ipatasertib

12/01/2022 - "A statistically significant correlation between ipatasertib AUCSS and improved survival was found in patients with PTEN-loss tumors (hazard ratio [HR]: 0.92 per 1000 ng h/mL AUCSS, 95% confidence interval [CI] 0.87-0.98, p = 0.011). "
11/04/2019 - "GDC-0068 is a pan-Akt inhibitor that has shown to be effective in various preclinical tumor models as well as in clinical trials. "
12/01/2021 - "Population pharmacokinetic models of ipatasertib and M1 were developed separately using data from 342 individuals with cancer from 5 phase 1 and 2 studies. "
01/01/2019 - "The current study assessed the safety, tolerability, and pharmacokinetics of ipatasertib in Japanese patients with solid tumors. "
01/01/2019 - "SIGNIFICANCE: This study describes the patient-driven discovery of the first AKT1 fusion-driven cancer and its treatment with the AKT inhibitor ipatasertib. "

01/01/2019 - "Exposure-Response-Based Product Profile-Driven Clinical Utility Index for Ipatasertib Dose Selection in Prostate Cancer."
12/01/2022 - "Characterization of exposure-response relationships of ipatasertib in patients with metastatic castration-resistant prostate cancer in the IPATential150 study."
01/01/2019 - "The aims of this work were to characterize ipatasertib exposure-response (E-R) relationships in a phase II study and to quantitatively assess benefit-risk using a clinical utility index approach to support ipatasertib phase III dose selection in patients with metastatic castration-resistant prostate cancer. "
10/01/2022 - "Ipatasertib is a selective, small molecule Akt inhibitor that is currently being developed for the treatment of metastatic castration-resistant prostate cancer. "
01/01/2019 - "Ipatasertib 400 mg daily, showing the highest probability of achieving the minimal product profiles and better benefit-risk balance than other doses (200-500 mg daily), was selected for further development in metastatic castration-resistant prostate cancer."

10/01/2017 - "Ipatasertib warrants further investigation for the treatment of triple-negative breast cancer. "
10/01/2017 - "The oral AKT inhibitor ipatasertib is being investigated in cancers with a high prevalence of PI3K/AKT pathway activation, including triple-negative breast cancer. "
09/01/2021 - "Final results of the double-blind placebo-controlled randomized phase 2 LOTUS trial of first-line ipatasertib plus paclitaxel for inoperable locally advanced/metastatic triple-negative breast cancer."
01/01/2021 - "Additionally, phase III trials of capivasertib and ipatasertib are already under way in HR+ and triple-negative breast cancer. "
01/01/2019 - "This hypothesis-generating trial evaluated neoadjuvant ipatasertib-paclitaxel for early triple-negative breast cancer (TNBC). "

11/04/2019 - "In in vitro studies, antitumor activity of GDC-0068 was assessed in breast cancer cells of phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha (PIK3CA)-mutant and PIK3CA-wildtype breast cancer cell lines using cell viability and apoptosis assays, cell cycle analysis, and western blots. "
01/01/2021 - "Durable Clinical Activity to the AKT Inhibitor Ipatasertib in a Heavily Pretreated Patient With an AKT1 E17K Mutant Metastatic Breast Cancer."
11/04/2019 - "The purpose of this study was to analyze the efficacy of GDC-0068 in a breast cancer brain metastases model. "
11/04/2019 - "In vivo, the efficacy of GDC-0068 was analyzed in a PIK3CA-mutant breast cancer brain metastasis orthotopic xenograft mouse model and evaluated by repeated bioluminescent imaging and immunohistochemistry. "
11/04/2019 - "This study suggests that the Akt inhibitor GDC-0068 may be an encouraging targeted treatment strategy for breast cancer brain metastasis patients with activating mutations in the PI3K pathway. "

11/04/2019 - "In vivo, the efficacy of GDC-0068 was analyzed in a PIK3CA-mutant breast cancer brain metastasis orthotopic xenograft mouse model and evaluated by repeated bioluminescent imaging and immunohistochemistry. "
11/04/2019 - "This study suggests that the Akt inhibitor GDC-0068 may be an encouraging targeted treatment strategy for breast cancer brain metastasis patients with activating mutations in the PI3K pathway. "
01/01/2020 - "The Akt inhibitors ipatasertib, capivasertib, uprosertib, and MK-2206 not only suppress cancer cell proliferation and metastasis, but may also inhibit cytokine regulation and PD-L1 expression. "