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Drug intelligence / Profile preview
binimetinib + hydroxychloroquine
- Development stage
- Phase 2
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A combination therapy consisting of binimetinib, a MEK 1/2 inhibitor, and hydroxychloroquine, an autophagy inhibitor. This combination was developed based on preclinical evidence suggesting synthetic lethality in RAS-mutant tumors when MEK inhibition is combined with autophagy blockade. The scientific rationale is that KRAS mutations activate the MAPK signaling cascade, and while MEK inhibition alone often leads to resistance mechanisms including upregulation of autophagy, blocking autophagy with hydroxychloroquine may overcome this resistance.
02
Targets
MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)Neuraminidase
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