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gefitinib + etoposide
- Development stage
- Phase 2
- Lead developer
- AstraZeneca
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Gefitinib + etoposide is a combination of two small molecule anticancer agents used experimentally and in clinical trials for the treatment of various malignancies. Gefitinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that blocks EGFR signaling by binding to its ATP-binding site, thereby inhibiting downstream pathways involved in cell proliferation and survival. Etoposide is a topoisomerase II inhibitor that induces DNA strand breaks and inhibits DNA synthesis by stabilizing the enzyme-DNA complex during replication. The combination has shown synergistic effects in preclinical studies; gefitinib can enhance the cytotoxicity of etoposide by inhibiting repair of DNA damage induced by etoposide and promoting apoptosis. This combination has been investigated primarily for solid tumors such as non-small cell lung cancer and bladder cancer[1][2].
- Brand names
- Toposar
- Other names
- gefitinibetoposide
02
Targets
TOP2A (DNA topoisomerase II)EGFR (Epidermal growth factor receptor)
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