Dasatinib

Product name: Dasatinib

Product synonyms: SPRYCEL;BMS354825;DASATINIB(BMS354825);CS-1968;N-(2-chloro-6-Methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-Methyl-4-pyriMidinyl]aMino]-1,3-thiazole-5-carboxaMide;sprycelDasatinib;Dasatinib(DasatinibMonohydrate)Tablet

CAS NO: 302962-49-8

Molecular formula C22H26ClN7O2S

Molecular Weight 488.01

Dasatinib is an oral potent oncogenic kinase inhibitor, which can block signal of cancer cell replication acceleration , in May 2009, the US Food and Drug Administration (FDA) formally approved the sale of dasatinib , It has been clinically used for the treatment of various chronic myeloid leukemia (CML), including treatment of chronic myeloid leukemia which is resistant or intolerant to the treating programs including imatinib mesylate., Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph + ALL) and the treatment of patients with solid tumors.

Dasatinib is a white to off-white powder and has a melting point of 280°-286° C. The drug substance is insoluble in water and slightly soluble in ethanol and methanol. SPRYCEL™ (dasatinib) is an inhibitor of multiple tyrosine kinases.SPRYCEL tablets are white to offwhite, biconvex, film-coated tablets containing dasatinib, with the following inactive ingredients: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, hydroxypropyl cellulose, and magnesium stearate. The tablet coating consists of hypromellose, titanium dioxide, and polyethylene glycol.

Dasatinib is administered orally. The drug is rapidly absorbed, peak plasma concentrations occur 0.5-3 h after administration. The intake of food is not relevant for pharmacokinetics of dasatinib. In a dose range of 25-120 mg twice daily, the area under the plasma concentration—time curve (AUC) increased proportionally. The drug is extensively metabolized in the liver, predominantly by cytochrome P 450 (CYP) 3A4, only 30 % remain unchanged. The metabolites of the compound are unlikely to play a pharmacologic role. There were linear elimination characteristics over the above-mentioned dose range with a terminal elimination half-life of 5-6 h.
Elimination occurs mostly in the feces (85 %) only little in urine (4 %). Dasatinib is excreted as metabolites, only 19% of a dose was recovered as unchanged drug in the feces (SprycelÒBMS 2012).

Suitable for treatment of chronic myeloid leukemia which is resistant or intolerant to the treating programs including imatinib mesylate.
Dasatinib is used to treat a certain type of chronic myeloid leukemia (CML; a type of cancer of the white blood cells) as a first treatment and in people who can no longer benefit from other leukemia medications including imatinib (Gleevec) or in those who cannot take these medications because of side effects. Dasatinib is also used to treat a certain type of chronic CML in children. Dasatinib is also used to treat a certain type of acute lymphoblastic leukemia (ALL; a type of cancer of the white blood cells) in people who can no longer benefit from other leukemia medications or who cannot take these medications because of side effects. Dasatinib is in a class of medications called kinase inhibitors. It works by blocking the action of an abnormal protein that signals cancer cells to multiply. This helps stop the spread of cancer cells.

Melting point 275-286°C

Density1.408±0.06g/cm3(Predicted)

Storage condition Sealedindry, Storeinfreezer, under-20°C

Solubility SolubleinDMSO(upto200mg/ml).

Acidity coefficient (pKa)10.94±0.70(Predicted)

AppearanceWhitepowder.

Color Whiteoroff-white

Stability Stable for 1 year from date of purchase as supplied.