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 dosage

The respective median times since Original diagnosis were 186 and 171 weeks in studies 1199 and 1036, and a 600–800 mg maximum prior Imatinib dose was the most frequent in both studies (43 % in Study 1199 and 47 % in Study 1036). [source, 2016]
For patients receiving long-term Imatinib treatment, maintaining the continued administration at a sufficient dose is critical for maintaining the clinical effectiveness of Imatinib [11,12]. [source, 2016]
Imatinib is generally well tolerated and most adverse events are mild and can be managed without dose reduction or treatment interruption [2-5]; however, some patients experience severe toxicity which may result in reduced patient compliance and dose intensity. [source, 2016]
This analysis focused on a group of 42 patients who developed severe skin rash requiring major interventions defined as interruption or dose reduction of Imatinib and/or systemic steroid use (group 1). [source, 2016]
Major interventions for skin rash were administered in the remaining 40 patients, including systemic steroids only (n=17, 40.5%), Imatinib dose modification only (dose reduction only [n=6, 14.3%], dose interruption only [n=2, 4.8%], dose reduction+ interruption [n=6, 14.3%]), or the combined use of systemic steroids and Imatinib dose modification (steroids+dose reduction [n=2, 4.8%], steroids+interruption [n=3, 7.1%], steroids+dose reduction+interruption [n=4, 9.5%]). [source, 2016]
Of 14 patients whose first intervention failed, three patients (21.4%) discontinued Imatinib due to uncontrolled severe rash and a second intervention was administered in the remaining 11 patients (78.6%); only systemic steroids (n=6, 42.9%), Imatinib dose modification (n=2, 14.3%; dose reduction and interruption in each one), and systemic steroids+Imatinib dose modification (steroids+Imatinib reduction [n=1, 7.1%], steroids+Imatinib interruption [n=2, 14.3%]). [source, 2016]
Of six patients whose second intervention failed, two patients (33.2%) discontinued Imatinib and a third intervention was administered in the remaining four patients: systemic steroids (n=1, 25.0%), Imatinib dose reduction (n=1, 25.0%), or steroids Imatinib dose reduction (n=2, 50.0%). [source, 2016]
Interventions were successful over the entire clinical course in 28 patients (66.8%) who were able to Maintain Imatinib without permanent discontinuation due to skin rash with a dose of 800 mg/day (n=1), 400 mg/day (n=19), 300 mg/day (n=5), or 200 mg/day (n=3). [source, 2016]
Of note, patients administered systemic steroids for rash tended to Maintain a higher Imatinib dose intensity than patients who did not (median relative dose intensity at 6 months, 1.00 vs. 0.79, respectively; p=0.122) [source, 2016]
No association was observed between the outcomes of the first intervention and clinical factors (e.g., sex, age), and the nature of the interventions, including types of intervention (e.g., Imatinib dose modification, systemic steroid use—starting dose, duration of starting or tapering dose) (Table 2). [source, 2016]