2- (3- (2- (1- isopropyl- 3- methyl- 1H- 1,2- 4- triazol- 5- yl)- 5,6- dihydrobenzo(f)imidazo(1,2- d)(1,4)oxazepin- 9- yl)- 1H- pyrazol- 1- yl)- 2- methylpropanamide

01/01/2020 - "In summary, these data suggest that development of taselisib in breast cancer should occur in a PIK3CA-mutant setting with cotreatments determined by the specific subtypes under investigation."
01/01/2020 - "We further assessed how taselisib modulates downstream signaling in the different genomic backgrounds that occur within breast cancer. "
05/01/2018 - "These preliminary data suggest that taselisib may be effective in patients with PIK3CA-mutated solid tumors or HR-positive advanced breast cancer."
01/01/2020 - "The trial investigated the safety and efficacy of the AR-antagonist enzalutamide alone or in combination with the PI3K inhibitor taselisib in patients with metastatic AR+ (≥10%) breast cancer. "
01/01/2019 - "Neoadjuvant letrozole plus taselisib versus letrozole plus placebo in postmenopausal women with oestrogen receptor-positive, HER2-negative, early-stage breast cancer (LORELEI): a multicentre, randomised, double-blind, placebo-controlled, phase 2 trial."

11/01/2018 - "Correction: Phase I Dose-Escalation Study of Taselisib, an Oral PI3KInhibitor, in Patients with Advanced Solid Tumors."
01/01/2017 - "Phase I Dose-Escalation Study of Taselisib, an Oral PI3K Inhibitor, in Patients with Advanced Solid Tumors."
06/13/2013 - "One of these compounds, GDC-0032 (11l), was progressed to clinical trials and is currently under phase I evaluation as a potential treatment for human malignancies."
01/01/2022 - "Whether PIK3CA mutations predict sensitivity to taselisib in other cancer types is unknown. "
01/01/2021 - "Taselisib had limited activity in the tumor types tested and is no longer in development. "

12/01/2021 - "Safety and efficacy of low-dose PI3K inhibitor taselisib in adult patients with CLOVES and Klippel-Trenaunay syndrome (KTS): the TOTEM trial, a phase 1/2 multicenter, open-label, single-arm study."

04/15/2016 - "Hence, we investigated the therapeutic efficacy of inhibiting PI3K with GDC-0032, a PI3K inhibitor with potent activity against p110α, in combination with radiation in HNSCC. "
04/15/2016 - "GDC-0032 has increased potency in HNSCC cell lines harboringPIK3CA-activating aberrations. "
04/15/2016 - "Pretreatment with GDC-0032 radiosensitizedPIK3CA-mutant HNSCC cells, enhanced radiation-induced apoptosis, impaired DNA damage repair, and prolonged G2-M arrest following irradiation. "
04/15/2016 - "GDC-0032 inhibited potently PI3K signaling and displayed greater antiproliferative activity in HNSCC cell lines withPIK3CAmutations or amplification, whereas cell lines withPTENalterations were relatively resistant to its effects. "
04/15/2016 - "The efficacy of GDC-0032 was assessedin vitroin 26 HNSCC cell lines with crystal violet proliferation assays, and changes in PI3K signaling were measured by Western blot analysis. "

11/01/2014 - "To evaluate the efficacy of taselisib, a selective inhibitor of PIK3CA, against primary uterine serous carcinomas (USC) harboring PIK3CA mutations and HER2/neu gene amplification. "
11/01/2014 - "Taselisib, a selective inhibitor of PIK3CA, is highly effective on PIK3CA-mutated and HER2/neu amplified uterine serous carcinoma in vitro and in vivo."