Clofarabine

Highest phase reached

Approved

www.ebi.ac.uk

Drug type

Small molecule

www.ebi.ac.uk

First approval year

2004

www.ebi.ac.uk

First approval year: 2004
www.ebi.ac.uk

Listing at source: Listed

Highest phase reached: Approved
www.ebi.ac.uk

Drug type: Small molecule
www.ebi.ac.uk

Drug name: Clofarabine
www.ebi.ac.uk

Molecular weight: 303.68
www.ebi.ac.uk

Structure (SMILES): Nc1nc(Cl)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@@H]1F
www.ebi.ac.uk

clolar
Clolar
evoltra
Evoltra
ivozall
Ivozall

2 chloro 9 2 deoxy 2 fluoro beta d arabinofuranosyl 9h purin 6 amine
2-CHLORO-9-(2-DEOXY-2-FLUORO-.BETA.-D-ARABINOFURANOSYL)-9H-PURIN-6-AMINE
9h purin 6 amine 2 chloro 9 2 deoxy 2 fluoro beta d arabinofuranosyl
9H-PURIN-6-AMINE, 2-CHLORO-9-(2-DEOXY-2-FLUORO-.BETA.-D-ARABINOFURANOSYL)
bortezomib plus clofarabine
clofarabina
Clofarabina
clofarabine
Clofarabine
CLOFARABINE
clofarabine (IV formulation)
clofarabine (oral formulation)
CLOFARABINE [EMA EPAR]
clofarabine [INN]
CLOFARABINE [JAN]
CLOFARABINE [MART.]
CLOFARABINE [MI]
CLOFARABINE [ORANGE BOOK]
CLOFARABINE [USAN]
CLOFARABINE [VANDF]
Clofarabine [WHO-DD]
clofarabine ema epar
clofarabine inn
clofarabine jan
clofarabine mart

And 8 more, listed on the interactive page.

ATC classification codes

L01BB06

Sources for recorded values

www.ebi.ac.uk

CAS registry numbers

123318-82-1

ChEMBL ID: CHEMBL1750
www.ebi.ac.uk

InChIKey: WDDPHFBMKLOVOX-AYQXTPAHSA-N
www.ebi.ac.uk

PubChem compound IDs

119182

RxNorm IDs (RxCUI)

44151

FDA ingredient codes (UNII)

762RDY0Y2H

Applicant: GENZYME
Approval date: 28 Dec 2004
Application number: NDA021673

Status: Authorised
Status date: 29 May 2006
Authorisation date: 29 May 2006
Approved indications: Treatment of acute lymphoblastic leukaemia (ALL) in paediatric patients who have relapsed or are refractory after receiving at least two prior regimens and where there is no other treatment option anticipated to result in a durable response. Safety and efficacy have been assessed in studies of patients ? 21 years old at initial diagnosis.
Product number: EMEA/H/C/000613
Authorisation holder: Sanofi B.V.
Priority medicines scheme: No
Generic: No
Biosimilar: No
Generic medicines: 0
Biosimilar medicines: 0
Advanced therapy: No
Conditional approval: No
Additional monitoring: Yes
Accelerated assessment: No
Exceptional circumstances: Yes

Therapeutic areas

Precursor Cell Lymphoblastic Leukemia-Lymphoma

European medicines record

www.ema.europa.eu

Patents: 0
Designations: 1
First in class: No
Fast track: No
Breakthrough designation: No
Orphan designation: No
Priority review: No
Orphan exclusivity: No
Accelerated approval: No
Availability: Prescription only

Pharmacology name: clofarabine
Type: Synthetic organic
Drug name stem: -arabine
Approval recorded by Guide to Pharmacology: Yes

Administration routes

Parenteral

Action
Inhibition
Action type
Inhibitor
Target
ribonucleotide reductase catalytic subunit M1
Gene symbol
RRM1
Protein identifier
P23921
Median affinity
8.3
Affinity units
pIC50
Action
Inhibition
Action type
Inhibitor
Target
ribonucleotide reductase regulatory subunit M2
Gene symbol
RRM2
Protein identifier
P31350
Median affinity
8.3
Affinity units
pIC50
Primary target
Yes
Mechanism
DNA inhibitor
Action type
Inhibitor
Target
DNA
Mechanism
DNA polymerase (alpha/delta/epsilon) inhibitor
Action type
Inhibitor
Target
DNA polymerase (alpha/delta/epsilon)
Protein identifier
P09884
Mechanism
DNA polymerase (alpha/delta/epsilon) inhibitor
Action type
Inhibitor
Target
DNA polymerase (alpha/delta/epsilon)
Protein identifier
P28340
Mechanism
DNA polymerase (alpha/delta/epsilon) inhibitor
Action type
Inhibitor
Target
DNA polymerase (alpha/delta/epsilon)
Protein identifier
P49005
Mechanism
DNA polymerase (alpha/delta/epsilon) inhibitor
Action type
Inhibitor
Target
DNA polymerase (alpha/delta/epsilon)
Protein identifier
P49642
Mechanism
DNA polymerase (alpha/delta/epsilon) inhibitor
Action type
Inhibitor
Target
DNA polymerase (alpha/delta/epsilon)
Protein identifier
P49643
Mechanism
DNA polymerase (alpha/delta/epsilon) inhibitor
Action type
Inhibitor
Target
DNA polymerase (alpha/delta/epsilon)
Protein identifier
P56282
Mechanism
DNA polymerase (alpha/delta/epsilon) inhibitor
Action type
Inhibitor
Target
DNA polymerase (alpha/delta/epsilon)
Protein identifier
Q07864
Mechanism
DNA polymerase (alpha/delta/epsilon) inhibitor
Action type
Inhibitor
Target
DNA polymerase (alpha/delta/epsilon)
Protein identifier
Q14181
Mechanism
DNA polymerase (alpha/delta/epsilon) inhibitor
Action type
Inhibitor
Target
DNA polymerase (alpha/delta/epsilon)
Protein identifier
Q15054
Mechanism
DNA polymerase (alpha/delta/epsilon) inhibitor
Action type
Inhibitor
Target
DNA polymerase (alpha/delta/epsilon)
Protein identifier
Q9HCU8
Mechanism
DNA polymerase (alpha/delta/epsilon) inhibitor
Action type
Inhibitor
Target
DNA polymerase (alpha/delta/epsilon)
Protein identifier
Q9NRF9
Mechanism
Ribonucleoside-diphosphate reductase RR1 inhibitor
Action type
Inhibitor
Target
Ribonucleoside-diphosphate reductase RR1
Protein identifier
P23921
Mechanism
Ribonucleoside-diphosphate reductase RR1 inhibitor
Action type
Inhibitor
Target
Ribonucleoside-diphosphate reductase RR1
Protein identifier
P31350
Mechanism
Ribonucleoside-diphosphate reductase RR1 inhibitor
Action type
Inhibitor
Target
Ribonucleoside-diphosphate reductase RR1
Protein identifier
Q7LG56

Mechanism
DNA polymerase (alpha/delta/epsilon) inhibitor
Action type
Inhibitor
Target
DNA polymerase (alpha/delta/epsilon)
Mechanism
Ribonucleoside-diphosphate reductase RR1 inhibitor
Action type
Inhibitor
Target
Ribonucleoside-diphosphate reductase RR1

Action type
Inhibitor
Gene symbol
POLA1
Protein identifier
P09884
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
RRM1
Protein identifier
P23921
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
RRM2
Protein identifier
P31350
Organism
Homo sapiens
Target development level
Clinical

Condition
Leukemia, Lymphocytic, Chronic, B-Cell
Highest recorded phase
2
Condition identifier
EFO:0000095
Subject identifier
D015451
Condition
Lymphoma, Follicular
Highest recorded phase
1
Condition identifier
EFO:0000096
Subject identifier
D008224
Condition
Hodgkin Disease
Highest recorded phase
2
Condition identifier
EFO:0000183
Subject identifier
D006689
Condition
Myelodysplastic Syndromes
Highest recorded phase
2
Condition identifier
EFO:0000198
Subject identifier
D009190
Condition
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Highest recorded phase
4
Condition identifier
EFO:0000220
Subject identifier
D054198
Condition
Leukemia, Myeloid, Acute
Highest recorded phase
3
Condition identifier
EFO:0000222
Subject identifier
D015470
Condition
Leukemia, Promyelocytic, Acute
Highest recorded phase
1
Condition identifier
EFO:0000224
Subject identifier
D015473
Condition
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Highest recorded phase
2
Condition identifier
EFO:0000339
Subject identifier
D015464
Condition
Leukemia
Highest recorded phase
3
Condition identifier
EFO:0000565
Subject identifier
D007938
Condition
Lymphoma
Highest recorded phase
2
Condition identifier
EFO:0000574
Subject identifier
D008223
Condition
Neoplasms
Highest recorded phase
4
Condition identifier
EFO:0000616
Subject identifier
D009369
Condition
Multiple Myeloma
Highest recorded phase
2
Condition identifier
EFO:0001378
Subject identifier
D009101
Condition
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Highest recorded phase
4
Condition identifier
EFO:0004289
Subject identifier
D054198
Condition
Hematologic Diseases
Highest recorded phase
2
Condition identifier
EFO:0005803
Subject identifier
D006402
Condition
Lymphoma, Non-Hodgkin
Highest recorded phase
2
Condition identifier
EFO:0005952
Subject identifier
D008228
Condition
Histiocytosis, Langerhans-Cell
Highest recorded phase
2
Condition identifier
EFO:1000318
Subject identifier
D006646
Condition
Leukemia, Myelomonocytic, Chronic
Highest recorded phase
2
Condition identifier
EFO:1001779
Subject identifier
D015477
Condition
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Highest recorded phase
4
Condition identifier
MONDO:0000873
Subject identifier
D054198
Condition
Neoplasms
Highest recorded phase
4
Condition identifier
MONDO:0004992
Subject identifier
D009369
Condition
Graft vs Host Disease
Highest recorded phase
2
Condition identifier
MONDO:0013730
Subject identifier
D006086
Condition
Osteopetrosis
Highest recorded phase
2
Condition identifier
MONDO:0017198
Subject identifier
D010022
Condition
Leukemia, Biphenotypic, Acute
Highest recorded phase
2
Condition identifier
MONDO:0019460
Subject identifier
D015456

Condition identifier
EFO_0000095
Highest recorded phase
1
Condition identifier
EFO_0000096
Highest recorded phase
1
Condition identifier
EFO_0000198
Condition identifier
EFO_0000220
Condition identifier
EFO_0000222
Highest recorded phase
3
Condition identifier
EFO_0000565
Condition identifier
EFO_0000574
Highest recorded phase
2
Condition identifier
EFO_0000616
Condition identifier
EFO_0001378
Highest recorded phase
2
Condition identifier
EFO_0004251
Highest recorded phase
1
Condition identifier
EFO_0005952
Highest recorded phase
2
Condition identifier
EFO_1000318
Highest recorded phase
2
Condition identifier
EFO_1001779
Highest recorded phase
2
Condition identifier
HP_0002863
Highest recorded phase
2
Condition identifier
MONDO_0000814
Highest recorded phase
2
Condition identifier
MONDO_0000872
Highest recorded phase
2
Condition identifier
MONDO_0000873
Highest recorded phase
2
Condition identifier
MONDO_0002280
Highest recorded phase
2
Condition identifier
MONDO_0002561
Condition identifier
MONDO_0003539
Highest recorded phase
2
Condition identifier
MONDO_0004948
Highest recorded phase
1
Condition identifier
MONDO_0004952
Highest recorded phase
1
Condition identifier
MONDO_0004963
Highest recorded phase
2
Condition identifier
MONDO_0004967
Highest recorded phase
4
Condition identifier
MONDO_0004992
Highest recorded phase
2

And 35 more, listed on the interactive page.

Event
acute graft versus host disease
Reports
11
Reporting signal score
25.1867
Event
acute graft versus host disease in liver
Reports
5
Reporting signal score
18.0592
Event
acute graft versus host disease in skin
Reports
12
Reporting signal score
35.5834
Event
acute lymphocytic leukaemia recurrent
Reports
13
Reporting signal score
42.7711
Event
acute myeloid leukaemia
Reports
11
Reporting signal score
17.1446
Event
acute myeloid leukaemia recurrent
Reports
13
Reporting signal score
52.884
Event
adenovirus infection
Reports
8
Reporting signal score
21.1961
Event
alanine aminotransferase increased
Reports
100
Reporting signal score
172.111
Event
alpha haemolytic streptococcal infection
Reports
9
Reporting signal score
34.3108
Event
aplasia
Reports
12
Reporting signal score
35.4328
Event
aspartate aminotransferase increased
Reports
95
Reporting signal score
169.246
Event
bacteraemia
Reports
15
Reporting signal score
25.1966
Event
bacterial infection
Reports
15
Reporting signal score
24.9462
Event
blood bilirubin increased
Reports
68
Reporting signal score
151.351
Event
blood culture positive
Reports
17
Reporting signal score
51.0381
Event
bone marrow failure
Reports
52
Reporting signal score
107.971
Event
bronchopulmonary aspergillosis
Reports
13
Reporting signal score
28.883
Event
caecitis
Reports
8
Reporting signal score
32.362
Event
capillary leak syndrome
Reports
29
Reporting signal score
114.75
Event
cystitis haemorrhagic
Reports
27
Reporting signal score
88.6079
Event
cytomegalovirus infection
Reports
25
Reporting signal score
45.4768
Event
decreased appetite
Reports
41
Reporting signal score
19.3701
Event
demodicidosis
Reports
4
Reporting signal score
19.0907
Event
disseminated intravascular coagulation
Reports
13
Reporting signal score
21.4485
Event
dizziness
Reports
3
Reporting signal score
22.9647

And 51 more, listed on the interactive page.

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And 78 more, listed on the interactive page.

Dose: 52 mg/m2
Route: Intravenous
How often: Daily for 5 consecutive days

Administer over 2 hours
No other medication through same line
Use within 24 hours of preparation

Hydrogen bond acceptors: 8
Hydrogen bond donors: 3
Polar surface area: 119.31
Calculated partition coefficient (ALogP): -0.35
Calculated partition coefficient (XLogP): 0.9
Prodrug: Yes
Chirality: Single enantiomer
Inorganic: No
Rule-of-five violations: 0
Rotatable bonds: 2
Heavy atoms: 20
Molecular formula: C10H11ClFN5O3
Monoisotopic mass: 303.0534451
Natural product: No

43598-309
49315-003
55150-326
63323-572
68083-386
71288-128
72205-394
72266-108
70121-1236

Recorded assays: 953
Active assays: 191

Confirmatory
Other
Screening
Summary

Antimetabolites, Antineoplastic
id.nlm.nih.gov

Oral bioavailability

Median: 57
Mean: 57
Minimum: 57
Maximum: 57
Unit: %
Assays: 1
Standard deviation: 0
Summary method: median
Censored results excluded: 0
Other units excluded: 0
Unknown units excluded: 0

Measurement types

Related records

Trials (337)

2 Arm Study of Clofarabine IV in MDS Patients
A 6-Part Study In Healthy Volunteers To Evaluate Safety, Tolerability and Uptake Of MEDI7219 in the Body When Given as Single and Multiple Doses
A Clinical Trial of CSL's 2010/2011 Formulation of Enzira® in a Healthy Adult Population
A Clinical Trial of MK-1403 in Healthy Participants (MK-1403-007)
A Clinical Trial of Multiple Formulations of MK-4082 in Healthy Overweight and Obese Participants (MK-4082-007)
A Clinical Trial of SIBP-A13 Injection in the Treatment of Advanced Malignant Solid Tumor Patients.
A Dose Confirmation Study of Oral Clofarabine for Adult Patients Previously Treated for Myelodysplastic Syndromes (MDS)
A Healthy Volunteer Study to Investigate the Relative Bioavailability of Two Forms of GSK598809 Capsules.
A Phase 1 Study of E2022 Tape Formulation for Different Application Sites and Intervals in Japanese Healthy Elderly Males
A Phase 2a Trial of FOL-005 Topical Formulations to Investigate Hair Growth Potential and Safety in Healthy Male Volunteers
A Phase I Trial of Myeloablative Conditioning w/ Clofarabine and HD Busulfan for Pts w/ Refractory Heme Malignancies Undergoing Allo PBSCT
A Phase I/II Trial of a Tetravalent Live Attenuated Dengue Vaccine in Flavivirus Antibody Naïve Children
A Phase II Open-Label Study of High-Dose Cytarabine and Clofarabine in Adult Patients With Refractory or Relapsed Acute Myelogenous Leukemia or Refractory or Relapsed Acute Lymphoblastic Leukemia
A Phase II Study of Clofarabine in Patients With Aggressive Non-Hodgkin's Lymphoma
A Phase II Study of Clofarabine in Patients With Relapsed or Refractory Multiple Myeloma
A Phase II Trial to Compare a Liquid-frozen and a Freeze-dried Formulation of IMVAMUNE (MVA-BN®) Smallpox Vaccine in Vaccinia-naïve Healthy Subjects
A Phase II, Open-Label Study of Clofarabine in Paediatric Patients With Refractory/Relapsed Acute Lymphoblastic Leukaemia
A Phase II, Randomized, Double-blind, Placebo-controlled Study to Examine the Effects of DAS181 in Immunocompromised Subjects With Lower Respiratory Tract Parainfluenza Infection on Supplemental Oxygen
A Research Study Looking Into Blood Levels of Semaglutide and NNC0480-0389 When Given in the Same Injection or in Two Separate Injections in Healthy People
A Safety and Tolerability Study of Clofarabine, Etoposide, Cyclophosphamide, PEG-asparaginase, and Vincristine in Pediatric Acute Lymphoblastic Leukemia (ALL)

Approved for (5)

Acute lymphoblastic leukemia
Cancer
Lymphoblastic lymphoma
Lymphoid leukemia
Neoplasm

In development for (17)

Acute leukemia of ambiguous lineage Phase 2
Acute myeloid leukemia Phase 3
Acute promyelocytic leukemia Phase 1
B-cell chronic lymphocytic leukemia Phase 2
Chronic myeloid leukemia Phase 2
Chronic myelomonocytic leukemia Phase 2
Graft versus host disease Phase 2
Hematologic disorder Phase 2
Hodgkins lymphoma Phase 2
Langerhans cell histiocytosis Phase 2
Leukemia Phase 3
Lymphoma Phase 2
Myelodysplastic syndrome Phase 2
Neoplasm of mature B-cells Phase 1
Non-Hodgkin lymphoma Phase 2
Osteopetrosis Phase 2
Plasma cell myeloma Phase 2

Targets (14)

POLA1 DNA polymerase (alpha/delta/epsilon) inhibitor
POLA2 DNA polymerase (alpha/delta/epsilon) inhibitor
POLD1 DNA polymerase (alpha/delta/epsilon) inhibitor
POLD2 DNA polymerase (alpha/delta/epsilon) inhibitor
POLD3 DNA polymerase (alpha/delta/epsilon) inhibitor
POLD4 DNA polymerase (alpha/delta/epsilon) inhibitor
POLE DNA polymerase (alpha/delta/epsilon) inhibitor
POLE2 DNA polymerase (alpha/delta/epsilon) inhibitor
POLE3 DNA polymerase (alpha/delta/epsilon) inhibitor
PRIM1 DNA polymerase (alpha/delta/epsilon) inhibitor
PRIM2 DNA polymerase (alpha/delta/epsilon) inhibitor
RRM1 Ribonucleoside-diphosphate reductase RR1 inhibitor
RRM2 Ribonucleoside-diphosphate reductase RR1 inhibitor
RRM2B Ribonucleoside-diphosphate reductase RR1 inhibitor

Clofarabine

Development status

Names and chemistry

Brand names (6)

Other names (33)

Identifiers

Regulatory information

United States

European Union

Therapeutic areas

Other regulatory facts

Pharmacology

Drug classification

Administration routes

Mechanisms of action (17)

Open Targets mechanisms (2)

DrugCentral mechanisms (3)

Investigated indications (22)

Open Targets indications (60)

Reported adverse events (76)

Trial references (103)

Dosing

Conditions of use (3)

Chemical properties

National Drug Codes

Evidence counts

Active assay types (4)

Pharmacologic actions

Biological measurements

Observed measurements

Oral bioavailability

Measurement types

Related records

Trials (337)

Approved for (5)

In development for (17)

Targets (14)