Clofarabine

Clofarabine

Clinical data
Trade names	Clolar, Evoltra
AHFS/Drugs.com	Monograph
MedlinePlus	a607012
Routes of administration	Intravenous
ATC code	L01BB06 (WHO)
Legal status
Legal status	℞ (Prescription only)
Identifiers
IUPAC name 5-(6-amino-2-chloro-purin-9-yl) -4-fluoro-2- (hydroxymethyl)oxolan-3-ol
CAS Number	123318-82-1 Y
PubChem (CID)	119182
IUPHAR/BPS	6802
DrugBank	DB00631 Y
ChemSpider	106472 Y
UNII	762RDY0Y2H Y
KEGG	D03546 Y
ChEBI	CHEBI:681569 Y
ChEMBL	CHEMBL1750 Y
ECHA InfoCard	100.159.663
Chemical and physical data
Formula	C10H11ClFN5O3
Molar mass	303.677 g/mol
3D model (Jmol)	Interactive image
SMILES Clc1nc(c2ncn(c2n1)[C@@H]3O[C@@H]([C@@H](O)[C@@H]3F)CO)N
InChI InChI=1S/C10H11ClFN5O3/c11-10-15-7(13)5-8(16-10)17(2-14-5)9-4(12)6(19)3(1-18)20-9/h2-4,6,9,18-19H,1H2,(H2,13,15,16)/t3-,4+,6-,9-/m1/s1 Y Key:WDDPHFBMKLOVOX-AYQXTPAHSA-N Y
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Clofarabine is a purine nucleoside antimetabolite marketed in the US and Canada as Clolar. In Europe and Australia/New Zealand the product is marketed under the name Evoltra. It is FDA-approved for treating relapsed or refractory acute lymphoblastic leukaemia (ALL) in children after at least two other types of treatment have failed. It is not known if it extends life expectancy. Some investigations of effectiveness in cases of acute myeloid leukaemia (AML) and juvenile myelomonocytic leukaemia (JMML) have been carried out. Ongoing trials are assessing its efficacy, if any, for managing other cancers.

Side effects

• Tumor lysis syndrome (TLS). Clofarabine quickly kills leukaemia cells in the blood. The body may react to this. Signs include hyperkalemia, hyperuricemia, and hyperphosphatemia. TLS is very serious and can lead to death if it is not treated right away.
• Systemic inflammatory response syndrome (SIRS): symptoms include fast breathing, fast heartbeat, low blood pressure, and fluid in the lungs.
• Bone marrow problems (suppression). Clofarabine can stop the bone marrow from making enough red blood cells, white blood cells, and platelets. Serious side effects that can happen because of bone marrow suppression include severe infection (sepsis), bleeding, and anemia.
• Effects on pregnancy and breastfeeding. Girls and women should not become pregnant or breastfeed during treatment which may harm the baby.
• Dehydration and low blood pressure. Clofarabine can cause vomiting and diarrhea which may lead to low body fluid (dehydration). Signs and symptoms of dehydration include dizziness, lightheadedness, fainting spells, or decreased urination.
• Other side effects. The most common side effects are stomach problems (including vomiting, diarrhea, and nausea), and effects on blood cells (including low red blood cells count, low white blood cell count, low platelet count, fever, and infection. Clofarabine can also cause tachycardia and can affect the liver and kidneys.

Contraindications

• pregnancy or planned pregnancy
• breast-feeding
• liver problems
• kidney problems

Drug interactions

• nephrotoxic drugs
• hepatotoxic drugs

Delivery

• By intravenous infusion.
• Dosage is a 2-hour infusion (52 mg/m²) every day for five days. The cycle is repeated every 2 to 6 weeks.
• Regular blood tests to monitor his or her blood cells, kidney function, and liver function.

Approval

Clolar was Food and Drug Administration (FDA) approved 28 December 2004. (Under accelerated approval regulations requiring further clinical studies.)

External links

• FDA usage leaflet.
• Clolar.com homepage.
• FDA approval notice.