Buparlisib (Novartis) is a pan-phosphoinositide 3-kinase (PI3K) inhibitor that attempts to counteract the dysregulation of the PI3K/protein kinase B (AKT) pathway in cancerous tissues. Mechanisms that contribute to PI3K dysregulation include aberrant activation of upstream receptors of PI3K, amplification mutations in the phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha gene that encodes the catalytic subunit of PI3K, as well as inactivation of the phosphatase and tensin homolog tumor suppressor protein. PI3K signaling plays a fundamental role in tumorigenesis, governing cell proliferation, survival, and motility, as well as angiogenesis.
Novartis is attempting to position its phosphoinositide 3-kinase (PI3K) inhibitors buparlisib and alpelisib as the standard option for PI3K-mutated breast cancers, which represents the most common molecular mutation subtype in hormone receptor-positive (HR+)/human epidermal growth factor receptor 2-negative (HER2-) breast cancer patients. If approved, buparlisib will be indicated as a combination therapy with Faslodex (fulvestrant; AstraZeneca). The Phase III BELLE-2 trial of buparlisib plus Faslodex met its primary endpoint of increasing progression-free survival (PFS) in relapsed hormone-resistant HR+/HER2- breast cancer patients, indicating that the combination could meet some of the high unmet need in this patient population.
TABLE OF CONTENTS
4 PRODUCT PROFILES
4 buparlisib : Breast cancer: HR+/HER2- LIST OF FIGURES
17 Figure 1: Buparlisib for HR+/HER2- breast cancer – SWOT analysis
17 Figure 2: Datamonitor Healthcare’s drug assessment summary of buparlisib in HR+/HER2-
18 Figure 3: Datamonitor Healthcare’s drug assessment summary of buparlisib in HR+/HER2-
LIST OF TABLES
4 Table 1: Buparlisib drug profile
7 Table 2: Buparlisib pivotal trial data in HR+/HER2- breast cancer
12 Table 3: Buparlisib ongoing Phase III trial in HR+/HER2- breast cancer
14 Table 4: Buparlisib early-phase data in HR+/HER2- breast cancer
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