What is dasatinib, and how does it work (mechanism of action)?
: 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.
What brand names are available for dasatinib?
Sprycel
Is dasatinib available as a generic drug?
GENERIC AVAILABLE: No
Do I need a prescription for dasatinib?
Yes
What are the side effects of dasatinib?
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.
What is the dosage for dasatinib?
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.
Which drugs or supplements interact with dasatinib?
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.
Is dasatinib safe to take if I’m pregnant or breastfeeding?
Dasatinib is harmful to the fetus and should not be used during
pregnancy.
It is unknown whether dasatinib is excreted in
human milk.
What else should I know about dasatinib?
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).