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Therapy Name | Imatinib + PKF118-310 |
Synonyms | |
Therapy Description | |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Imatinib | Gleevec | CGP-57148B|STI571|Imatinib mesylate | ABL Inhibitor (pan) 9 BCR-ABL Inhibitor 32 CSF1R Inhibitor 28 KIT Inhibitor 57 PDGFR Inhibitor (Pan) 30 | Gleevec (imatinib) is a multi-target inhibitor of c-Kit, Pdgfr, and Bcr-Abl (PMID: 12200353). Gleevec (imatinib) is FDA approved for c-KIT positive GIST and dermatofibrosarcoma protuberans, Philadelphia chromosome positive chronic myeloid leukemia, and FIP1L1-PDGFRA positive chronic eosinophilic leukemia (FDA.gov). |
PKF118-310 | CTNNB1 Inhibitor 27 KDM4 Inhibitor 4 | PKF118-310 inhibits KDM4A activity (PMID: 27767379) and the CTNNB1/TCF interaction, which results in apoptosis and anti-tumor activity (PMID: 19662654). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
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KIT exon11 | gastrointestinal stromal tumor | sensitive | Imatinib + PKF118-310 | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with the combination of PKF118-310 and Gleevec (imatinib) resulted in decreased viability of gastrointestinal stromal tumor (GIST) cell lines harboring KIT exon 11 mutations compared to Gleevec (imatinib) alone, in culture (PMID: 28611108). | 28611108 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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