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Association details:
| Biomarker: | BRAF mutation |
|---|---|
| Cancer: | Colorectal Cancer |
| Drug: | Mektovi (binimetinib) (MEK inhibitor) + bocodepsin (OKI-179) (HDAC inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
LB204 / 17 - The class I selective, oral HDAC inhibitor OKI-179 increases tumor regressions when combined with the MEK inhibitor binimetinib in models of NRAS melanoma
Published date:
03/09/2022
Excerpt:
Here we show synergistic activity of combining OKI-179 with the MEK inhibitor binimetinib (bini) or bini + RAF-inhibitor encorafenib (enco/bini) in both CDX and PDX models of NRAS-mutated melanoma and BRAF-mutated colorectal cancer (CRC). In vitro, combining OKI-179 with bini in SKMEL-2 NRASMT melanoma cells shows strong synergy, inducing a significant increase in cell death compared to single agents at clinically achievable drug concentrations....A similar outcome was also observed in HT29 tumors (BRAFmt CRC) where the combination of OKI-179 and enco/bini showed regression in 50% of tumors, compared to 0% for OKI-179 or enco/bini alone.
