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Alpelisib

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https://www.readbyqxmd.com/read/27816049/pi3k%C3%AE-inhibition-reduces-obesity-in-mice
#1
Elena Lopez-Guadamillas, Maribel Muñoz-Martin, Sonia Martinez, Joaquin Pastor, Pablo J Fernandez-Marcos, Manuel Serrano
Partial inhibition of PI3K is one of the best-validated and evolutionary conserved manipulations to extend longevity. The best known health beneficial effects of reduced PI3K are related to metabolism and include increased energy expenditure, reduced nutrient storage, and protection from obesity. We have previously shown that a dual chemical inhibitor of the alpha and delta PI3K isoforms (CNIO-PI3Ki) reduces obesity in mice and monkeys, without evident toxic effects after long-term treatment. Here, we dissect the role of the alpha and delta PI3K isoforms by making use of selective inhibitors against PI3Kα (BYL-719 also known as alpelisib) or PI3Kδ (GS-9820 also known as acalisib)...
November 4, 2016: Aging
https://www.readbyqxmd.com/read/27220786/-current-progress-and-feasibility-of-using-molecular-targeted-agent-combinations-for-metastatic-colorectal-cancer
#2
Toshiki Masuishi, Kei Muro
The efficacy of molecular-targeted agent combinations for the treatment of metastatic colorectal cancer has become increasingly evident over recent years, although none of these combinations have been recognized yet as a standard therapy. The intention here is to provide a synopsis of current progress in this developing area by reviewing existing publications and ongoing clinical trials. While bevacizumab plus anti-EGFR agents exhibit detrimental effects in first-line setting , a combination of bevacizumab with erlotinib has been suggested as an effective maintenance therapy...
April 2016: Gan to Kagaku Ryoho. Cancer & Chemotherapy
https://www.readbyqxmd.com/read/27126994/a-phase-ib-study-of-alpelisib-byl719-a-pi3k%C3%AE-specific-inhibitor-with-letrozole-in-er-her2-metastatic-breast-cancer
#3
Ingrid A Mayer, Vandana G Abramson, Luigi Formisano, Justin M Balko, Mónica V Estrada, Melinda E Sanders, Dejan Juric, David Solit, Michael F Berger, Helen H Won, Yisheng Li, Lewis C Cantley, Eric Winer, Carlos L Arteaga
PURPOSE: Alpelisib, a selective oral inhibitor of the class I PI3K catalytic subunit p110α, has shown synergistic antitumor activity with endocrine therapy against ER(+)/PIK3CA-mutated breast cancer cells. This phase Ib study evaluated alpelisib plus letrozole's safety, tolerability, and preliminary activity in patients with metastatic ER(+) breast cancer refractory to endocrine therapy. PATIENTS AND METHODS: Twenty-six patients received letrozole and alpelisib daily...
April 28, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/26830312/treatment-strategies-for-advanced-hormone-receptor-positive-and-human-epidermal-growth-factor-2-negative-breast-cancer-the-role-of-treatment-order
#4
Edith A Perez
Although survival rates among patients with breast cancer have improved in recent years, those diagnosed with advanced disease with distant metastasis face a 5-year survival rate of less than 25%, making the management of these patients an area still in significant need of continued research. Selecting the optimal treatment order from among the variety of currently available therapy options presents a relevant challenge for medical oncologists. With the understanding that the majority of patients with breast cancer and those who succumb to this disease have HR-positive disease, this review will focus on treatment options and treatment order in patients with HR-positive advanced breast cancer...
January 2016: Drug Resistance Updates: Reviews and Commentaries in Antimicrobial and Anticancer Chemotherapy
https://www.readbyqxmd.com/read/26793003/pi3k-inhibitors-as-new-cancer-therapeutics-implications-for-clinical-trial-design
#5
REVIEW
Cristian Massacesi, Emmanuelle Di Tomaso, Patrick Urban, Caroline Germa, Cornelia Quadt, Lucia Trandafir, Paola Aimone, Nathalie Fretault, Bharani Dharan, Ranjana Tavorath, Samit Hirawat
The PI3K-AKT-mTOR pathway is frequently activated in cancer. PI3K inhibitors, including the pan-PI3K inhibitor buparlisib (BKM120) and the PI3Kα-selective inhibitor alpelisib (BYL719), currently in clinical development by Novartis Oncology, may therefore be effective as anticancer agents. Early clinical studies with PI3K inhibitors have demonstrated preliminary antitumor activity and acceptable safety profiles. However, a number of unanswered questions regarding PI3K inhibition in cancer remain, including: what is the best approach for different tumor types, and which biomarkers will accurately identify the patient populations most likely to benefit from specific PI3K inhibitors? This review summarizes the strategies being employed by Novartis Oncology to help maximize the benefits of clinical studies with buparlisib and alpelisib, including stratification according to PI3K pathway activation status, selective enrollment/target enrichment (where patients with PI3K pathway-activated tumors are specifically recruited), nonselective enrollment with mandatory tissue collection, and enrollment of patients who have progressed on previous targeted agents, such as mTOR inhibitors or endocrine therapy...
2016: OncoTargets and Therapy
https://www.readbyqxmd.com/read/26254025/absorption-distribution-metabolism-and-excretion-of-14-c-byl719-alpelisib-in-healthy-male-volunteers
#6
Alexander James, Lars Blumenstein, Ulrike Glaenzel, Yi Jin, Arnold Demailly, Annamaria Jakab, Regine Hansen, Katharine Hazell, Anuradha Mehta, Lucia Trandafir, Piet Swart
PURPOSE: To determine the pharmacokinetics of the p110α-selective inhibitor alpelisib (BYL719) in humans, to identify metabolites in plasma and excreta, and to characterize pathways of biotransformation. METHODS: Four healthy male volunteers received a single oral dose of [(14)C]-labeled alpelisib (400 mg, 2.78 MBq). Blood, urine, and feces samples were collected throughout the study. Total radioactivity was measured by liquid scintillation counting, and metabolites were quantified and identified by radiometry and mass spectrometry...
October 2015: Cancer Chemotherapy and Pharmacology
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