Drug intelligence / Profile preview

zileuton + dasatinib

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

Zileuton + dasatinib is a combination of two small molecule drugs with distinct mechanisms of action. Zileuton is a selective inhibitor of 5-lipoxygenase, the enzyme responsible for leukotriene synthesis from arachidonic acid. By inhibiting leukotriene formation (including LTB4, LTC4, LTD4, and LTE4), zileuton reduces inflammation and bronchoconstriction in the airways and is primarily used for prophylaxis and treatment of chronic asthma[3][4]. Dasatinib is an orally available multikinase inhibitor that targets BCR-ABL tyrosine kinase as well as several SRC-family kinases (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. It binds both active and inactive conformations of ABL kinase with high affinity. Dasatinib is indicated for the treatment of Philadelphia chromosome-positive chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL)[1][2][5][6]. There are no approved indications or established clinical uses for this specific drug combination.

02

Targets

ALOX12 (Arachidonate 12-lipoxygenase, 12S type)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)EPHA2 (Ephrin type-A receptor 2)PDGFRB (Platelet-derived growth factor receptor beta)SFK (SRC family kinases)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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