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Drug intelligence / Profile preview
vemurafenib + cobimetinib
- Development stage
- Phase 3
- Lead developer
- Genentech
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Vemurafenib and cobimetinib is an oral combination therapy used to treat unresectable or metastatic melanoma in patients whose tumors harbor BRAF V600E or V600K mutations. Vemurafenib is a selective inhibitor of the BRAF serine-threonine kinase, while cobimetinib is a reversible inhibitor of mitogen-activated protein kinase (MAPK)/extracellular signal-regulated kinases MEK1 and MEK2. By targeting two different kinases within the RAS/RAF/MEK/ERK pathway, this combination blocks abnormal signaling that drives cancer cell proliferation and survival. The dual inhibition results in increased apoptosis and reduced tumor growth compared to either agent alone. This regimen has demonstrated improved progression-free survival for patients with advanced melanoma carrying BRAF mutations[1][3][5][6][8].
- Brand names
- Cotellic + Zelboraf
- Other names
- vemurafenib + cobimetinib
02
Targets
MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)BRAF (B-Raf proto-oncogene, serine/threonine kinase)
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