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Mobocertinib was the first oral drug for EGFR exon 20 insertion lung cancer, approved in 2021 and withdrawn in 2023-24 after its confirmatory trial failed.
Mobocertinib is a covalent EGFR inhibitor designed for exon 20 insertion mutations, which resist earlier EGFR TKIs, while sparing wild-type EGFR relative to those agents. It received accelerated US approval in 2021 on a 28% response rate in patients who had progressed after platinum chemotherapy, the first oral drug for this subgroup. The confirmatory EXCLAIM-2 trial (2023) failed to beat platinum chemotherapy in the first-line setting, and Takeda withdrew the drug globally, with the US withdrawal completed in 2024. Diarrhoea and QT prolongation were prominent toxicities. Amivantamab and sunvozertinib now cover the exon 20 insertion indication. Mobocertinib shows how an accelerated approval can be reversed when the confirmatory trial does not deliver.
Covalent EGFR inhibitor designed for exon 20 insertion mutations, sparing wild-type EGFR relative to earlier TKIs. Connects to EGFR.
1.Mobocertinib slips into a pocket on EGFR.
Background: ADC sequencing, Antigen escape (antigen loss, lineage switch), BCG-unresponsive, Castration-resistant prostate cancer (CRPC), Circulating tumour DNA (ctDNA). Also on OnCo: Resistance: how tumours escape each drug class · Lines of therapy.
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Treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with EGFR exon 20 insertion mutations, as detected by an FDA-approved test, whose disease has progressed on or after platinum-based chemotherapy
Accelerated approval on a surrogate endpoint, with a confirmatory trial required.
Treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with EGFR exon 20 insertion mutations, as detected by an FDA-approved test, whose disease has progressed on or after platinum-based chemotherapy
Withdrawn: the indication came off the label 2.8 years after its accelerated approval.
| Region | Year | Indication |
|---|---|---|
| US | 2021 | EGFR exon 20 insertion NSCLC after platinum · Withdrawn 2023-24 |
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Query for this drug: (TITLE:"Mobocertinib" OR ABSTRACT:"Mobocertinib" OR TITLE:"Exkivity" OR ABSTRACT:"Exkivity") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Mobocertinib, not a curated reading list.
Shares EGFR exon 20 insertion, EGFR exon 20 insertion, EGFR-mutated non-small-cell lung cancer, EGFR.
Shares Takeda, EGFR-mutated non-small-cell lung cancer, Non-small-cell lung cancer.
Shares EGFR exon 20 insertion, EGFR-mutated non-small-cell lung cancer, EGFR, Non-small-cell lung cancer.
Shares Lung cancer: the failed and stopped programmes, and why, EGFR, Non-small-cell lung cancer.
Shares Lung cancer: the failed and stopped programmes, and why, Lung cancer (all types), Non-small-cell lung cancer.
Shares Lung cancer: the failed and stopped programmes, and why, Lung cancer (all types).
Shares EGFR exon 20 insertion, EGFR exon 20 insertion, Non-small-cell lung cancer.
Shares Takeda, Non-small-cell lung cancer.