Drug intelligence / Profile preview

inavolisib + olaparib

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

This entry refers to the combination of **inavolisib** and **olaparib**, currently under investigation for the treatment of breast cancer, particularly in patients with hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) metastatic or locally advanced breast cancer with PIK3CA mutations and/or BRCA mutations. **Inavolisib** is a selective inhibitor of phosphatidylinositol 3-kinase alpha (PI3Kα), disrupting downstream cell proliferation and survival signaling driven by PIK3CA mutations. **Olaparib** is a poly (ADP-ribose) polymerase (PARP) inhibitor that exploits deficiencies in DNA repair—particularly in tumors harboring BRCA1/2 mutations—leading to synthetic lethality and cancer cell death. This combination constitutes a dual targeted, small molecule approach: inhibiting tumor cell growth/proliferation (inavolisib) and impairing DNA repair (olaparib). While both agents are individually approved for indications in breast cancer, their combination is under early-phase clinical research in advanced/metastatic disease to evaluate safety and synergistic efficacy in select molecular subgroups.

Brand names
Itovebi (inavolisib)Lynparza (olaparib)
Other names
inavolisib + olaparib
02

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)PARP2 (Poly (adp-ribose) polymerase 2)

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