Drug intelligence / Profile preview

risovalisib mesylate

Development stage
Phase 2
Lead developer
Haihe
Modality
Small Molecules
Administration
Oral
01

Overview

Risovalisib mesylate (CYH33) is a novel, orally bioavailable, highly potent and selective inhibitor of the alpha subunit of class I phosphatidylinositol 3-kinase (PI3Kα), encoded by the PIK3CA gene. It demonstrates superior inhibitory activity compared to alpelisib in multiple cancer cell lines and tumor xenograft models. Risovalisib has shown encouraging anti-tumor efficacy in patients with advanced solid tumors, particularly those harboring PIK3CA hotspot mutations. Clinical development includes studies as monotherapy or in combination with other anti-tumor agents such as fulvestrant for hormone receptor-positive, HER2-negative advanced breast cancer[1][3][4][5].

Other names
risovalisib
02

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)

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