Latest research on Imatinib

Imatinib is a small molecule kinase inhibitor used to treat certain types of cancer. It is currently marketed by Novartis as Gleevec (USA) or Glivec (Europe/Australia) as its mesylate salt, imatinib mesilate (INN). It is occasionally referred to as CGP57148B or STI571 (especially in older publications). It is used in treating chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and a number of other malignancies. It is the first member of a new class of agents that act by inhibiting particular tyrosine kinase enzymes, instead of non-specifically inhibiting rapidly dividing cells.

Imatinib side effects

Upon treatment of bleomycin-induced lung disease with Imatinib, the improvement seen in aerated lung volume and lung function was not accompanied by a normalization of the progressively increased total lung volume. [source, 2016]
Imatinib (STI-571) that is specific for Abl and PDGF receptors attenuated liver fibrosis and increased apoptosis, suppressed expression of α-SMA and type I collagen, and further reduced proliferation (Kuo et al., 2012). [source, 2016]
Stuart Lichtman (Memorial Sloan Kettering Cancer Centre, Commack, USA) drew particular attention to the following possibilities: altered coagulation in patients taking Warfarin and Capecitabine, increased exposure to the active metabolite of Irinotecan when taken together with Ketoconazole, and increased clearance of Imatinib in patients taking St John’s wort, which is an inducer of CYP3A4. [source, 2016]
Patients with typical BCR-ABL1 transcripts (that is, b2a2 and/or b3a2) and ⩽3 months of prior Imatinib treatment were included in the molecular analysis population for evaluating molecular response rates (patients with atypical BCR-ABL1 transcripts were excluded because standard RQ-PCR methodology was not optimized for detection of atypical BCR-ABL1 transcripts; patients with >3 months of Imatinib therapy (a protocol violation) were excluded to be as conservative as possible in analyzing the efficacy of frontline nilotinib by avoiding potential confounding effects of prior Imatinib). [source, 2016]
In addition, acute liver failure caused by Imatinib and Sunitinib have also been observed (Cross et al., 2006; Tonyali et al., 2010; Shah et al., 2013). [source, 2016]
Current treatment guidelines recommend long-term continuous Imatinib therapy in advanced GIST patients, as long as clinical benefits are maintained, because rapid disease progression often occurs following treatment interruption [9-11]. [source, 2016]
PFS was calculated from the date Imatinib was started for advanced GIST to the date of disease progression or death due to any cause, whichever occurred first. [source, 2016]
Because severe skin rash occurs very early in the Imatinib treatment course, as reported here (median, 2.8 months), reduction of Imatinib dose due to severe rash may considerably decrease the overall dose intensity. [source, 2016]
The predominant infiltration of CD8+ T-lymphocytes and enhanced interleukin (IL)-18 and IL-1β was reported in drug eruption caused by Imatinib [15]. [source, 2016]
Unfortunately, it soon became apparent that certain point mutations in the kinase domain can result in Complete lack of treatment effectiveness even with increased doses of Imatinib. [source, 2016]