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Therapy Name | VS-5584 |
Synonyms | |
Therapy Description |
VS-5584 inhibits mTOR kinase and all class I PI3K isoforms, disrupting phosphorylation of substrates downstream of PI3K and mTOR, thereby preventing cell proliferation and inhibiting tumor growth (PMID: 23270925). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
VS-5584 | SB-2343|SB2343|VS5584 | mTOR Inhibitor 51 PI3K Inhibitor (Pan) 38 | VS-5584 (SB-2343) inhibits mTOR kinase and all class I PI3K isoforms, disrupting phosphorylation of substrates downstream of PI3K and mTOR, thereby preventing cell proliferation and inhibiting tumor growth (PMID: 23270925, PMID: 32286946). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
Unknown unknown | breast cancer | not applicable | VS-5584 | Preclinical - Patient cell culture | Actionable | In a preclinical study, treatment with VS-5584 resulted in decreased cancer stem cell (CSC) number in a triple-negative breast cancer cell line in culture and in xenograft models, and decreased CSCs in patient breast cancer tumor samples in culture (PMID: 25432176). | 25432176 |
FLT3 act mut | acute myeloid leukemia | sensitive | VS-5584 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, VS-5584 inhibited PI3K/mTOR signaling and cell proliferation in a FLT3-ITD positive human acute myeloid leukemia cell line in culture, and inhibited tumor growth in xenograft models (PMID: 23270925). | 23270925 |
PIK3CA mutant | Advanced Solid Tumor | sensitive | VS-5584 | Preclinical | Actionable | In preclinical studies, VS-5584 demonstrated efficacy in a variety of cancer cell lines, particularly those harboring PIK3CA mutations (PMID: 23270925). | 23270925 |
Unknown unknown | Advanced Solid Tumor | not applicable | VS-5584 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, VS-5584 inhibited growth of a variety of human tumor cell lines in culture and inhibited tumor growth in cell line xenograft models (PMID: 23270925). | 23270925 |
Unknown unknown | ovarian cancer | not applicable | VS-5584 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, VS-5584 reduced the proportion of cancer stem cells in primary ovarian tumors in culture, and reduced tumorigenicity of dissociated human ovarian tumors in xenograft models (PMID: 25432176). | 25432176 |
PIK3CA mutant | breast cancer | sensitive | VS-5584 | Preclinical | Actionable | In a preclinical study, PIK3CA mutant breast cancer cells showed increased sensitivity to VS-5584 compared to PIK3CA wild-type cells in culture (PMID: 23270925). | 23270925 |
PIK3CA E542K | colon adenocarcinoma | sensitive | VS-5584 | Preclinical | Actionable | In preclinical studies, VS-5584 demonstrated efficacy in a variety of cancer cell lines, particularly those harboring PIK3CA mutations (PMID: 23270925). | 23270925 |
ERBB2 over exp | gastric adenocarcinoma | sensitive | VS-5584 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, VS-5584 inhibited tumor growth in human gastric cancer cell line xenograft models overexpressing ERBB2 (HER2) (PMID: 23270925). | 23270925 |
ERBB2 act mut PIK3CA act mut | breast cancer | sensitive | VS-5584 | Preclinical | Actionable | In a preclinical study, breast cancer cells with mutations in both ERBB2 (HER2) and PIK3CA were more sensitive to VS-5584 (PMID: 23270925). | 23270925 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT01991938 | Phase I | VS-5584 | Phase I Dose Escalation Study of VS-5584 in Subjects With Advanced Non-Hematologic Malignancies or Lymphoma | Terminated | USA | 1 |