dasatinib dasatinib dasatinib, sold under the brand name sprycel among others, is a targeted therapy medication used to treat certain cases of chronic myelogenous leukemia (cml) and acute lymphoblastic leukemia (all). specifically it is used to treat cases that are philadelphia chromosome-positive (ph+). it is taken by mouth. dasatinibclinical datatrade namessprycel, dasanixahfs/drugs.commonographmedlineplusa607063license data eu ema: by inn us dailymed: dasatinib us fda: dasatinib pregnancycategory au: d routes ofadministrationby mouth (tablets)atc codel01ea02 (who) legal statuslegal status au: s4 (prescription only) uk: pom (prescription only) us: ℞-only eu: rx-only in general: ℞ (prescription only) pharmacokinetic dataprotein binding96%metabolismliverelimination half-life1.3 to 5 hoursexcretionfecal (85%), kidney (4%)identifiers iupac name n-(2-chloro-6-methylphenyl)-2--2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide monohydrate cas number302962-49-8 ypubchem cid3062316iuphar/bps5678drugbankdb01254 ychemspider2323020 yuniix78ug0a0rnkeggd03658 nchebichebi:49375 ychemblchembl1421 ycomptox dashboard (epa)dtxsid4040979 echa infocard100.228.321 chemical and physical dataformulac22h26cln7o2smolar mass488.01 g·mol−13d model (jsmol)interactive image smiles cc1cccc(c1nc(=o)c2cnc(s2)nc3cc(nc(n3)c)n4ccn(cc4)cco)cl inchi inchi=1s/c22h26cln7o2s/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31/h3-5,12-13,31h,6-11h2,1-2h3,(h,28,32)(h,24,25,26,27) ykey:zbnzxtgutayrhi-uhfffaoysa-n y ny (what is this?) (verify) common adverse effects include low white blood cells, low blood platelets, anemia, swelling, rash, and diarrhea. severe adverse effects may include bleeding, pulmonary edema, heart failure, and prolonged qt syndrome. use during pregnancy may result in harm to the baby. it is a tyrosine-kinase inhibitor and works by blocking a number of tyrosine kinases such as bcr-abl and the src kinase family. dasatinib was approved for medical use in the united states and in the european union in 2006. it is on the world health organization's list of essential medicines. medical uses dasatinib is used to treat people with chronic myeloid leukemia and people with acute lymphoblastic leukemia who are positive for the philadelphia chromosome. in the eu dasatinib is indicated for children with newly diagnosed philadelphia chromosome-positive chronic myelogenous leukaemia in chronic phase (ph+ cml cp) or ph+ cml cp resistant or intolerant to prior therapy including imatinib. newly diagnosed ph+ acute lymphoblastic leukaemia (all) in combination with chemotherapy. newly diagnosed ph+ cml in chronic phase (ph+ cml-cp) or ph+ cml-cp resistant or intolerant to prior therapy including imatinib. and adults with newly diagnosed philadelphia-chromosome-positive (ph+) chronic myelogenous leukaemia (cml) in the chronic phase; chronic, accelerated or blast phase cml with resistance or intolerance to prior therapy including imatinib mesilate; ph+ acute lymphoblastic leukaemia (all) and lymphoid blast cml with resistance or intolerance to prior therapy. adverse effects the most common side effects are infection, suppression of the bone marrow (decreasing numbers of leukocytes, erythrocytes, and thrombocytes), 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. neutropenia and myelosuppression were common toxic effects. fifteen people (of 84, i.e. 18%) in the above-mentioned study developed pleural effusions, which was a suspected side effect of dasatinib. some of these people required thoracentesis or pleurodesis to treat the effusions. other adverse events included mild to moderate diarrhea, peripheral edema, and headache. a small number of people developed abnormal liver function tests which returned to normal without dose adjustments. mild hypocalcemia was also noted, but did not appear to cause any significant problems. several cases of pulmonary arterial hypertension (pah) were found in people treated with dasatinib, possibly due to pulmonary endothelial cell damage. 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). symptoms of pah may include shortness of breath, fatigue, and swelling of the body (such as the ankles and legs). in reported cases, people developed pah after starting dasatinib, including after more than one year of treatment. information about the risk was added to the warnings and precautions section of the sprycel drug label. in studies between 2009 and 2017 dasatinib-induced pah was initiated between 0.3 and 74 months of daily drug usage at doses from 70 to 140 mg. reported dasatinib-induced pah had improvements after cessation of drug treatment. pharmacology crystal structure (pdb 2gqg) of abl kinase domain (blue) in complex with dasatinib (red). dasatinib is an atp-competitive protein tyrosine kinase inhibitor. the main targets of dasatinib are bcr/abl (the "philadelphia chromosome"), src, c-kit, ephrin receptors, and several other tyrosine kinases. strong inhibition of the activated bcr-abl kinase distinguishes dasatinib from other cml treatments, such as imatinib and nilotinib. although dasatinib only has a plasma half-life of three to five hours, the strong binding to bcr-abl1 results in a longer duration of action. history