Dasatinib

[3] Severe adverse effects may include bleeding, pulmonary edema, heart failure, and prolonged QT syndrome.

[5] In the EU dasatinib is indicated for children with and adults with The most common side effects are infection, suppression of the bone marrow (decreasing numbers of leukocytes, erythrocytes, and thrombocytes),[6] headache, hemorrhage (bleeding), pleural effusion (fluid around the lungs), dyspnea (difficulty breathing), diarrhea, vomiting, nausea (feeling sick), abdominal pain (belly ache), skin rash, musculoskeletal pain, tiredness, swelling in the legs and arms and in the face, fever.

A small number of people developed abnormal liver function tests which returned to normal without dose adjustments.

[8] On October 11, 2011, the U.S. Food and Drug Administration (FDA) announced that dasatinib may increase the risk of a rare but serious condition in which there is abnormally high blood pressure in the arteries of the lungs (pulmonary hypertension, PAH).

The main targets of dasatinib are BCR/Abl (the "Philadelphia chromosome"), Src, c-Kit, ephrin receptors, and several other tyrosine kinases.

[12] Strong inhibition of the activated BCR-ABL kinase distinguishes dasatinib from other CML treatments, such as imatinib and nilotinib.

[13] Dasatinib was developed by collaboration of Bristol-Myers Squibb and Otsuka Pharmaceutical Co., Ltd,[14][15][16] and named for Bristol-Myers Squibb research fellow Jagabandhu Das, whose program leader says that the drug would not have come into existence had he not challenged some of the medicinal chemists' underlying assumptions at a time when progress in the development of the molecule had stalled.

[17] Dasatinib was approved for used in the United States in June 2006 and in the European Union in November 2006[18][2] In October 2010, dasatinib was approved in the United States for the treatment of newly diagnosed adults with Philadelphia chromosome positive chronic myeloid leukemia in chronic phase (CP-CML).

In England and Wales, the National Institute for Health and Care Excellence recommended against dasatinib because of the high cost-benefit ratio.

Crystal structure [ 11 ] ( PDB 2GQG ) of Abl kinase domain (blue) in complex with dasatinib (red).