Molecular Profile Detail

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Profile Name KEAP1 inact mut
Gene Variant Detail

KEAP1 inact mut (loss of function)

Relevant Treatment Approaches

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Molecular Profile Indication/Tumor Type Response Type Relevant Treatment Approaches Therapy Name Approval Status Evidence Type Efficacy Evidence References
KEAP1 inact mut gallbladder cancer resistant Fluorouracil Preclinical Actionable In a preclinical study, gallbladder cancer cells harboring KEAP inactivating mutations had increased NRF2 activation and demonstrated resistance to Adrucil (fluorouracil) in culture (PMID: 18692501). 18692501
KEAP1 inact mut lung adenocarcinoma sensitive Carboplatin + MSU38225 Preclinical - Cell line xenograft Actionable In a preclinical study, MSU38225 and Paraplatin (carboplatin) combination treatment synergistically inhibited growth of a lung cancer cell line harboring a KEAP1 inactivating mutation in culture and slowed tumor growth in a cell line xenograft model compared to vehicle or Paraplatin (carboplatin) alone (PMID: 34158350). 34158350
KEAP1 inact mut lung adenocarcinoma sensitive MSU38225 Preclinical - Cell culture Actionable In a preclinical study, MSU38225 inhibited Nrf2 transcriptional activity and downstream pathway activation, increased Nrf2 degradation, and inhibited growth of lung cancer cells harboring a KEAP1 inactivating mutation in 2D and 3D culture (PMID: 34158350). 34158350
KEAP1 inact mut lung adenocarcinoma sensitive Fluorouracil + MSU38225 Preclinical - Cell culture Actionable In a preclinical study, MSU38225 and Adrucil (fluorouracil) combination treatment inhibited growth of a lung cancer cell line harboring a KEAP1 inactivating mutation in culture (PMID: 34158350). 34158350