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| Profile Name | KEAP1 inact mut |
| Gene Variant Detail | |
| Relevant Treatment Approaches |
| 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 |