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omipalisib + trametinib
- Development stage
- Discontinued
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
This combination therapy consists of omipalisib (GSK2126458) and trametinib (GSK1120212), both originally developed by GSK. Omipalisib is a potent, orally bioavailable, dual inhibitor of phosphoinositide 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR), targeting all four class I PI3K isoforms (alpha, beta, delta, and gamma) as well as mTORC1 and mTORC2. Trametinib is a highly selective, allosteric inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2). The combination was designed to achieve vertical inhibition of the PI3K/AKT/mTOR and RAS/RAF/MEK/ERK pathways, which are frequently co-activated in various malignancies. This dual-pathway inhibition strategy aims to enhance anti-tumor efficacy and overcome potential resistance mechanisms in advanced solid tumors, including colorectal, pancreatic, and gynecological cancers.
- Brand names
- Mekinist
- Other names
- Omipalisib + Trametinib
02
Targets
DNA-PK (DNA-dependent protein kinase)PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)mTOR (Mammalian target of rapamycin kinase)PIK3CD (Phosphatidylinositol 3-kinase delta)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)
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