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Details

Stereochemistry ABSOLUTE
Molecular Formula C10H14ClFN5O12P3
Molecular Weight 543.617
Optical Activity UNSPECIFIED
Defined Stereocenters 4 / 4
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of Clofarabine triphosphate

SMILES

NC1=C2N=CN([C@@H]3O[C@H](COP(O)(=O)OP(O)(=O)OP(O)(O)=O)[C@@H](O)[C@@H]3F)C2=NC(Cl)=N1

InChI

InChIKey=ILZCVFJUTWHERD-AYQXTPAHSA-N
InChI=1S/C10H14ClFN5O12P3/c11-10-15-7(13)5-8(16-10)17(2-14-5)9-4(12)6(18)3(27-9)1-26-31(22,23)29-32(24,25)28-30(19,20)21/h2-4,6,9,18H,1H2,(H,22,23)(H,24,25)(H2,13,15,16)(H2,19,20,21)/t3-,4+,6-,9-/m1/s1

HIDE SMILES / InChI

Description
Curator's Comment: description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021673s024lbl.pdf

Clofarabine is a anti-cancer drug which was approved by FDA for the treatment of pediatric patients with relapsed or refractory acute lymphoblastic leukemia. After crossing the cell membrane the drug is rapidly metabolized by deoxycytidine kinase to diphosphate and triphosphate metabolites and these metabolites reversibly inhibit hRNR by binding to alpha subunit. Also the triphosphate is incorporated to DNA where it acts as a chain terminator.

CNS Activity

CNS Penetrant
2554
Curator's Comment: Only a small amount of the drug was shown to cross the blood brain barrier in non-human primates.

Originator

Approval Year

2004
210
Targets

Targets

Primary TargetPharmacologyConditionPotency
Binding Agent
1064
Inhibitor
8297
 17.0 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
CLOLAR

Approved Use

Clolar® (clofarabine) Injection is indicated for the treatment of pediatric patients 1 to 21 years old with relapsed or refractory acute lymphoblastic leukemia after at least two prior regimens.

Launch Date

2004
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
308 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/28509593
40 mg/m² 1 times / day multiple, intravenous
dose: 40 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered: CYTARABINE
CYTARABINE
 CLOFARABINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1793 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/28509593
40 mg/m² 1 times / day multiple, intravenous
dose: 40 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered: CYTARABINE
CYTARABINE
 CLOFARABINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
28 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/29773602
40 mg/m² 1 times / day multiple, intravenous
dose: 40 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
CLOFARABINE blood
Homo sapiens
population: UNHEALTHY
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
4.9 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/28509593
40 mg/m² 1 times / day multiple, intravenous
dose: 40 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered: CYTARABINE
CYTARABINE
 CLOFARABINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1.5 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/29773602
40 mg/m² 1 times / day multiple, intravenous
dose: 40 mg/m²
route of administration: Intravenous
experiment type: MULTIPLE
co-administered:
CLOFARABINE blood
Homo sapiens
population: UNHEALTHY
age: CHILD
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
55 mg/m2 1 times / day multiple, intravenous
Highest studied dose
Dose: 55 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 55 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
unhealthy, 42 years
n = 4
Health Status: unhealthy
Condition: acute leukemia
Age Group: 42 years
Sex: M+F
Population Size: 4
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
Other AEs: Nausea, Diarrhea...
Other AEs:
Nausea (grade 1-2, 2 patients)
Diarrhea (grade 1, 3 patients)
Hepatotoxicity (grade 3, 2 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
40 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 40 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 40 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
unhealthy, 42 years
n = 31
Health Status: unhealthy
Condition: acute leukemia
Age Group: 42 years
Sex: M+F
Population Size: 31
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
Other AEs: Nausea, Fatigue...
Other AEs:
Nausea (grade 1-2, 3 patients)
Fatigue (grade 3, 1 patient)
Diarrhea (grade 1, 2 patients)
Cramp (grade 1, 1 patient)
Anorexia (grade 1, 1 patient)
Mucositis (grade 1, 1 patient)
Edema (grade 1, 1 patient)
Hepatotoxicity (grade 3-4, 4 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
2 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 2 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 2 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
unhealthy, 51 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: 51 years
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
DLT: Myelosuppression...
Dose limiting toxicities:
Myelosuppression (grade 3, 2 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
6 mg 1 times / day multiple, oral
Highest studied dose
Dose: 6 mg, 1 times / day
Route: oral
Route: multiple
Dose: 6 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24415560
unhealthy, 60-76 years
n = 1
Health Status: unhealthy
Condition: Acute Myeloid Leukemia
Age Group: 60-76 years
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/24415560
Other AEs: Nausea, Hypoalbuminemia...
Other AEs:
Nausea (grade 1-2, 1 patient)
Hypoalbuminemia (grade 1-2, 1 patient)
Blood bilirubin decreased (grade 1-2, 1 patient)
Lymphopenia (grade 3-4)
Sources:
https://pubmed.ncbi.nlm.nih.gov/24415560
70 mg/m2 1 times / day multiple, intravenous
Highest studied dose
Dose: 70 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 70 mg/m2, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/021673lbl.pdf
unhealthy, child
n = 2
Health Status: unhealthy
Condition: ALL
Age Group: child
Population Size: 2
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/021673lbl.pdf
Other AEs: Hyperbilirubinemia, Vomiting...
Other AEs:
Hyperbilirubinemia (grade 4, 2 patients)
Vomiting (grade 2-3, 2 patients)
Maculopapular rash (grade 3, 2 patients)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/021673lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Diarrhea grade 1, 3 patients
55 mg/m2 1 times / day multiple, intravenous
Highest studied dose
Dose: 55 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 55 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
unhealthy, 42 years
n = 4
Health Status: unhealthy
Condition: acute leukemia
Age Group: 42 years
Sex: M+F
Population Size: 4
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
Nausea grade 1-2, 2 patients
55 mg/m2 1 times / day multiple, intravenous
Highest studied dose
Dose: 55 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 55 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
unhealthy, 42 years
n = 4
Health Status: unhealthy
Condition: acute leukemia
Age Group: 42 years
Sex: M+F
Population Size: 4
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
Hepatotoxicity grade 3, 2 patients
55 mg/m2 1 times / day multiple, intravenous
Highest studied dose
Dose: 55 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 55 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
unhealthy, 42 years
n = 4
Health Status: unhealthy
Condition: acute leukemia
Age Group: 42 years
Sex: M+F
Population Size: 4
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
Anorexia grade 1, 1 patient
40 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 40 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 40 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
unhealthy, 42 years
n = 31
Health Status: unhealthy
Condition: acute leukemia
Age Group: 42 years
Sex: M+F
Population Size: 31
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
Cramp grade 1, 1 patient
40 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 40 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 40 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
unhealthy, 42 years
n = 31
Health Status: unhealthy
Condition: acute leukemia
Age Group: 42 years
Sex: M+F
Population Size: 31
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
Edema grade 1, 1 patient
40 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 40 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 40 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
unhealthy, 42 years
n = 31
Health Status: unhealthy
Condition: acute leukemia
Age Group: 42 years
Sex: M+F
Population Size: 31
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
Mucositis grade 1, 1 patient
40 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 40 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 40 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
unhealthy, 42 years
n = 31
Health Status: unhealthy
Condition: acute leukemia
Age Group: 42 years
Sex: M+F
Population Size: 31
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
Diarrhea grade 1, 2 patients
40 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 40 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 40 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
unhealthy, 42 years
n = 31
Health Status: unhealthy
Condition: acute leukemia
Age Group: 42 years
Sex: M+F
Population Size: 31
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
Nausea grade 1-2, 3 patients
40 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 40 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 40 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
unhealthy, 42 years
n = 31
Health Status: unhealthy
Condition: acute leukemia
Age Group: 42 years
Sex: M+F
Population Size: 31
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
Fatigue grade 3, 1 patient
40 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 40 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 40 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
unhealthy, 42 years
n = 31
Health Status: unhealthy
Condition: acute leukemia
Age Group: 42 years
Sex: M+F
Population Size: 31
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
Hepatotoxicity grade 3-4, 4 patients
40 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 40 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 40 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
unhealthy, 42 years
n = 31
Health Status: unhealthy
Condition: acute leukemia
Age Group: 42 years
Sex: M+F
Population Size: 31
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
Myelosuppression grade 3, 2 patients
DLT
2 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 2 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 2 mg/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
unhealthy, 51 years
n = 6
Health Status: unhealthy
Condition: solid tumors
Age Group: 51 years
Sex: M+F
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/12637486
Blood bilirubin decreased grade 1-2, 1 patient
6 mg 1 times / day multiple, oral
Highest studied dose
Dose: 6 mg, 1 times / day
Route: oral
Route: multiple
Dose: 6 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24415560
unhealthy, 60-76 years
n = 1
Health Status: unhealthy
Condition: Acute Myeloid Leukemia
Age Group: 60-76 years
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/24415560
Hypoalbuminemia grade 1-2, 1 patient
6 mg 1 times / day multiple, oral
Highest studied dose
Dose: 6 mg, 1 times / day
Route: oral
Route: multiple
Dose: 6 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24415560
unhealthy, 60-76 years
n = 1
Health Status: unhealthy
Condition: Acute Myeloid Leukemia
Age Group: 60-76 years
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/24415560
Nausea grade 1-2, 1 patient
6 mg 1 times / day multiple, oral
Highest studied dose
Dose: 6 mg, 1 times / day
Route: oral
Route: multiple
Dose: 6 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24415560
unhealthy, 60-76 years
n = 1
Health Status: unhealthy
Condition: Acute Myeloid Leukemia
Age Group: 60-76 years
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/24415560
Lymphopenia grade 3-4
6 mg 1 times / day multiple, oral
Highest studied dose
Dose: 6 mg, 1 times / day
Route: oral
Route: multiple
Dose: 6 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24415560
unhealthy, 60-76 years
n = 1
Health Status: unhealthy
Condition: Acute Myeloid Leukemia
Age Group: 60-76 years
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/24415560
Vomiting grade 2-3, 2 patients
70 mg/m2 1 times / day multiple, intravenous
Highest studied dose
Dose: 70 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 70 mg/m2, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/021673lbl.pdf
unhealthy, child
n = 2
Health Status: unhealthy
Condition: ALL
Age Group: child
Population Size: 2
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/021673lbl.pdf
Maculopapular rash grade 3, 2 patients
70 mg/m2 1 times / day multiple, intravenous
Highest studied dose
Dose: 70 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 70 mg/m2, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/021673lbl.pdf
unhealthy, child
n = 2
Health Status: unhealthy
Condition: ALL
Age Group: child
Population Size: 2
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/021673lbl.pdf
Hyperbilirubinemia grade 4, 2 patients
70 mg/m2 1 times / day multiple, intravenous
Highest studied dose
Dose: 70 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 70 mg/m2, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/021673lbl.pdf
unhealthy, child
n = 2
Health Status: unhealthy
Condition: ALL
Age Group: child
Population Size: 2
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/021673lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP450
65
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP450
65
 no
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:681569
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:681569
MolPort
MolPort-005-941-711
https://www.molport.com/shop/molecule-link/MolPort-005-941-711
Selleck Chemicals
Clofarabine
http://www.selleckchem.com/products/Clofarabine.html
ZINC
ZINC000003798247
http://zinc15.docking.org/substances/ZINC000003798247
eMolecules
29256989
https://www.emolecules.com/cgi-bin/more?vid=29256989
eMolecules
30512527
https://www.emolecules.com/cgi-bin/more?vid=30512527
PubMed

PubMed

TitleDatePubMed
Effects of 2-chloro-9-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)adenine on K562 cellular metabolism and the inhibition of human ribonucleotide reductase and DNA polymerases by its 5'-triphosphate.
1991 May 1
Mechanisms of the apoptotic activity of Cl-F-araA in a human T-ALL cell line, CCRF-CEM.
2002 Sep
Induction of complete remission using single agent clofarabine in a patient with primary refractory acute myeloblaste leukemia.
2003 Dec
Down-regulation of deoxycytidine kinase in human leukemic cell lines resistant to cladribine and clofarabine and increased ribonucleotide reductase activity contributes to fludarabine resistance.
2003 Jan 15
New designs for phase 2 clinical trials.
2003 Jul 15
Phase I clinical and pharmacology study of clofarabine in patients with solid and hematologic cancers.
2003 Mar 15
Clofarabine.
2004
Prognostic factors and therapeutic options for relapsed or refractory acute myeloid leukemia.
2004 Aug
In vitro assessment of nucleoside analogs in multiple myeloma.
2004 Aug
Gateways to clinical trials.
2004 Jan-Feb
Gateways to clinical trials.
2004 Jul-Aug
Purine nucleoside antimetabolites in development for the treatment of cancer.
2004 Jun
New nucleoside analogs in the treatment of hematological disorders.
2004 May-Jun
Clofarabine in adult acute leukemias: clinical success and pharmacokinetics.
2004 Oct
Plasma and cerebrospinal fluid pharmacokinetics of clofarabine in nonhuman primates.
2005 Aug 15
Clofarabine in the treatment of acute myeloid leukaemia and acute lymphoblastic leukaemia: a review.
2005 Dec
New drugs and dosage forms.
2005 Feb 1
Gateways to clinical trials.
2005 Jun
Clofarabine.
2005 May
Clofarabine.
2005 May
New agents in the treatment of childhood leukemias and myelodysplastic syndromes.
2005 Nov
Gateways to clinical trials.
2005 Sep
Purine nucleoside analogues for the treatment of hematological malignancies: pharmacology and clinical applications.
2005 Sep
New drugs: tigecycline, ziconotide, and clofarabine.
2005 Sep-Oct
Purine nucleoside analogs as immunosuppressive and antineoplastic agents: mechanism of action and clinical activity.
2006
New agents for the treatment of acute myeloid leukemia.
2006
New drugs 06, part I.
2006 Feb
A comparison of the transportability, and its role in cytotoxicity, of clofarabine, cladribine, and fludarabine by recombinant human nucleoside transporters produced in three model expression systems.
2006 Jan
Gateways to clinical trials.
2006 Nov
The activity and toxicity of low dose clofarabine against relapsed or refractory myeloma.
2006 Nov
Clofarabine and nelarabine: two new purine nucleoside analogs.
2006 Nov
Gateways to clinical trials.
2006 Oct
Discovery and development of clofarabine: a nucleoside analogue for treating cancer.
2006 Oct
In vitro cytotoxicity of nelarabine, clofarabine and flavopiridol in paediatric acute lymphoblastic leukaemia.
2007 Apr
Clofarabine: new drug. Children with acute lymphoblastic leukaemia: a last resort.
2007 Dec
Three new drugs for acute lymphoblastic leukemia: nelarabine, clofarabine, and forodesine.
2007 Dec
Pharmacogenetics of deoxycytidine kinase: identification and characterization of novel genetic variants.
2007 Dec
Clofarabine for the treatment of acute lymphoblastic leukemia.
2007 Feb
Comparison of fast liquid chromatography/tandem mass spectrometric methods for simultaneous determination of cladribine and clofarabine in mouse plasma.
2007 Jun 28
Advances in the management of AML in the elderly.
2007 Mar
Clofarabine induced durable complete remission in heavily pretreated adolescents with relapsed and refractory leukemia.
2007 Sep
Cytotoxic nucleoside analogues: different strategies to improve their clinical efficacy.
2008
Treating refractory leukemias in childhood, role of clofarabine.
2008 Apr
Clofarabine acts as radiosensitizer in vitro and in vivo by interfering with DNA damage response.
2008 Jan 1
Novel purine nucleoside analogues for hematological malignancies.
2008 Jun
Fatal skin and liver toxicity in a patient treated with clofarabine.
2008 May
Clofarabine: in search of combinations for the treatment of patients with high-risk acute myeloid leukemia.
2008 Oct 15
Clofarabine combinations as acute myeloid leukemia salvage therapy.
2008 Oct 15
Contribution of the drug transporter ABCG2 (breast cancer resistance protein) to resistance against anticancer nucleosides.
2008 Sep
Enhancement of the in vivo antitumor activity of clofarabine by 1-beta-D-[4-thio-arabinofuranosyl]-cytosine.
2009 Jul
Patents

Patents

20040192735
3

Sample Use Guides

In Vivo Use Guide
The recommended pediatric dose is 52 mg/m2 given as an intravenous infusion over 2 hours daily for 5 consecutive days of a 28-day cycle. Repeat cycles every 2-6 week.
Route of Administration: Intravenous
In Vitro Use Guide
HL-60 cells or HL/ara-C20 cells were incubated with different concentrations of clofarabine for 72 h. The 50%-growth-inhibitory concentration IC50 was 50 nM for HL60 and 320 nM for HL/ara-C20 cells.
Name Type Language
Clofarabine triphosphate
Common Name English
9H-Purin-6-amine, 2-chloro-9-[2-deoxy-2-fluoro-5-O-[hydroxy[[hydroxy(phosphonooxy)phosphinyl]oxy]phosphinyl]-β-D-arabinofuranosyl]-
Systematic Name English
2-Chloro-9-[2-deoxy-2-fluoro-5-O-[hydroxy[[hydroxy(phosphonooxy)phosphinyl]oxy]phosphinyl]-β-D-arabinofuranosyl]-9H-purin-6-amine
Systematic Name English
Code System Code Type Description
PUBCHEM
9915350
Created by admin on Sat Dec 16 19:23:27 GMT 2023 , Edited by admin on Sat Dec 16 19:23:27 GMT 2023
PRIMARY
FDA UNII
YPJ8ZV99ZP
Created by admin on Sat Dec 16 19:23:27 GMT 2023 , Edited by admin on Sat Dec 16 19:23:27 GMT 2023
PRIMARY
CAS
134646-41-6
Created by admin on Sat Dec 16 19:23:27 GMT 2023 , Edited by admin on Sat Dec 16 19:23:27 GMT 2023
PRIMARY
EPA CompTox
DTXSID00432746
Created by admin on Sat Dec 16 19:23:27 GMT 2023 , Edited by admin on Sat Dec 16 19:23:27 GMT 2023
PRIMARY
PRODRUG (METABOLITE ACTIVE)
Structure of CLOFARABINE
NIH
NCATS
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HHS VULNERABILITY DISCLOSURE
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