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apitolisib + abiraterone
- Development stage
- Discontinued
- Lead developer
- Genentech
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Apitolisib + abiraterone is an investigational combination therapy used primarily in clinical trials for metastatic castration-resistant prostate cancer (mCRPC), usually in conjunction with prednisone. Apitolisib (GDC-0980) is a highly selective dual inhibitor of phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR), which blocks both PI3K-alpha and mTOR pathways, impeding cell growth and survival signaling. Abiraterone (CB7630, Zytiga) is a potent and irreversible inhibitor of CYP17A1, blocking androgen biosynthesis and thereby suppressing androgen receptor (AR) signaling that drives prostate cancer progression. The combination is designed to disrupt compensatory signaling between the androgen receptor pathway and the PI3K/mTOR pathway, aiming to overcome resistance mechanisms in advanced prostate cancer.
- Other names
- apitolisib + abirateroneapitolisibGDC-0980GDC0980GDC 0980abirateroneCB7630CB-7630CB 7630
02
Targets
mTOR (Mammalian target of rapamycin kinase)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)
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