Itovebi (inavolisib)

P1/2, N=1132, Recruiting, Hoffmann-La Roche | N=792 --> 1132

A 62-year-old man with metastatic PSA underwent splenectomy followed by first-line paclitaxel, achieving stable disease for 7 months...Sequential treatment with liposomal doxorubicin, eribulin, toripalimab, and lenvatinib failed to control the disease failed to control the disease...To our knowledge, this is the first reported use of inavolisib in angiosarcoma. The rapid biochemical and radiological response observed in this PIK3CA-mutated PSA supports early genomic profiling to identify actionable alterations and warrants prospective evaluation of combined phosphoinositide 3-kinase and vascular endothelial growth factor pathway inhibition in refractory angiosarcoma.

In BCs with alterations in the AKT/PIK3CA pathway, capivasertib, alpelisib, and inavolisib have recently improved progression-free survival (PFS). Inavolisib (GC0077) differs from the other drugs targeting this pathway by its high potency and tolerability when combined with endocrine therapy, mostly with fulvestrant, and a CDK4/6 inhibitor. Its recent use in the first-line combined treatment for advanced HR+/HER2-negative BC has shown a PFS benefit compared to placebo in the INAVO120 trial, suggesting its role as a valid treatment option in PIK3CA-mutated patients. Further studies are warranted to confirm these results in terms of prolonging efficacy and maintaining durable responses - with a manageable safety profile - in clinical practice.

P2, N=160, Not yet recruiting, Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University

P1, N=30, Active, not recruiting, Hoffmann-La Roche | Trial completion date: Sep 2028 --> Jul 2027 | Trial primary completion date: Sep 2028 --> Jul 2027

This analysis demonstrates the generally consistent, manageable and tolerable safety profile of inavolisib plus palbociclib-fulvestrant. Key selected adverse events were generally reversible and were controlled by concomitant medications and dose modifications.

Normal baseline glycemic indices do not reliably exclude the risk of severe toxicity. Early metabolic assessment, close glucose monitoring, prompt interruption of inavolisib when clinically indicated, and rapid insulin-based management are essential for timely recognition and safe clinical care.

P1, N=30, Active, not recruiting, Hoffmann-La Roche | Recruiting --> Active, not recruiting

P3, N=420, Active, not recruiting, Hoffmann-La Roche | Trial primary completion date: Apr 2026 --> Nov 2026

P2, N=100, Recruiting, Hoffmann-La Roche

P1/2, N=792, Recruiting, Hoffmann-La Roche | N=56 --> 792

PI3Kα inhibitors, particularly alpelisib and inavolisib, combined with endocrine therapy improved progression-free survival in PIK3CA-mutated HR+/HER2- advanced breast cancer, while alpelisib was the only agent to demonstrate an overall survival benefit. PI3Kα inhibitors show promising efficacy in PIK3CA-mutated HR+/HER2- breast cancer, but publication bias, resistance, target-specific toxicity, and geographic disparities remain major barriers. Mandatory trial reporting, biomarker-guided treatment, and international collaboration should be prioritized.