Drug intelligence / Profile preview

trametinib + palbociclib

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

**Trametinib + palbociclib** is a combination drug regimen consisting of trametinib, a selective inhibitor of MEK1 and MEK2 in the RAF/MEK/ERK pathway, and palbociclib, a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). This combination has been investigated for synergistic anti-tumor effects in cancer therapies, particularly to overcome resistance mechanisms such as protective autophagy induced by palbociclib. Trametinib mitigates autophagy and enhances the anti-cancer efficacy of palbociclib. Clinical trials have evaluated this regimen in breast cancer and melanoma, and preclinical models in pancreatic cancer. Trametinib is developed and manufactured by GSK, and palbociclib is developed and manufactured by Pfizer[1][2][3][4][5][7][8][9].

Brand names
IbranceMekinist
Other names
trametinib plus palbociclibtrametinib and palbociclib
02

Targets

MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)

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