dasatinib

: Dasatinib is an oral medication used for treating chronic myeloid leukemia and acute lymphoblastic leukemia. It is classified as a kinase inhibitor. Kinase inhibitors include Erlotinib (Tarceva), gefitinib (Iressa), imatinib (Gleevec), nilotinib (Tasigna), pazopanib (Votrient), sunitinib (Sutent), and vandetanib (Caprelsa). Kinase inhibitors prevent the growth of tumors by reducing the action of proteins that control cell division, growth, and survival. These proteins are usually present in larger quantities or are more active in cancer cells. By reducing the activity of these proteins, growth and survival of cancer cells are reduced. The FDA approved dasatinib in June 2006.

Sprycel

GENERIC AVAILABLE: No

Yes

Common side effects are:

• fluid retention,
• headache,
• diarrhea,
• constipation,
• weakness,
• nausea and vomiting,
• abdominal distention,
• weight loss or gain,
• rash,
• itching,
• chills,
• dizziness, and
• muscle pain.

Other important and serious side effects of dasatinib include:

• fever associated with reduced white blood cells,
• reduced platelets,
• reduced blood cell counts,
• infection,
• stomach or intestinal bleeding,
• bleeding in the brain,
• heart failure, and
• fluid in the lungs.

The recommended dose range of dasatinib is 100-180 mg orally once daily. For newly diagnosed Ph+ CML treatment starts at 100 mg and is increased to 140 mg daily as needed. For advanced Ph+ CML or Ph+ ALL treatment is started at 140 mg and increased to 180 mg daily as needed.

The blood concentration of dasatinib may be increased by several drugs that reduce its break down by liver enzymes. Increased blood concentrations of dasatinib may increase the occurrence of adverse effects. Examples include ketoconazole, itraconazole (Sporanox), clarithromycin (Biaxin), atazanavir (Reyataz), indinavir (Crixivan), nelfinavir (Viracept), ritonavir (Norvir), saquinavir (Invirase), telithromycin (Ketek), voriconazole (Vfend), and grapefruit juice. A dose reduction should be considered if there are no alternative medications that will not interact with dasatinib, for example a reduction in dose from 100 mg to 20 mg or 140 mg to 40 mg daily.

Certain drugs decrease the concentration of dasatinib resulting in decreased blood levels and possibly reduced effect. Examples include dexamethasone, carbamazepine, phenobarbital, rifampin, phenobarbital, and St John's Wort. A dose increase should be considered if dasatinib is combined with such drugs.

Drugs that reduce production of acid in the stomach reduce the absorption of dasatinib. Examples include proton pump inhibitors (PPIs) such as omeprazole (Prilosec) and H2 blocking drugs such as famotidine (Pepcid). Antacids used 2 hours before or after administration of dasatinib are reasonable alternatives to drugs that reduce the production of acid in the stomach.

Dasatinib increases the blood concentration of simvastatin (Zocor) by reducing the activity of enzymes that break down simvastatin in the liver. This may increase the side effects of simvastatin. Dasatinib may interact with other drugs that are broken down in a similar way as simvastatin.

Dasatinib is harmful to the fetus and should not be used during pregnancy.

It is unknown whether dasatinib is excreted in human milk.

What preparations of dasatinib are available?

Tablets: 20, 50, 70, 80, 100, and 140 mg

How should I keep dasatinib stored?

Dasatinib should be stored at room temperature between 15 C - 30 C (59 F -86 F).