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Epidermal growth factor receptor (EGFR) exon 20 insertion (EGFRex20ins) mutations are approximately found in 4-12% of non-small cell lung cancer ( NSCLC ) patients with EGFR mutations .
Epidermal growth factor receptor (EGFR) exon 20 insertion (EGFRex20ins) mutations are approximately found in 4-12% of non-small cell lung cancer ( NSCLC ) patients with EGFR mutations .
Mobocertinib (TAK-788) is an oral EGFR inhibitor targeting NSCLC EGFR gene mutations (including EGFRex20ins).
Mobocertinib (TAK-788) is an oral EGFR inhibitor targeting NSCLC EGFR gene mutations (including EGFRex20ins).
This study is a phase 1/2 dose escalation/expansion trial that evaluated the efficacy and safety of the recommended phase 2 dose of Mobocertinib for NSCLC with EGFRex20ins mutations.
Mobocertinib plasma concentration changes on the 1st day of the first course of treatment
Mobocertinib plasma concentration changes on the 1st day of the first course of treatmentIn the dose escalation cohort, 160 mg/day was determined as the recommended phase 2 dose and the maximum tolerated dose .
160mg/day is the recommended phase 2 dose and maximum tolerated dose 160mg/day is the recommended phase 2 dose and maximum tolerated dose
TRAEs
TRAEsAmong the 136 patients who received Mobocertinib 160 mg/day, the most common treatment-related adverse reactions of any grade (TRAE; >25%) were diarrhea (83%), nausea (43%), and rash (33%) ) And vomiting (26%), of which diarrhea (21%) is the only TRAE with a grade 3 and above incidence rate of more than 5%.
The most common treatment-related adverse reactions of any grade (TRAE; >25%) were diarrhea (83%), nausea (43%), rash (33%) and vomiting (26%), of which diarrhea (21%) It is the only TRAE with an incidence of more than 5% of grade 3 and above.
Anti-tumor activity
Anti-tumor activityAmong the 28 patients with EGFRex20ins mutation who received the recommended phase 2 dose of Mobocertinib, the investigator's assessment confirmed the remission rate was 43% (12/28; 95% CI 24-63%), and the median remission period was 14 Months (5.
Among the 28 patients with EGFRex20ins mutation who received the recommended phase 2 dose of Mobocertinib, the investigator's assessment confirmed the remission rate was 43% (12/28; 95% CI 24-63%), and the median remission period was 14 Months (5.
Mobocertinib has shown anti-tumor activity in NSCLC patients with different EGFRex20ins mutations, and its safety is consistent with other EGFR inhibitors.
Original source:
Riely Gregory J, Neal Joel W, Camidge D Ross et al.
org/10.
1158/2159-8290.
CD-20-1598">Activity and Safety of Mobocertinib (TAK- 788) in Previously Treated Non-Small Cell Lung Cancer With EGFR Exon 20 Insertion Mutations From a Phase 1/2 Trial in this message