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trametinib + everolimus
- Development stage
- Unknown
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Trametinib + everolimus is a combination of two targeted small molecule inhibitors used in oncology clinical trials, particularly for the treatment of recurrent or advanced solid tumors such as gliomas and pancreatic cancer. Trametinib is a selective inhibitor of MEK1 and MEK2, components of the MAPK/ERK pathway, thereby disrupting tumor cell proliferation and survival. Everolimus is an inhibitor of mammalian target of rapamycin (mTOR), blocking a separate signaling pathway involved in cell growth, proliferation, and survival. The rationale for combining these agents is to simultaneously inhibit two critical pathways that contribute to tumor progression and resistance mechanisms. This combination has been studied in phase I/II trials for pediatric gliomas and advanced solid tumors but has shown significant toxicity at higher doses[1][2]. Trametinib is developed by Novartis (as Mekinist), while everolimus (marketed as Afinitor) was also developed by Novartis[4][7].
- Brand names
- AfinitorZortressCerticanVotubiaMekinist
- Other names
- trametinib + everolimus
02
Targets
mTOR (Mammalian target of rapamycin kinase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)
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