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DRUG:

TAS-121

i
Other names: TAS-121, TAS 121
Associations
Trials
Company:
Otsuka
Drug class:
EGFR inhibitor
Related drugs:
Associations
Trials
almost4years
HSP90 inhibition overcomes EGFR amplification-induced resistance to third-generation EGFR-TKIs. (PubMed, Thorac Cancer)
EGFR amplification confers resistance to third-generation EGFR-TKIs which can be overcome by HSP90 inhibition. The results provide a preclinical rationale for the use of HSP90 inhibitors to overcome EGFR amplification-mediated resistance.
Journal
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R • EGFR T790M • EGFR amplification • EGFR overexpression
|
Tagrisso (osimertinib) • TAS-121
over4years
TAS-121, a selective mutant EGFR inhibitor, shows activity against tumors expressing various EGFR mutations including T790M and uncommon mutations G719X. (PubMed, Mol Cancer Ther)
TAS-121 potently inhibited common activating and resistance EGFR mutations to the same extent as another third-generation EGFR-TKI (osimertinib). Moreover, TAS-121 displayed antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models, and achieved an objective response in NSCLC patients with EGFR mutations including G719A mutation. In conclusion, TAS-121 is a novel third-generation EGFR-TKI and demonstrates anti-tumor activities in patients with NSCLC expressing either common or uncommon EGFR mutations.
Journal
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R • EGFR T790M • EGFR expression • EGFR L861Q • EGFR G719X • EGFR G719A • EGFR G719S
|
Tagrisso (osimertinib) • TAS-121