eganelisib

Eganelisib is an orally bioavailable, highly selective small molecule inhibitor of the gamma isoform of phosphoinositide 3-kinase (PI3K-gamma), developed as a first-in-class immunomodulating and antineoplastic agent. By selectively inhibiting PI3K-gamma (encoded by PIK3CG), eganelisib disrupts the PI3K/AKT/mTOR signaling pathway, which is critical for tumor cell proliferation and survival. This mechanism also modulates anti-tumor immune responses by reprogramming tumor-associated macrophages and reducing tumor-mediated immunosuppression. Eganelisib has demonstrated activity both as monotherapy and in combination with immune checkpoint inhibitors such as PD-1/PD-L1 antibodies in preclinical models and early clinical trials. It is being investigated primarily for cancer indications including triple-negative breast cancer (TNBC) and urothelial carcinoma, with additional exploration in acute myeloid leukemia (AML) and potential applications in inflammatory conditions like COVID-19 due to its effects on myeloid cell trafficking[1][2][3][4][5][6][7].

Other names

eganelisib [USAN]