Taselisib is a p110-alpha isoform-specific PI3K inhibitor. PI3K signaling plays a fundamental role in
tumorigenesis, governing cell proliferation, survival, and motility, as well as angiogenesis. 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
(PIK3CA) gene that encodes the catalytic subunit of PI3K, as well as inactivation of the phosphatase
and tensin homolog (PTEN) tumor suppressor protein (Massacesi et al., 2013; Wymann et al., 2003).
Taselisib (Roche/Chugai) is a phosphoinositide 3-kinase (PI3K) inhibitor predicted to be the second
such drug to reach the market behind Novartis’s late-phase candidate buparlisib. Despite early signs
of efficacy as a combination treatment with letrozole, taselisib’s commercial attractiveness will be
limited by the potentially high cost of treatment and its small patient population, which is limited to
hormone receptor-positive (HR+)/human epidermal growth factor receptor 2-negative (HER2-) breast
cancers with PI3K mutations.
TABLE OF CONTENTS
4 PRODUCT PROFILES
4 taselisib : Breast cancer: HR+/HER2-
LIST OF FIGURES
8 Figure 1: Taselisib for HR+/HER2- breast cancer – SWOT analysis
8 Figure 2: Datamonitor Healthcare’s drug assessment summary of taselisib in HR+/HER2-
9 Figure 3: Datamonitor Healthcare’s drug assessment summary of taselisib in HR+/HER2-
LIST OF TABLES
4 Table 1: Taselisib drug profile
5 Table 2: Taselisib Phase III trial in HR+/HER2- breast cancer
7 Table 3: Taselisib early-phase data in HR+/HER2- breast cancer
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