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Drug intelligence / Profile preview
IDE196 + binimetinib
- Development stage
- Phase 2
- Lead developer
- IDEAYA Biosciences
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A combination of **darovasertib (IDE196)**, a selective small molecule **protein kinase C (PKC) inhibitor**, and **binimetinib (Mektovi)**, a **MEK inhibitor**, developed for the treatment of solid tumors harboring GNAQ or GNA11 mutations or PRKC fusions, including metastatic uveal melanoma (MUM), cutaneous melanoma, colorectal cancer, and other solid tumors. Darovasertib inhibits the PKC pathway, a key oncogenic pathway in these cancers, while binimetinib inhibits the MEK component of the MAPK pathway, providing preclinically suggested synergistic antitumor activity. This combination is being evaluated in a multi-arm Phase 1/2 clinical trial for safety, tolerability, pharmacokinetics, and anti-tumor efficacy[1][3][4].
- Other names
- darovasertib + binimetinibIDE196 + MEK162
02
Targets
MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)PKC (Protein kinase C family)
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