Drug intelligence / Profile preview

alpelisib + trametinib

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

Overview

This combination therapy consists of alpelisib, a PI3K-alpha inhibitor, and trametinib, a MEK inhibitor. It is currently being investigated in a Phase 1 clinical trial (NCT03631953) sponsored by Assistance Publique Hopitaux De Marseille for the treatment of aggressive, refractory Grade II-III meningiomas that have failed standard surgery and radiotherapy. The rationale for the combination is to simultaneously inhibit the PI3K-AKT-mTOR and MAP kinase pathways, which are frequently co-activated in aggressive meningiomas, to induce apoptosis and overcome therapeutic resistance. Both components were originally developed by Novartis; trametinib is marketed as Mekinist for melanoma and other indications, while alpelisib is marketed as Piqray for breast cancer.

Other names
Alpelisib and Trametinib combinationTrametinib + Alpelisib
02

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)

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