Gleevec

Definition

Gleevec, also known as imatinib, is a targeted cancer therapy drug primarily used to treat certain types of leukemia and gastrointestinal stromal tumors (GISTs). It works by inhibiting specific tyrosine kinases, such as BCR-ABL, that are involved in the proliferation of cancer cells. Gleevec represents a significant advancement in rational drug design, as its development was based on understanding the molecular mechanisms underlying these cancers.

5 Must Know Facts For Your Next Test

1. Gleevec was approved by the FDA in 2001 and was one of the first drugs to successfully use targeted therapy against cancer.
2. The drug specifically targets the BCR-ABL fusion protein found in chronic myeloid leukemia (CML) cells, which allows for a more effective treatment with fewer side effects than traditional chemotherapy.
3. Gleevec revolutionized treatment protocols for GISTs, providing significant survival benefits for patients who previously had limited options.
4. It has transformed the prognosis for many patients with CML from a life-threatening condition to a manageable chronic disease.
5. Gleevec's development exemplifies the principles of rational drug design, where drug efficacy is directly linked to its ability to inhibit a specific molecular target associated with cancer cell growth.

Review Questions

• How does Gleevec exemplify the principles of rational drug design in treating cancer?
  • Gleevec exemplifies rational drug design by targeting the specific molecular abnormality associated with certain cancers, particularly the BCR-ABL fusion protein in chronic myeloid leukemia (CML). Researchers understood that this fusion protein was critical for the uncontrolled proliferation of cancer cells, and by designing Gleevec to inhibit this target, they were able to create an effective treatment that directly disrupts the cancer's growth mechanism. This targeted approach minimizes damage to normal cells compared to conventional chemotherapy.
• Discuss the role of tyrosine kinases in cancer biology and how Gleevec interferes with their function.
  • Tyrosine kinases are enzymes that play a pivotal role in signaling pathways that regulate cell division, survival, and differentiation. In many cancers, including CML, abnormal activation of tyrosine kinases leads to unchecked cellular proliferation. Gleevec functions as a tyrosine kinase inhibitor, specifically blocking the action of BCR-ABL and other related kinases. By inhibiting these pathways, Gleevec effectively disrupts the signaling that promotes cancer cell growth, resulting in reduced tumor size and improved patient outcomes.
• Evaluate the impact of Gleevec on patient outcomes compared to traditional chemotherapy treatments.
  • The introduction of Gleevec has significantly changed patient outcomes for those with chronic myeloid leukemia and gastrointestinal stromal tumors. Unlike traditional chemotherapy, which often causes widespread damage to rapidly dividing cells—both cancerous and healthy—Gleevec specifically targets cancer cells with minimal impact on normal tissues. This targeted approach leads to fewer side effects and a better quality of life for patients while transforming previously fatal conditions into manageable chronic diseases. The success of Gleevec has paved the way for further development of targeted therapies across various cancers.

Related terms

Tyrosine Kinase Inhibitors: A class of drugs that block the action of enzymes known as tyrosine kinases, which play a crucial role in cell signaling and cancer cell growth.

Rational Drug Design: A systematic approach to drug discovery that uses knowledge of biological targets to design new therapeutic agents with specific action against diseases.

BCR-ABL Fusion Protein: An abnormal protein created by the fusion of parts of two different genes, BCR and ABL, which is commonly associated with chronic myeloid leukemia (CML).