Last reviewed 2026-04-23 · How we verify

Erlotinib /Gefitinib

Erlotinib /Gefitinib is a EGFR tyrosine kinase inhibitor Small molecule drug developed by Zhejiang Cancer Hospital. It is currently in Phase 3 development for Non-small cell lung cancer (NSCLC) with EGFR mutations, Advanced or metastatic NSCLC. Also known as: EGFR-TKI.

Erlotinib and gefitinib are tyrosine kinase inhibitors that block epidermal growth factor receptor (EGFR) signaling to inhibit cancer cell proliferation.

Erlotinib and gefitinib are tyrosine kinase inhibitors that block epidermal growth factor receptor (EGFR) signaling to inhibit cancer cell proliferation. Used for Non-small cell lung cancer (NSCLC) with EGFR mutations, Advanced or metastatic NSCLC.

At a glance

Mechanism of action

Both drugs competitively inhibit EGFR tyrosine kinase activity, preventing autophosphorylation and downstream signaling through the MAPK and PI3K/AKT pathways. This leads to cell cycle arrest and apoptosis in EGFR-dependent tumors, particularly those with activating EGFR mutations. They are selective for EGFR over other receptor tyrosine kinases.

Approved indications

• Non-small cell lung cancer (NSCLC) with EGFR mutations
• Advanced or metastatic NSCLC

Common side effects

• Rash/acneiform dermatitis
• Diarrhea
• Nausea
• Vomiting
• Fatigue
• Anorexia
• Interstitial lung disease

Key clinical trials

• A Prospective Cohort Study of Zorifertinib as a First-line Treatment in Patients With Epidermal Growth Factor Receptor-mutant Advanced Non-small Cell Lung Cancer With Central Nervous System (CNS) Metastases
• Emulation of the FLAURA (NCT02296125) Trial Using Specialty Oncology Electronic Health Records Databases
• A Study of Ramucirumab (LY3009806) in Combination With Erlotinib in Previously Untreated Participants With EGFR Mutation-Positive Metastatic NSCLC (RELAY) (PHASE3)
• A Prospective Multicenter Study of the Association Between TCM Syndromes and EGFR-TKI Efficacy in Lung Cancer Patients
• AZD9291 Versus Gefitinib or Erlotinib in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer (PHASE3)
• An Autologous NK/CIK Cell Product (PB101) in Combination With EGFR-TKI for Treating Lung Cancer (PHASE1)
• Study to Assess the Effect of Itraconazole (a CYP3A4 Inhibitor) on the Pharmacokinetics of AZD9291, in Patients With EGFR Positive Non-small Cell Lung Cancer. Patients Will be Chosen From Those Who Have Already Been Prescribed an EGFR TKI Medicine (Such as Iressa or Tarceva) (PHASE1)
• First Line Treatment in EGFR Mutation Positive Advanced NSCLC Patients With Central Nervous System (CNS) Metastases (PHASE2, PHASE3)

Primary sources

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Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Erlotinib /Gefitinib CI brief — competitive landscape report
• Erlotinib /Gefitinib updates RSS · CI watch RSS
• Zhejiang Cancer Hospital portfolio CI

Frequently asked questions about Erlotinib /Gefitinib

Related

• Drug class: All EGFR tyrosine kinase inhibitor drugs
• Target: All drugs targeting EGFR (Epidermal Growth Factor Receptor)
• Manufacturer: Zhejiang Cancer Hospital — full pipeline
• Therapeutic area: All drugs in Oncology
• Indication: Drugs for Non-small cell lung cancer (NSCLC) with EGFR mutations
• Indication: Drugs for Advanced or metastatic NSCLC
• Also known as: EGFR-TKI
• Compare: Erlotinib /Gefitinib vs similar drugs
• Pricing: Erlotinib /Gefitinib cost, discount & access