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Drug intelligence / Profile preview
decitabine + vemurafenib + cobimetinib
- Development stage
- Discontinued
- Lead developer
- Genentech
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
This investigational combination therapy consists of three active ingredients: decitabine, vemurafenib, and cobimetinib. It is being evaluated in a Phase 1/2 clinical trial (NCT01876641) led by Dr. Mohammed M. Milhem at the University of Iowa for the treatment of BRAF-mutated metastatic melanoma. The regimen combines standard-of-care MAPK pathway inhibition—using the BRAF inhibitor vemurafenib and the MEK inhibitor cobimetinib—with low-dose decitabine, a DNA methyltransferase inhibitor. The rationale for this triple combination is that epigenetic modulation via decitabine may reverse or prevent resistance to BRAF/MEK inhibitors, potentially improving response rates and durability in patients with resistant or advanced disease.
- Other names
- Decitabine with Vemurafenib and CobimetinibVemurafenib + Cobimetinib + Decitabine
02
Targets
BRAF V600EDNMT1 (DNA (cytosine-5)-methyltransferase 1)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)
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