Drug intelligence / Profile preview

buparlisib + E7046

Development stage
Preclinical
Lead developer
Adlai Nortye
Modality
Small Molecules
Administration
Oral
01

Overview

**Buparlisib + E7046** is an experimental combination therapy consisting of two small molecule inhibitors: - **Buparlisib (BKM120)** is a pan-class I phosphoinositide 3-kinase (PI3K) inhibitor, designed to block PI3K signaling, which is often upregulated in cancer cells. Buparlisib’s mechanism leads to reduced survival and growth of malignant cells[1][9][13][15]. - **E7046** is a highly selective antagonist of the E-type prostanoid receptor 4 (EP4), the receptor for prostaglandin E2 (PGE2). EP4 signaling is implicated in immunosuppression within the tumor microenvironment, with E7046 acting to counteract these immunosuppressive signals and promote antitumor immunity[4]. This combination is intended for use in oncology, especially in tumors associated with high PI3K pathway activation and immune-suppressive microenvironments. Both drugs are orally administered small molecules. The developer for buparlisib is Novartis, and for E7046 is Eisai[9][4]. There is no evidence of a unique brand name or formal approval; the combination is likely in early clinical or preclinical evaluation as of the current date.

02

Targets

PTGER4 (Prostaglandin E2 receptor EP4 subtype)PIK3CA (Phosphoinositide 3-kinase alpha)

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