study. | 2003 May |
|
Signaling role of intracellular iron in NF-kappaB activation. | 2003 May 16 |
|
Labile plasma iron in iron overload: redox activity and susceptibility to chelation. | 2003 Oct 1 |
|
Safety and effectiveness of long-term therapy with the oral iron chelator deferiprone. | 2003 Sep 1 |
|
Bone mass and metabolism in thalassemic children and adolescents treated with different iron-chelating drugs. | 2004 |
Sample Use Guides
25 mg/kg to 33 mg/kg body weight, orally, three times per day, for a total daily dose of 75 mg/kg to 99 mg/kg body weight.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21807124
Proliferating CD4+ T cells from control and RRMS subjects, cultured with or without IL-2, decreased in response to 75 μM deferiprone, although the extent of decreased proliferation of CD4+ T cells from RRMS subjects was less than for control subjects. Proliferating CD8+ T cells from control subjects, cultured with or without IL-2, also decreased in response to 75 μM deferiprone, and this decrease was seen in proliferating CD8+ T cells from RRMS cultured with IL-2.
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:09:00 GMT 2025
by
admin
on
Mon Mar 31 18:09:00 GMT 2025
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Record UNII |
2BTY8KH53L
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
EU-Orphan Drug |
EU/3/10/832
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
|
||
|
NCI_THESAURUS |
C62357
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
|
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FDA ORPHAN DRUG |
340011
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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FDA ORPHAN DRUG |
581217
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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FDA ORPHAN DRUG |
264308
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
|
||
|
EMA ASSESSMENT REPORTS |
FERRIPOX (AUTHORIZED: BETA-THALASSEMIA)
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
|
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|
LIVERTOX |
NBK548086
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
|
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|
FDA ORPHAN DRUG |
150701
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
|
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|
NDF-RT |
N0000175522
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
|
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|
WHO-ATC |
V03AC02
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
|
||
|
WHO-VATC |
QV03AC02
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
DEFERIPRONE
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
|
PRIMARY | |||
|
30652-11-0
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
|
PRIMARY | |||
|
CHEMBL70927
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
|
PRIMARY | |||
|
68554
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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PRIMARY | |||
|
100000085431
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
|
PRIMARY | |||
|
6958
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
|
PRIMARY | |||
|
C044919
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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PRIMARY | |||
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DB08826
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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PRIMARY | |||
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11645
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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PRIMARY | RxNorm | ||
|
m4132
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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PRIMARY | Merck Index | ||
|
7456
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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PRIMARY | |||
|
2BTY8KH53L
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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PRIMARY | |||
|
4188
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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PRIMARY | |||
|
WW-29
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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PRIMARY | |||
|
DTXSID6040666
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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PRIMARY | |||
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SUB06941MIG
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
|
PRIMARY | |||
|
2BTY8KH53L
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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PRIMARY | |||
|
758880
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
|
PRIMARY | |||
|
Deferiprone
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
|
PRIMARY | |||
|
C73030
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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PRIMARY | |||
|
8335
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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PRIMARY | |||
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2972
Created by
admin on Mon Mar 31 18:09:00 GMT 2025 , Edited by admin on Mon Mar 31 18:09:00 GMT 2025
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PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLIC ENZYME -> SUBSTRATE |
MINOR
|
||
|
METABOLIC ENZYME -> SUBSTRATE |
MINOR
|
||
|
TARGET->LIGAND | |||
|
METABOLIC ENZYME -> SUBSTRATE |
MINOR
|
||
|
EXCRETED UNCHANGED |
URINE
|
||
|
BINDER->LIGAND |
BINDING
|
||
|
EXCRETED UNCHANGED |
URINE
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE -> PARENT | |||
|
METABOLITE -> PARENT | |||
|
METABOLITE -> PARENT | |||
|
METABOLITE -> PARENT |
MAJOR
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Volume of Distribution | PHARMACOKINETIC |
|
|
|||
Tmax | PHARMACOKINETIC |
|
SINGLE DOSE IN THE FED STATE |
|
||
Tmax | PHARMACOKINETIC |
|
SINGLE DOSE IN FASTED HEALTHY SUBJECTS |
|
||
Biological Half-life | PHARMACOKINETIC |
|
|
|||