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Therapy Name | Ceritinib + Selumetinib |
Synonyms | |
Therapy Description | |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Ceritinib | Zykadia | LDK378 | ALK Inhibitor 32 ROS1 Inhibitor 20 | Zykadia (ceritinib) inhibits ALK, including ALK mutations and fusions, and has additional activity against ROS1 fusions, potentially resulting in decreased tumor cell growth (PMID: 25322323, PMID: 26372962). Zykadia (ceritinib) is FDA approved for ALK-positive (rearrangements and fusions) metastatic non-small cell lung cancer (FDA.gov). |
Selumetinib | Koselugo | AZD6244|ARRY-142886 | MEK inhibitor (Pan) 26 MEK1 Inhibitor 26 MEK2 Inhibitor 24 | Koselugo (selumetinib) inhibits mitogen-activated protein kinase kinases (MEK or MAPK/ERK kinases) 1 and 2, which may prevent the activation of MEK1/2-dependent effector proteins and transcription factors, reducing cellular proliferation in various cancers (PMID: 27467210). Koselugo (selumetinib) is FDA approved for use in pediatric patients of 2 years or older with neurofibromatosis type 1 (NF1) who have symptomatic, inoperable plexiform neurofibromas (FDA.gov). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
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ALK rearrange MAP2K1 K57N | lung non-small cell carcinoma | sensitive | Ceritinib + Selumetinib | Preclinical - Patient cell culture | Actionable | In a preclinical study, NSCLC patient derived cells harboring an ALK rearrangement demonstrated resistance to Zykadia (ceritinib) due to the acquired mutation MAP2K1 K57N, however, sensitivity was restored to Zykadia (ceritinib) with the addition of Koselugo (selumetinib), resulting in decreased cell survival in culture and reduced tumor volume in xenograft models (PMID: 25394791). | 25394791 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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