Drug intelligence / Profile preview

buparlisib + E7046 + atezolizumab

Development stage
Unknown
Lead developer
Adlai Nortye
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

This is an experimental combination therapy consisting of **buparlisib**, **E7046**, and **atezolizumab** for the treatment of advanced solid tumors or cancers. - **Buparlisib** is a pan-class I PI3K inhibitor that acts by inhibiting the phosphatidylinositol-3-kinase (PI3K) pathway, which is frequently dysregulated in cancers and is important for cellular proliferation and survival[1][4]. - **E7046** is a small molecule antagonist of the prostaglandin E2 (PGE2) receptor EP4, targeting myeloid-derived suppressor cell-mediated immunosuppression in the tumor microenvironment[3]. - **Atezolizumab** is a monoclonal antibody and immune checkpoint inhibitor targeting programmed death-ligand 1 (PD-L1), enhancing antitumor immune responses by blocking PD-L1-mediated immune evasion by tumor cells[5][6]. Research on this triple combination, including buparlisib and E7046 with atezolizumab, is ongoing for solid tumors. Preliminary rationale for such combinations includes potential synergy: targeting the PI3K pathway may overcome resistance to immune checkpoint inhibitors like atezolizumab, and blocking the EP4 receptor may further modulate the immunosuppressive tumor microenvironment[3][1].

Other names
buparlisib + E7046 + atezolizumab
02

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)CD274 (Programmed cell death protein 1 ligand 1)PTGER4 (Prostaglandin E2 receptor EP4 subtype)

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