Clofarabine inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase. Induces apoptosis by directly altering mitochondrial transmembrane potential. Demonstrates growth inhibition and cytotoxic activity in a variety of leukemias and solid tumors.
|Cell lines||hela cells|
|Preparation method||Radiosensitivity assay.
Cells were treated with indicated dose of clofarabine, and then media was changed 20 hours later. The cultures were incubated for 10-12 days, harvested, and stained with 0.5% crystal violet in methanol. The colony number was determined with a dissecting microscope. a population of >50 cells was counted as one colony, and the number of colonies was expressed as a percentage of the value for untreated controls and those treated with clofarabine. the survival curves were plotted by linear regression analyses, and the D0 value represents the radiation dose that lead to 37% survival.
|Concentrations||0, 10, 100, and 1000 n M|
|Animal models||male nude mice bearing DLD-1 human tumour xenografts model|
|Dosages||30mg/kg daily for 12 days|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
The Role of Clofarabine in Acute Myeloid Leukemia.
Ghanem et al. Leuk Lymphoma. 2012 Sep 7. PMID: 22957815.
Phase I dose-escalation trial of clofarabine followed by escalating doses of fractionated cyclophosphamide in children with relapsed or refractory acute leukemias.
Abd Elmoneim et al. Pediatr Blood Cancer. 2012 Aug 8. PMID: 22887831.
Synergism between clofarabine and decitabine through p53R2: A pharmacodynamic drug-drug interaction modeling.
Thudium et al. Leuk Res. 2012 Aug 9. PMID: 22884950.
Clofarabine Targets the Large Subunit (α) of Human Ribonucleotide Reductase in Live Cells by Assembly into Persistent Hexamers.
Aye et al. Chem Biol. 2012 Jul 27;19(7):799-805. PMID: 22840768.
Retrospective comparison of clofarabine versus fludarabine in combination with high dose cytarabine with or without granulocyte colony-stimulating factor as salvage therapies for acute myeloid leukemia.
Becker et al. Haematologica. 2012 Jul 16. PMID: 22801963.
Clofarabine Combined with Busulfan Provides Excellent Disease Control in Adult Patients with Acute Lymphoblastic Leukemia Undergoing Allogeneic Hematopoietic Stem Cell Transplantation.
Kebriaei et al. Biol Blood Marrow Transplant. 2012 Jun 29. PMID: 22750645.
Clofarabine acts as radiosensitizer in vitro and in vivo by interfering with DNA damage response.
Cariveau MJ, et al. Int J Radiat Oncol Biol Phys. 2008 Jan 1;70(1):213-20. PMID: 18037589.
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