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izorlisib

Development stage: Phase 2
Lead developer: Chugai Pharmaceutical
Modality: Small Molecules
Administration: Oral

Overview

Izorlisib (CH5132799) is an orally bioavailable small molecule inhibitor of class I phosphatidylinositol 3-kinase (PI3K), developed by Chugai Pharmaceutical. It demonstrates potent inhibitory activity against PI3K isoforms, particularly PI3Kα and PI3Kγ, with nanomolar IC50 values. The drug targets the PI3K/AKT/mTOR signaling pathway, which is frequently hyperactivated in various cancers due to PIK3CA mutations or PTEN loss. In Phase I clinical studies, izorlisib was evaluated in patients with advanced solid tumors, including breast, ovarian, and endometrial cancers, showing a manageable safety profile and evidence of clinical activity in patients with PIK3CA mutations.

Other names: MEN1611MEN-1611MEN 1611

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)

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