Drug intelligence / Profile preview

gefitinib + cisplatin + 5-fluorouracil

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral (gefitinib), Intravenous (cisplatin), Intravenous (5-fluorouracil)
01

Overview

Gefitinib + cisplatin + 5-fluorouracil is a three-drug combination therapy, typically used experimentally or in clinical research for certain solid tumors. **Gefitinib** is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that blocks EGFR autophosphorylation and downstream signaling, leading to suppression of tumor cell proliferation and survival[1][2]. **Cisplatin** is a platinum-based chemotherapy agent that crosslinks DNA, causing DNA damage and triggering apoptosis[1][3]. **5-fluorouracil (5-FU)** is an antimetabolite chemotherapy that inhibits thymidylate synthase, interfering with DNA and RNA synthesis and function[3][5]. This combination aims to target tumor cells via multiple independent mechanisms—EGFR pathway inhibition (targeted therapy), DNA damage (alkylating agent), and antimetabolite activity (chemotherapy). Synergistic effects have been observed in preclinical models, particularly where EGFR inhibitors like gefitinib sensitize tumor cells to cisplatin-induced apoptosis[1]. The combination is primarily studied in head and neck cancers, colorectal cancers, and other epithelial malignancies, but is not universally approved for a specific indication and typically used in clinical trials or research settings.

Brand names
Adrucil
Other names
gefitinib + cisplatin + 5-fluorouracil
02

Targets

DNA-PK (DNA-dependent protein kinase)ERBB2 (Erb-b2 receptor tyrosine kinase 2)DNATS (Thymidylate synthase)

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