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PI3K alpha Inhibitor MLN1117

Known as: TAK 117, MLN-1117, MLN1117 
An orally bioavailable inhibitor of the class I phosphoinositide 3-kinase (PI3K) alpha isoform with potential antineoplastic activity. PI3K alpha… 
National Institutes of Health

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Papers overview

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2019
2019
Dose Optimization for Anticancer Drug Combinations: Maximizing Therapeutic Index via Clinical Exposure-Toxicity/Preclinical Exposure-Efficacy Modeling
Purpose: Recommended phase II dose (RP2D) determination for combination therapy regimens is a constrained optimization problem of… 
2019
2019
Novel Oral mTORC1/2 Inhibitor TAK-228 Has Synergistic Antitumor Effects When Combined with Paclitaxel or PI3Kα Inhibitor TAK-117 in Preclinical Bladder Cancer Models
Advanced bladder cancer is associated with a poor prognosis and limited treatment options. The PI3K/AKT/mTOR pathway is… 
2018
2018
Characterizing the Sources of Pharmacokinetic Variability for TAK‐117 (Serabelisib), an Investigational Phosphoinositide 3‐Kinase Alpha Inhibitor: A Clinical Biopharmaceutics Study to Inform…
TAK‐117 (also known as MLN1117 or serabelisib) is an orally available inhibitor of phosphoinositide 3‐kinase alpha being… 
Highly Cited
2017
Highly Cited
2017
A First-in-Human, Phase I, Dose-Escalation Study of TAK-117, a Selective PI3Kα Isoform Inhibitor, in Patients with Advanced Solid Malignancies
Purpose: To evaluate the safety, MTD, pharmacokinetics, pharmacodynamics, and preliminary antitumor activity of TAK-117 (MLN1117… 
2017
2017
Co-targeting aurora kinase with PD-L1 and PI3K abrogates immune checkpoint mediated proliferation in peripheral T-cell lymphoma: a novel therapeutic strategy
Peripheral T-cell non-Hodgkin lymphoma (PTCL) are heterogeneous, rare, and aggressive diseases mostly incurable with current cell… 
2016
2016
A phase 1b multicenter, open-label study of investigational TAK-228 (MLN0128) plus TAK-117 (MLN1117) in adult patients with advanced nonhematologic malignancies
Review
2015
Review
2015
PI3K inhibitors in inflammation, autoimmunity and cancer
2015
2015
First-in-human, phase I, dose-escalation study of selective PI3K{alpha} isoform inhibitor MLN1117 in patients (pts) with advanced solid malignancies.
2501 Background: PI3K signaling is aberrantly activated in many solid tumors; isoform-selective targeting may enable robust… 
2014
2014
Effects of Novel Isoform-Selective Phosphoinositide 3-Kinase Inhibitors on Natural Killer Cell Function
Phosphoinositide 3-kinases (PI3Ks) are promising targets for therapeutic development in cancer. The class I PI3K isoform p110… 
Highly Cited
2012
Highly Cited
2012
Selective Inhibition of Phosphoinositide 3-Kinase p110α Preserves Lymphocyte Function*
Background: The class IA PI3K isoform p110α is a promising drug target in cancer therapy yet its role in lymphocytes is not known… 
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