Drug intelligence / Profile preview

pilaralisib

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

Overview

Pilaralisib is an orally available small molecule inhibitor that selectively targets class I phosphoinositide 3-kinases (PI3K), including the alpha, beta, gamma, and delta isoforms. By inhibiting PI3K activity, pilaralisib disrupts a key signaling pathway involved in tumor cell growth, survival, and resistance to chemotherapy and radiotherapy. Preclinical studies demonstrated that pilaralisib could slow tumor growth or induce tumor shrinkage in various cancer models such as breast, lung, ovarian, prostate cancers, and gliomas. It has also shown the ability to enhance the effects of other chemotherapeutic agents and EGFR inhibitors in preclinical settings. Pilaralisib was developed by Exelixis and Sanofi for use primarily as an antineoplastic agent but its clinical development has been discontinued for all indications[1][2][4][5].

Other names
pilaralisib
02

Targets

PIK3CD (Phosphatidylinositol 3-kinase delta)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CA (Phosphoinositide 3-kinase alpha)

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