Information on How GLEEVEC Works for KIT+ GIST
How GLEEVEC Works
GLEEVEC® is designed to affect what is believed to be the root cause of KIT–positive gastrointestinal stromal tumors (KIT+ GIST)–the KIT protein created by the c-kit gene. By blocking the signal from the abnormal KIT protein that causes the build up of abnormal GIST cells, GLEEVEC halts cell proliferation in vitro and induces apoptosis.
By slowing the rate of growth and restoring normal cellular life cycles to these abnormal cells, GLEEVEC helps prevent rampant cellular growth and tumor formation in patients with KIT+ GIST. While Gleevec is targeted for KIT+ GIST, it targets several receptor tyrosine kinase activities (RTK): c-KIT, Bcr-Abl, platelet derived growth factor (PDGF), and stem cell factor (SCF)—preventing or inhibiting activation.
GLEEVEC tablets are indicated for:
- Patients with Kit (CD117)–positive gastrointestinal stromal tumors (GIST) that are cancerous, cannot be surgically removed, and/or have spread to other parts of the body
- If GISTs have spread to other parts of the body, KIT+ GIST is classified as metastatic
- Adult patients after surgery who have had their Kit (CD117)–positive GISTs completely removed
- In this case, the use of GLEEVEC is classified as adjuvant therapy
- GLEEVEC is the only approved front-line adjuvant therapy for KIT+ GIST
- GLEEVEC significantly improves recurrence-free survival (with a median follow-up of 14 months [range, 0 to ~54 months])
- In the adjuvant clinical study, GLEEVEC was administered for 1 year in patients with tumor size ≥3cm. The optimal duration of GLEEVEC therapy is unknown.
It is important to follow your doctor's instructions for taking GLEEVEC every day.
DO NOT TAKE GLEEVEC IF...
- You are pregnant or could be pregnant. Harm to the unborn child can occur when administered to pregnant women. Therefore, women should not become pregnant and should be advised of the potential risk to the unborn child if GLEEVEC is used during pregnancy
- You are breast-feeding, because of the potential for serious adverse reactions in nursing infants
- Sexually active females should use highly effective birth control while taking GLEEVEC