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capecitabine + gefitinib
- Development stage
- Unknown
- Lead developer
- AstraZeneca
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Capecitabine + gefitinib is an investigational combination therapy consisting of two oral small molecule drugs used in oncology. Capecitabine is a prodrug of 5-fluorouracil (5-FU), classified as an antimetabolite, which interferes with DNA synthesis and disrupts cancer cell proliferation by inhibiting thymidylate synthase and incorporating into DNA and RNA, leading to apoptosis[3][6]. Gefitinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that blocks EGFR-mediated signaling pathways involved in tumor cell proliferation and survival[4]. The combination has been studied primarily as a second-line treatment for advanced or metastatic cancers, including colorectal cancer, after failure of first-line chemotherapy. Clinical studies have reported significant skin toxicities such as exanthema and hand-foot syndrome with this regimen[1][2].
- Brand names
- IressaXeloda
- Other names
- none
02
Targets
EGFR (Epidermal growth factor receptor)TS (Thymidylate synthase)
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