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Therapy Name | Selumetinib + SHP099 |
Synonyms | |
Therapy Description | |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
SHP099 | SHP-099|SHP 099 | SHP2 Inhibitor 12 | SHP099 is an allosteric inhibitor of SHP2 that stabilizes SHP2 in its autoinhibited conformation, which reduces downstream signaling and potentially leads to decreased growth of receptor tyrosine kinase-driven tumors (PMID: 27362227, PMID: 31043123). | |
Selumetinib | Koselugo | AZD6244|ARRY-142886 | MEK inhibitor (Pan) 22 MEK1 Inhibitor 20 MEK2 Inhibitor 18 | 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 |
---|---|---|---|---|---|---|---|
Unknown unknown | ovarian cancer | not applicable | Selumetinib + SHP099 | Preclinical - Cell culture | Actionable | In a preclinical study, the combination therapy of Selumetinib (AZD6244) and SHP099 resulted in decreased colony formation and reduced cell viability in ovarian cancer cells in culture and inhibition of tumor growth and reduced tumor angiogenesis in a patient-derived xenograft (PDX) model of ovarian cancer (PMID: 30045908). | 30045908 |
PTPN11 T253M PTPN11 Q257L | lung non-small cell carcinoma | resistant | Selumetinib + SHP099 | Preclinical - Cell culture | Actionable | In a preclinical study, pancreatic ductal adenocarcinoma cells co-expressing PTPN11 T253M and PTPN11 Q257L were resistant to the combination therapy, Selumetinib (AZD6244) and SHP099, in culture (PMID: 30045908). | 30045908 |
Unknown unknown | triple-receptor negative breast cancer | not applicable | Selumetinib + SHP099 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination therapy of SHP099 and Selumetinib (AZD6244) led to decreased cell viability and reduced colony formation in triple-receptor negative breast cancer cells in culture and tumor regression in xenograft models (PMID: 30045908). | 30045908 |
Unknown unknown | pancreatic ductal adenocarcinoma | not applicable | Selumetinib + SHP099 | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, the combination of SHP099 and Selumetinib (AZD6244) resulted in greater sensitivity compared to either agent alone in pancreatic ductal adenocarcinoma cells, demonstrating decreased cell viability and reduced colony formation in culture and decreased tumor growth in patient-derived xenograft (PDX) models (PMID: 30045908). | 30045908 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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