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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
Structure of DEFERIPRONE

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

HIDE SMILES / InChI

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

Description
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%.

Originator

Curator's Comment: ApoPharma began formal development of deferiprone in 1993 (http://www.fda.gov/ucm/groups/fdagov-public/@fdagov-afda-adcom/documents/document/ucm275607.pdf; http://tircon.eu/tircon-partners/apopharma)

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
FERRIPROX

Approved Use

Indicated 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 Date

2011
Primary
FERRIPROX

Approved Use

Indicated 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 Date

2011
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
33.4 ug/mL
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
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
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
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
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
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
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
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
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
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
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

AUC

ValueDoseCo-administeredAnalytePopulation
95.4 ug*h/mL
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
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
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
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
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

T1/2

ValueDoseCo-administeredAnalytePopulation
1.77 h
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
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
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
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
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
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
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
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
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
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
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

Doses

DosePopulationAdverse 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
Health Status: unhealthy
Age Group: 29–71
Sex: M+F
Sources:
Disc. AE: Neutropenic sepsis, Fatigue...
AEs leading to
discontinuation/dose reduction:
Neutropenic sepsis (30%)
Fatigue (10%)
Sources:
100 mg/kg multiple, oral
Recommended
Dose: 100 mg/kg
Route: oral
Route: multiple
Dose: 100 mg/kg
Sources:
unhealthy
Health Status: unhealthy
Sex: M+F
Sources:
Disc. AE: Arthralgia, Joint effusion...
AEs leading to
discontinuation/dose reduction:
Arthralgia (non-serious)
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)
Sources:
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
Disc. AE: Agranulocytosis, Fetal damage...
AEs leading to
discontinuation/dose reduction:
Agranulocytosis (grade 3-5)
Fetal damage
Sources:
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
Disc. AE: Aspartate aminotransferase increased, Alanine aminotransferase increased...
AEs leading to
discontinuation/dose reduction:
Aspartate aminotransferase increased (0.78%)
Alanine aminotransferase increased (0.16%)
Sources:
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
Disc. AE: Nausea, Vomiting...
AEs leading to
discontinuation/dose reduction:
Nausea (1.6%)
Vomiting (1.6%)
Abdominal pain (1.6%)
Sources:
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
Health Status: unhealthy
Sources:
Other AEs: Neutropenia, Intestinal dilatation...
Other AEs:
Neutropenia (serious, 5 patients)
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)
Sources:
AEs

AEs

AESignificanceDosePopulation
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
Health Status: unhealthy
Age Group: 29–71
Sex: M+F
Sources:
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
Health Status: unhealthy
Age Group: 29–71
Sex: M+F
Sources:
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
Health Status: unhealthy
Sex: M+F
Sources:
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
Health Status: unhealthy
Sex: M+F
Sources:
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
Health Status: unhealthy
Sex: M+F
Sources:
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
Health Status: unhealthy
Sex: M+F
Sources:
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
Health Status: unhealthy
Sex: M+F
Sources:
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
Health Status: unhealthy
Sex: M+F
Sources:
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
Health Status: unhealthy
Sex: M+F
Sources:
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
Health Status: unhealthy
Sex: M+F
Sources:
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
Health Status: unhealthy
Sex: M+F
Sources:
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
Health Status: unhealthy
Sex: M+F
Sources:
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
Health Status: unhealthy
Sex: M+F
Sources:
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
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
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
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
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
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
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
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
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
Health Status: unhealthy
Sources:
Overview

Overview

Drug as perpetrator​Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
minor
minor
minor
no
no
no
no
no
no
no
no
yes
yes
yes
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
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
Patents

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
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 Mon Mar 31 18:09:00 GMT 2025
Edited
by admin
on Mon Mar 31 18:09:00 GMT 2025
Record UNII
2BTY8KH53L
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DEFERIPRONE
DASH   EMA EPAR   INN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
APO-066
Preferred Name English
4(1H)-PYRIDINONE, 3-HYDROXY-1,2-DIMETHYL-
Systematic Name English
DEFERIPRONE [EP MONOGRAPH]
Common Name English
NSC-758880
Code English
L-1
Code English
3-Hydroxy-1,2-dimethylpyridin-4(1H)-one
Systematic Name English
APO-66
Code English
DEFERIPRONE [MART.]
Common Name English
Deferiprone [WHO-DD]
Common Name English
L1
Code English
DEFERIPRONE [ORANGE BOOK]
Common Name English
3-HYDROXY-1,2-DIMETHYL-4(1H)-PYRIDONE
Systematic Name English
deferiprone [INN]
Common Name English
DEFERIPRONE [EMA EPAR]
Common Name English
CP-20
Code English
DN-180-01-AF
Code English
DEFERIPRONE [VANDF]
Common Name English
DN-18001AF
Code English
CP20
Code English
DEFERIPRONE [USAN]
Common Name English
DEFERIPRONE [MI]
Common Name English
DEFERIPRON
Common Name English
PL1
Code English
PL-1
Code English
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
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
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
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
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
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
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
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
Code System Code Type Description
WIKIPEDIA
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
CAS
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
ChEMBL
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
CHEBI
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
PRIMARY
SMS_ID
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
INN
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
MESH
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
PRIMARY
DRUG BANK
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
PRIMARY
RXCUI
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
PRIMARY RxNorm
MERCK INDEX
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
PRIMARY Merck Index
IUPHAR
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
PRIMARY
DAILYMED
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
PRIMARY
DRUG CENTRAL
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
PRIMARY
USAN
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
PRIMARY
EPA CompTox
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
PRIMARY
EVMPD
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
FDA UNII
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
PRIMARY
NSC
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
LACTMED
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
NCI_THESAURUS
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
PRIMARY
HSDB
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
PRIMARY
PUBCHEM
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
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
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