Gefitinib (Iressa)

Targeted Therapy · Approved since 2003

US Off-label EU EMA Approved ES Funded by SNS off-label in CRC Oral 8 Clinical Trials
EGFR

Description

Gefitinib is an oral tyrosine kinase inhibitor that targets the epidermal growth factor receptor (EGFR). While primarily approved for non-small cell lung cancer, gefitinib has been evaluated in colorectal cancer patients, particularly those with advanced or metastatic disease. The drug blocks EGFR signaling pathways that promote tumor growth and survival. In colorectal cancer, gefitinib has been tested both as monotherapy and in combination with conventional chemotherapy regimens.

Mechanism of Action

Gefitinib selectively inhibits the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) by binding to the ATP-binding site of the receptor's intracellular domain. This prevents EGFR autophosphorylation and downstream activation of signaling cascades including RAS/RAF/MEK/ERK and PI3K/AKT pathways. By blocking these pathways, gefitinib inhibits cellular processes essential for tumor growth, including proliferation, angiogenesis, and metastasis.

Molecular Targets

Side Effects

Diarrhea Skin rash Acne-like dermatitis Dry skin Nausea Vomiting Anorexia Asthenia Interstitial lung disease

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT00087334 Phase 1
Terminated
Capecitabine, Oxaliplatin, and Gefitinib in Treating Patients With Metastatic Colorectal Cancer
United States
NCT00234429 Phase 2
Archived
A Phase 2 Study of Tomudex & Iressa as Second Line Chemotherapy in Subjects With Colorectal Carcinoma
Spain
NCT00052585 Phase 2
Terminated
Gefitinib and Combination Chemotherapy in Treating Patients With Advanced or Recurrent Colorectal Cancer
United States
NCT00030524 Phase 2
Archived
ZD 1839 in Treating Patients With Locally Advanced or Metastatic Colorectal Cancer
United States
NCT00026364 Phase 1
Completed
ZD 1839 Plus Combination Chemotherapy in Treating Patients With Locally Advanced, Locally Recurrent, or Metastatic Colorectal Cancer
United States
NCT00025350 Phase 2
Archived
Gefitinib in Treating Patients With Recurrent Metastatic Colorectal Cancer
United States
View all 8 clinical trials →