Which medications in the drug class Antineoplastics, EGFR Inhibitor are used in the treatment of Non-Small Cell Lung Cancer (NSCLC)?

Updated: Jul 15, 2021
  • Author: Winston W Tan, MD, FACP; Chief Editor: Nagla Abdel Karim, MD, PhD  more...
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Answer

Antineoplastics, EGFR Inhibitor

EGFR is expressed on the cell surface of both normal and cancer cells and plays a role in the processes of cell growth and proliferation.

Osimertinib (Tagrisso)

EGFR kinase inhibitor, which binds irreversibly to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion). It is indicated for metastatic EGFR T790M mutation–positive NSCLC in patients whose disease has progressed on or after EGFR TKI therapy. It is also used as first-line treatment for metastatic NSCLC in patients with EGFR exon 19 deletions or exon 21 L858R mutations, and as adjuvant therapy after tumor resection in NSCLC patients whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations.

Gefitinib (Iressa)

Gefitinib reversibly inhibits the kinase activity of wild-type and certain activating mutations of epidermal growth factor receptor (EGFR), preventing autophosphorylation of tyrosine residues associated with the receptor, thereby inhibiting further downstream signalling and blocking EGFR-dependent proliferation. It is indicated for the treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test.

Erlotinib (Tarceva)

Erlotinib is pharmacologically classified as a HER1/epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). EGFR is expressed on the cell surface of normal cells and cancer cells. As of late 2016, it is approved for NSCLC in patients whose tumors have EGFR exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test for first-line treatment, maintenance treatment, or as second or greater line treatment after progression following at least 1 prior chemotherapy regimen. It also is indicated in combination with ramucirumab for first-line treatment of patients with metastatic NSCLC whose tumors have EGFR exon 19 deletions or exon 21 (L858R) substitution mutations.

Afatinib (Gilotrif)

Afatinib covalently binds to the kinase domains of EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) and irreversibly inhibits tyrosine kinase autophosphorylation, resulting in downregulation of ErbB signaling. It demonstrates inhibition of autophosphorylation and in vitro proliferation of cell lines expressing wild-type EGFR or those expressing selected EGFR exon 19 deletion mutations or exon 21 L858R mutations, including some with a secondary T790M mutations

Afatinib is indicated for first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) who tumors have non-resistant epidermal growth factor receptor (EGFR) mutations as detected by an FDA-approved test. Additionally, afatinib is indicated for first-line use in metastatic NSCLC for 3 additional nonresistant EGFR mutations (ie, L861Q, G719X, S768I). It is also indicated for metastatic squamous NSCLC which has progressed after platinum-based chemotherapy.

Dacomitinib (Vizimpro)

Irreversible kinase inhibitor of the human EGFR family (EGFR/HER1, HER2, and HER4) and certain EGFR-activating mutations (exon 19 deletion or the exon 21 L858R substitution mutation). It is indicated for first-line treatment of patients with metastatic non-small lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 19 deletion or exon 21 L858R substitution mutations as detected by an FDA-approved test.

Amivantamab (Amivantamab-vmjw, Rybrevant)

Bispecific antibody that binds to the extracellular domains of EGFR and MET; indicated for locally advanced or metastatic NSCLC with EGFR exon 20 insertion mutations, as detected by an FDA-approved test, in adults whose disease has progressed on or after platinum-based chemotherapy


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