Dasatinib is a kinase inhibitor indicated for the treatment
of newly diagnosed adults with Philadelphia chromosome-positive (Ph+) chronic
myeloid leukemia (CML) in chronic phase. It is also indicated for adults with
chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with
resistance or intolerance to prior therapy including Imatinib, and for adults
with Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL)
with resistance or intolerance to prior therapy.
CYP3A4 Inhibitors: May increase Dasatinib drug levels and
should be avoided. If coadministration cannot be avoided, monitor closely and
consider reducing Dasatinib dose.
CYP3A4 Inducers: May decrease Dasatinib drug levels. If
coadministration cannot be avoided, consider increasing Dasatinib dose.
Antacids: May decrease Dasatinib drug levels. Avoid
simultaneous administration. If needed, administer the antacid at least 2 hours
prior to or 2 hours after Dasatinib.
H2 Antagonists/Proton Pump Inhibitors: May decrease
Dasatinib drug levels. Consider using antacids instead.
The recommended starting dose of Dasatinib for chronic phase
CML is 100 mg administered orally once daily. The recommended starting dose of
Dasatinib for accelerated phase CML, myeloid or lymphoid blast phase CML, or
Ph+ ALL is 140 mg administered orally once daily. Tablets should not be crushed
or cut; they should be swallowed whole. Dasatinib can be taken with or without
a meal, either in the morning or evening.
The most common side effects are bloody or black tarry
stools, body aches or pain, burning, tingling, numbness or pain in the hands,
arms, feet or legs, chest pain, constipation, cough or hoarseness, difficulty
with breathing, dizziness, ear congestion, fainting, fast, slow or irregular
heartbeat, fever or chills, full or bloated feeling, headache, loss of voice,
lower back or side pain, and painful or difficult urination.
The most common side effects are bloody or black tarry
stools, body aches or pain, burning, tingling, numbness or pain in the hands,
arms, feet or legs, chest pain, constipation, cough or hoarseness, difficulty
with breathing, dizziness, ear congestion, fainting, fast, slow or irregular
heartbeat, fever or chills, full or bloated feeling, headache, loss of voice,
lower back or side pain, and painful or difficult urination.
Pregnancy: US FDA approved pregnancy category D. Based on limited
human data, Dasatinib can cause fetal harm when administered to a pregnant
woman. Adverse pharmacologic effects including hydrops fetalis, fetal
leukopenia, and fetal thrombocytopenia have been reported with maternal
exposure to Dasatinib.
Lactation: No data are available regarding the presence of
Dasatinib in human milk, its effects on the breastfed child, or the effects on
milk production. Breastfeeding is not recommended during treatment with
Dasatinib and for 2 weeks after the final dose.
Myelosuppression: Treatment is associated with severe
thrombocytopenia, neutropenia, and anemia, more frequent in advanced phase CML
or Ph+ ALL.
Bleeding Events: Dasatinib may cause platelet dysfunction in
addition to thrombocytopenia.
Fluid Retention: Severe fluid retention has been reported in
up to 10% of patients.
QT Prolongation: Use with caution in patients at risk.
Pulmonary Arterial Hypertension (PAH): May occur any time
after initiation, even after one year of treatment.
Embryo-fetal Toxicity: Can cause fetal harm. Women of
childbearing potential should avoid pregnancy during therapy.
Hepatic Impairment: Use with caution.
Geriatric Use: Patients aged 65 years and older are more
likely to experience adverse reactions including fatigue, pleural effusion,
diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite
disturbance, and should be monitored closely.
The highest overdose reported was 280 mg per day for 1 week
in two patients, both of whom developed severe myelosuppression and bleeding.
Store at a temperature not exceeding 30°C in a dry place.
Protect from light and moisture. Keep out of reach of children.
