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Updated: Sep 21, 2026

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
Published on: September 18, 2013
[Tyrosine kinase inhibitors--solid cancers]
1Dept. of 4th Internal Medicine, Kinki University School of Medicine.
Abstract:
Tyrosine kinase inhibitors have drawn the most attention in recent years as molecular target agents for cancer treatment. The reason for this can only be the dramatic antitumor effects shown in early clinical trials against small cell cancer and chronic myeloid leukemia by the EGFR tyrosine kinase inhibitor, ZD1839, and the BCR-Abl tyrosine kinase inhibitor, STI-571, respectively. Various hypotheses were advanced in the preliminary stages of the clinical development of such molecular target agents: "They only prevent cancer cell proliferation and have no killer cell activity; they are extremely weak, and can not be expected to reduce tumors at the clinical level. "Or:" A long time is required before their physiological activity will be expressed in an antitumor effect." However, with non-small cell lung cancer, the most difficult tumor among solid cancers for an anticancer agent to be effective, not only was ZD1839 effective, but showed clear effectiveness in combination chemotherapy in the pretreatment stage. Moreover, the time for the expression of its tumor reduction effect was virtually the same as with conventional anticancer drugs, and its effectiveness proved to last longer after its initial expression. ZD1839 has succeeded in remaking the very image of molecular target agents for cancer treatment. In what follows, we focus mainly on the EGFR tyrosine kinase inhibitor, ZD1839.
Insights
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors like ZD1839 demonstrate significant antitumor effects, challenging previous hypotheses about molecular targeted cancer therapies.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Tyrosine kinase inhibitors (TKIs) are emerging as key molecular agents for cancer treatment.
- Early trials showed promise for EGFR inhibitor ZD1839 in small cell cancer and BCR-Abl inhibitor STI-571 in chronic myeloid leukemia.
Purpose of the Study:
- To evaluate the efficacy of the EGFR tyrosine kinase inhibitor ZD1839, particularly in non-small cell lung cancer.
- To address preliminary hypotheses regarding the mechanism and timeline of TKI effectiveness.
Main Methods:
- Clinical trials involving ZD1839, focusing on non-small cell lung cancer.
- Combination chemotherapy including ZD1839 in the pretreatment stage.
Main Results:
- ZD1839 demonstrated effectiveness in non-small cell lung cancer, a notoriously difficult cancer to treat.
- Combination therapy with ZD1839 showed clear effectiveness.
- Tumor reduction effects were observed promptly and demonstrated sustained efficacy, comparable to conventional chemotherapy.
Conclusions:
- ZD1839 has significantly reshaped the perception of molecular targeted agents in cancer therapy.
- The study highlights the potent and rapid antitumor activity of EGFR TKIs.
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