Imatinib
mesylate is an orally administered,
synthetic tyrosine kinase inhibitor
(three known targets are ABL, c-kit,
PDGF receptor). It is rapidly absorbed
, and is highly bioavailable. Most of
imatinib is eliminated as metabolites,
only 25% of it is eliminated unchanged.
The half-lives of imatinib and its main
metabolite are 18 and 40 hours respectively.
It is used in the treatment of chronic
myeloid leukaemia (CML) and GIST. It
is also approved as a single agent for
the treatment of dermatofibrosarcoma
protuberans (DFSP), myelodysplastic
/ myeloproliferative diseases (MDS/MPD),
aggressive systemic mastocytosis (ASM),
hypereosinophilic syndrome/chronic eosinophilic
leukemia (HES/CEL), and relapsed/refractory
Philadelphia chromosome positive acute
lymphocytic leukemia (Ph+ ALL).
ImatiRel is available as 100 and 400
mg tablets.
