What is Dasatinib?
Dasatinib is an anticancer drug.
Dasatinib is used as a first-line treatment for a specific type of chronic myeloid leukemia (CML; a type of cancer of the white blood cells) in patients who no longer benefit from other leukemia medications, such as imatinib (Gleevec), or who are unable to take these medications due to side effects.
How does it work?
Dasatinib inhibits the following kinases at nanomolar concentrations: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFR. Dasatinib is predicted to bind to multiple conformations of the ABL kinase based on modeling studies. Dasatinib was active in vitro against leukemic cell lines derived from patients with imatinib mesylate-sensitive and -resistant disease. Dasatinib inhibited the growth of BCR-ABL-overexpressing chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines. Dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternative signaling pathways involving SRC family kinases (LYN, HCK), and overexpression of multidrug resistance genes under the conditions of the assays.
Dasatinib Dosage
Adult Dose Typical for Leukemia:
- CML in the chronic phase: 100 mg orally once daily
- CML, Myeloid or Lymphoid Blast Phase CML, Ph+ ALL: 140 mg orally once daily
Typical Pediatric Leukemia Dosage:
- 10 kg to less than 20 kg body weight: 40 mg once daily orally
- 20 kg to less than 30 kg body weight: 60 mg once daily orally
- 30 kg to less than 45 kg: 70 mg once daily orally
- At least 45 kg body weight: 100 mg orally once a day
Administration
Allow the tablets to dissolve completely in your mouth; do not split, chew, or crush them. When handling tablets that have been crushed or broken accidentally, wear latex or nitrile gloves to avoid contact with the medication.
Dasatinib side effects
Dasatinib may cause the following side effects:
- Headaches
- Symptoms similar to the flu
- Mild skin rash
- Mouth ulcers
- Weakness
- Loss of weight
- Impaired sensation
- Aches and pains in the muscles and joints
- Nausea
- Vomiting
- Stomach ache
- Appetite loss
- Indigestion
Drug interaction
It is not suggested to combine this medication with any of the following. Your doctor may opt to discontinue treatment with this drug or to alter the doses of other medications you are taking.
- Bepridil
- Dronedarone
- Fluconazole
- Lefamulin
- Live Measles Virus Vaccine
- Mesoridazine
- Live Mumps Virus Vaccine
- Nelfinavir
- Piperaquine
- Posaconazole
- Live Rotavirus Vaccine
- Live Rubella Virus Vaccine
- Saquinavir
- Sparfloxacin
- Terfenadine
- Thioridazine
- Live Varicella Virus Vaccine
- Ziprasidone
- Live Zoster Vaccine
Precautions/ safety information
- Inform your doctor or pharmacist before taking dasatinib if you are allergic to it; or if you have any other allergies. This product may include inactive substances (for example, lactose), which may cause allergic reactions or other complications. Consult your pharmacist for additional information.
- Inform your doctor or pharmacist of your medical history, particularly of any bleeding issues, current or recent infection, heart problems (such as an irregular heartbeat), or liver problems, prior to using this drug (such as hepatitis B).
- Dasatinib may produce an abnormal cardiac rhythm (QT prolongation). QT prolongation is uncommon but can result in serious (occasionally fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that require immediate medical intervention.
Storage
Dasatinib tablets should be stored between 68°F and 77°F (20°C and 25°C) at room temperature.
Contraindications
Dasatinib may result in fluid retention, which may manifest as pleural effusion (fluid build-up around your lungs). Consult your physician immediately if you experience decreased urine output, noisy or rattling breathing, difficulties breathing, swelling of the fingers, hands, feet, or lower legs, difficulty breathing, or weight gain.
Pregnancy or lactation
When dasatinib is delivered to a pregnant woman, it may cause fetal damage or death. Females with reproductive potential should avoid pregnancy; educate women about the fetal risk. Dasatinib crosses the placenta and has been detected at quantities comparable to those found in maternal plasma in fetal plasma and amniotic fluid. Congenital abnormalities (e.g., neural tube defects), hydrops fetalis, fetal leukopenia and thrombocytopenia, and adverse pharmacological effects have all been observed in women treated with dasatinib during pregnancy.
Breastfeeding is not suggested during dasatinib therapy or for two weeks following the last dosage due to the possibility of major adverse effects in nursing children. Dasatinib is not known to be excreted in human breast milk.
