Erlotinib (Tarceva)

Targeted Therapy · Approved since 2004

US Off-label EU EMA Approved ES Hospital use off-label in CRC Oral 20 Clinical Trials
EGFR

Description

Erlotinib is an oral tyrosine kinase inhibitor that targets the epidermal growth factor receptor (EGFR). In colorectal cancer, erlotinib has been evaluated as a maintenance therapy following standard chemotherapy and bevacizumab treatment, particularly in patients with specific KRAS mutation status. The drug represents an EGFR-targeted approach for patients with metastatic colorectal cancer, though its efficacy in CRC is limited compared to other tumor types.

Mechanism of Action

Erlotinib works by selectively inhibiting the tyrosine kinase activity of EGFR, blocking downstream signaling pathways that promote tumor cell proliferation and survival. By binding to the ATP-binding site of EGFR, erlotinib prevents autophosphorylation and subsequent activation of pathways such as RAS/RAF/MEK and PI3K/AKT that drive cancer progression.

Molecular Targets

Side Effects

Diarrhea Rash Fatigue Nausea Vomiting Decreased appetite Stomatitis Dry skin

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

Clinical Trials

NCT05525858 Not Applicable
Recruiting
KPMNG Study of MOlecular Profiling Guided Therapy Based on Genomic Alterations in Advanced Solid Tumors II
South Korea
NCT04449874 Phase 1
Active, not recruiting
A Study to Evaluate the Safety, Pharmacokinetics, and Activity of GDC-6036 Alone or in Combination in Participants With Advanced or Metastatic Solid Tumors With a KRAS G12C Mutation
United States, Australia, Belgium, Brazil, Canada, Hungary, Israel, Italy, Kenya
NCT04165031 Phase 1
Archived
A Study of LY3499446 in Participants With Advanced Solid Tumors With KRAS G12C Mutation
United States, Australia
NCT02961374 Phase 2
Archived
Erlotinib Hydrochloride in Reducing Duodenal Polyp Burden in Patients With Familial Adenomatous Polyposis at Risk of Developing Colon Cancer
United States, Puerto Rico
NCT03086538 Phase 2
Archived
Pemetrexed Plus Tarceva as Salvage Treatment in EGFR Overexpressed Metastatic Colorectal Cancer Patients Who Were Failed After Standard Chemotherapy
South Korea
NCT02723578 Phase 2
Archived
Pemetrexed and Erlotinib for Metastatic Colorectal Cancer
South Korea
View all 20 clinical trials →