GLEEVEC for KIT+ GIST
Redefining treatment of patients with KIT+ GIST
GLEEVEC® (imatinib mesylate) tablets are indicated for:
- Patients with KIT (CD117)-positive unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST)
- Adjuvant treatment of adult patients following complete gross resection of KIT (CD117)-positive GIST
Study findings† demonstrate that continuing adjuvant GLEEVEC (to 3 years) provided a significant RFS and OS benefit (median 42- and 48-month follow-up, respectively)1
GLEEVEC is designed to work by potentially inhibiting c-KIT, a tyrosine kinase receptor, which is mutated and activated in GIST cells. In this way, as demonstrated in vitro, cell proliferation is inhibited and apoptosis is induced. GLEEVEC is also an inhibitor of the receptor tyrosine kinases for breakpoint cluster region-Abelson (Bcr-Abl), platelet-derived growth factor (PDGF), and stem cell factor (SCF), and inhibits PDGF- and SCF-mediated cellular events.1
†Scandinavian Sarcoma Group (SSG) XVII/AIO Phase 3 trial: Multicenter, randomized, open-label trial with a median follow-up period of 42 and 48 months, respectively, for recurrence-free survival (RFS) and overall survival (OS); GLEEVEC 400 mg/day was the dosage for all patients on active therapy.1,2
Important Safety Considerations
GLEEVEC is often associated with edema and, occasionally, serious fluid retention. Severe fluid retention was reported in 9% to 13.1% of patients taking GLEEVEC for KIT+ GIST. Patients should be weighed and monitored regularly for signs and symptoms of fluid retention, which can be serious or life threatening, and be advised to report any rapid, unexpected weight gain. The probability of edema tended to be increased among older patients (>65 years) or those taking higher doses of GLEEVEC. Severe edema was observed in 182 patients (11.1%). If severe fluid retention occurs, manage with diuretic therapy and withhold GLEEVEC until the event has resolved, and then resume depending on the initial severity of the event.
Review the following clinical information before prescribing treatment with GLEEVEC for KIT+ GIST:
- Response rates
- Reducing severity of some adverse reactions
- Important Safety Information
- Case studies
RFS=recurrence-free survival; OS=overall survival.
1. GLEEVEC® (imatinib mesylate) tablets prescribing information. East Hanover, NJ: Novartis Pharmaceuticals Corporation; January 2012.
2. Scandinavian Sarcoma Group and Sarcoma Group of the AIO, Germany. Short (12 months) versus long (36 months) duration of adjuvant treatment with the tyrosine kinase inhibitor imatinib mesylate of operable GIST with a high risk for recurrence: a randomized phase III study. http://www.ssg-org.net/wp-content/uploads/2011/05/SSG-XVIII-April20091.pdf. Version April 2009. Accessed February 9, 2012.