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Zipalertinib is an investigational new drug that is being evaluated for the treatment of non-small cell lung cancer (NSCLC) with EGFR mutations, particularly exon 20 insertion mutations. [ 1 ] [ 2 ] [ 3 ]
Treatment of adults with locally advanced, unresectable (stage III) non-small cell lung cancer (NSCLC) whose disease has not progressed during or following concurrent or sequential platinum-based chemoradiation therapy and whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test [2] Repotrectinib
In the US, EGFR exon 19 deletions, exon 21 L858R mutations or the T790M status of the patient prior to treatment with osimertinib must be detected by a companion diagnostic test. [4] The Food and Drug Administration (FDA) has approved multiple tests, including FoundationOne CDx for this purpose. [ 13 ]
Erlotinib, sold under the brand name Tarceva among others, is a medication used to treat non-small cell lung cancer (NSCLC) and pancreatic cancer. [4] Specifically it is used for NSCLC with mutations in the epidermal growth factor receptor (EGFR) — either an exon 19 deletion (del19) or exon 21 (L858R) substitution mutation — which has spread to other parts of the body. [4]
Mobocertinib (Exkivity) was approved for medical use in the United States in September 2021, and it is indicated for adults with locally advanced or metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 20 insertion mutations, as detected by an FDA-approved test, whose disease has progressed on or after ...
In September 2024, the FDA approved amivantamab-vmjw with carboplatin and pemetrexed for adults with locally advanced or metastatic non-small-cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R substitution mutations whose disease has progressed on or after treatment with an EGFR tyrosine ...
T790M, also known as Thr790Met, is a gatekeeper mutation of the epidermal growth factor receptor (EGFR). The mutation substitutes a threonine (T) with a methionine (M) at position 790 of exon 20, [1] affecting the ATP binding pocket of the EGFR kinase domain.
EGFR signaling cascades Diagram of the EGF receptor highlighting important domains. Epidermal growth factor receptor (EGFR) is a transmembrane protein that is activated by binding of its specific ligands, including epidermal growth factor and transforming growth factor alpha (TGF-α). [7]