Buparlisib
Chemical compound
From Wikipedia, the free encyclopedia
Buparlisib (codenamed AN2025 and BKM120) is an experimental anti-cancer medication. It is a small molecule orally-available pan-class I phosphoinositide 3-kinase (PI3K) inhibitor.[1] Buparlisib was under investigation as a treatment for advanced breast cancer but was abandoned due to negative results. It is still under investigation as a potential treatment for head and neck squamous cell carcinoma (HNSCC).
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| Other names | AN2025, BKM120 |
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| ECHA InfoCard | 100.232.248 |
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| Formula | C18H21F3N6O2 |
| Molar mass | 410.401 g·mol−1 |
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Clinical trials
Buparlisib was under investigation as a treatment for advanced or metastatic HER2-negative breast cancer in several phase III clinical trials:
- The phase III trial BELLE-2 compared buparlisib + fulvestrant with fulvestrant alone in patients with advanced or metastatic HER2-negative, hormone receptor-positive (HR+) aromatase inhibitor-resistant breast cancer. Treatment with buparlisib prolonged progression-free survival (PFS) significantly but also resulted in excessive side effects.[2][3]
- Similar to BELLE-2, the phase III trial BELLE-3 compared buparlisib + fulvestrant with fulvestrant alone in patients with advanced or metastatic HER2-negative breast cancer, however in this trial, the disease had to be resistant to a mammalian target of rapamycin (mTOR) inhibitor. The trial was terminated due to excessive side effects.[4][5]
- The phase II/III trial BELLE-4 compared buparlisib + paclitaxel with paclitaxel alone in patients with advanced or metastatic HER2-negative breast cancer regardless of hormone receptor status. Addition of buparlisib to paclitaxel did not improve PFS, and the trial was stopped for futility at the end of phase II.[6][7]
These results led the trials' sponsor, Novartis, to cancel their breast cancer study program with buparlisib.
Buparlisib is still under investigation as a potential treatment for head and neck squamous cell carcinoma (HNSCC) in the ongoing phase III trial BURAN, which compares buparlisib + paclitaxel to paclitaxel alone in patients with recurrent or metastatic HNSCC. Results are expected for December 2022.[8]