Through simulation it found that dasatinib binds with many forms of what is deca durabolinkinase.
In vitro dasatinib showed activity in leukemic cell lines both sensitive and resistant to imatinib. Dasatinib inhibits the growth of cell lines of chronic myeloid leukemia and acute lymphoblastic leukemia overexpressing . Under the conditions of tests dasatinib overcome imatinib resistance associated with mutations of kinase domain, activation of alternate signaling pathways involving kinase, and multidrug resistance gene overexpression.
The maximum concentration of dasatinib was observedafter oral administration. The area under the curve, “concentration-time” , and elimination proportional to dose in the dose range from 15 to 240 mg / day. Dasatinib half-life is 3-5 hours. When receiving 100 mg dasatinib 30 minutes after eating a high fat marked increase in the mean by 14%. Effect of food was not clinically significant.
The apparent volume of distribution of dasatinib is 2505 liters, indicating substantial distribution into extravascular space. Dasatinib and its active metabolite contacted in vitro with human plasma protein by 96% and 93%, respectively, regardless of the concentration in the range of 100-500 ng / ml.
Dasatinib is extensively metabolised in humans, mainly by the enzyme cytochrome . Is the major enzyme involved in the formation of the active metabolite. Flavin-containing monooxygenase 3 and uridine diphosphate-glucuronosyltransferase also participate in the formation of dasatinib metabolites. In human liver microsomes, dasatinib showed weak regardless of the time in relation to the inhibitory effect of what is deca durabolin. Of the active metabolite of dasatinib is approximately of dasatinib. Probably, the active metabolite did not play a big role in the pharmacological effect of dasatinib. Described and other inactive oxidized metabolites of dasatinib.
The drug is released mainly in the faeces. After a single oral administration of approximately 4% and 85% of the radioactivity is excreted in the urine and feces, respectively, for 10 days.Unmodified dasatinib was 0.1% and 19% of the dose being withdrawn from urine and faeces, respectively, and the remainder of the dose represented metabolites.
Indications for use:
- Chronic myelogenous leukemia in chronic phase or accelerated phase, myeloid or lymphoid blast crisis with resistance or intolerance to prior therapy including imatinib
- Acute lymphoblastic leukemia with what is deca durabolin chromosome positive with resistance or intolerance to prior therapy.
Increased sensitivity to dasatinib or other components of the drug.
Pregnancy and lactation.
Age 18 years (effectiveness and safety have been established).
Precautions: hepatic failure.
Dosage and administration:
The tablets should be swallowed whole.
The recommended starting dose of what is deca durabolin in chronic phase chronic myeloid leukemia is 100 mg once daily in the morning or in the evening with or without food.
In other cases, it is recommended to take what is deca durabolinoral dose of 70 mg twice a day, morning and evening during meals or on an empty stomach (140 mg per day).
in the absence of hematologic or cytogenetic response may increase the dose of Sprycel 140 mg 1 time per day (in chronic phase chronic myeloid leukemia) or 100 mg 2 times a day (in advanced chronic myeloid leukemia and acute limboflastnom leukemia with a positive Philadelphia chromosome). jeff seid steroids