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buparlisib + buserelin + bicalutamide
- Development stage
- Unknown
- Lead developer
- Novartis
- Modality
- Peptides, Small Molecules
- Administration
- Oral, Subcutaneous
01
Overview
This investigational combination therapy is being evaluated by the Institut Paoli-Calmettes for the treatment of non-castrate metastatic prostate cancer (NCMPC). The regimen consists of three distinct pharmacological agents: buparlisib (BKM120), an oral pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor; buserelin (Suprefact), a luteinizing hormone-releasing hormone (LH-RH) agonist; and bicalutamide, a non-steroidal androgen receptor antagonist. The therapeutic rationale is based on the reciprocal feedback regulation between the androgen receptor (AR) and PI3K pathways in prostate cancer. By simultaneously inhibiting androgen production (via buserelin), blocking AR binding (via bicalutamide), and suppressing PI3K signaling (via buparlisib), the combination aims to delay or prevent the development of castration resistance in patients with hormone-sensitive metastatic disease.
- Brand names
- Casodex
- Other names
- BKM120 + suprefact + bicalutamidebuparlisib + buserelin + bicalutamideBKM120 + LH-RH agonists + bicalutamide
02
Targets
PIK3CA (Phosphoinositide 3-kinase alpha)GnRHR (Gonadotropin-releasing hormone receptor)AR (Adrenergic receptors)
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