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Drug intelligence / Profile preview
darovasertib + crizotinib
- Development stage
- Phase 3
- Lead developer
- IDEAYA Biosciences
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
**Darovasertib + crizotinib** is an oral combination therapy under active clinical development for the treatment of metastatic uveal melanoma (MUM) and certain solid tumors with activating GNAQ/GNA11 mutations or PKC fusions. Darovasertib is a small molecule inhibitor of protein kinase C (PKC) isoforms (conventional α, β and novel δ, ε, η, θ), while crizotinib is a small molecule inhibitor primarily targeting the c-Met receptor tyrosine kinase (also known as hepatocyte growth factor receptor, HGFR). This combination targets parallel signaling pathways (PKC/MAPK and PI3K/AKT) implicated in the growth and survival of uveal melanoma, aiming to overcome resistance associated with monotherapy. The regimen has demonstrated a high rate of tumor response and manageable safety in Phase 2 clinical trials in first-line and pretreated MUM. Darovasertib is developed by IDEAYA Biosciences, and crizotinib is marketed by Pfizer.
- Brand names
- Xalkori (crizotinib component)
- Other names
- darovasertib and crizotinib
02
Targets
ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)AXL (AXL receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)MST1R (Recepteur d'origine nantais)MUSK (Muscle skeletal receptor tyrosine-protein kinase MuSK)PRKCA (Protein kinase C alpha)PRKCB (Protein kinase C beta)PRKCD (Protein kinase C delta)PRKCE (Protein Kinase C epsilon)PRKCH (Protein kinase C eta)PRKCQ (Protein kinase C theta)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)
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