PI3Kδ inhibitors for the treatment of cancer: a patent review (2015-present)

Development of new agents for peripheral T-cell lymphoma

(2019) Yuta Ito et al.   EXPERT OPINION ON BIOLOGICAL THERAPY

Tolerability and activity of ublituximab, umbralisib, and ibrutinib in patients with chronic lymphocytic leukaemia and non-Hodgkin lymphoma: a phase 1 dose escalation and expansion trial

(2019) Loretta J Nastoupil et al.   Lancet Haematology

Parsaclisib, a potent and highly selective PI3Kδ inhibitor, in patients with relapsed or refractory B-cell malignancies

(2019) Andres Forero-Torres et al.   BLOOD

Synthesis and Biological Evaluation of 4-(Piperid-3-yl)amino Substituted 6-Pyridylquinazolines as Potent PI3Kδ Inhibitors

(2019) Yifan Feng et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors

(2019) Yuan-Yuan Hei et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Exploring a Future for PI3K Inhibitors in Chronic Lymphocytic Leukemia

(2019) Krish Patel et al.   Current Hematologic Malignancy Reports

T and B‐cell signaling in activated PI3K delta syndrome: From immunodeficiency to autoimmunity

(2019) Silvia Preite et al.   IMMUNOLOGICAL REVIEWS

Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors

(2018) Minhang Xin et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Phase 1 study of the PI3Kδ inhibitor INCB040093 ± JAK1 inhibitor itacitinib in relapsed/refractory B-cell lymphoma

(2018) Tycel J. Phillips et al.   BLOOD

Introduction of pyrrolidineoxy or piperidineamino group at the 4-position of quinazoline leading to novel quinazoline-based phosphoinositide 3-kinase delta (PI3Kδ) inhibitors

(2018) Minhang Xin et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Selectively Targeting the Kinome-Conserved Lysine of PI3Kδ as a General Approach to Covalent Kinase Inhibition

(2018) Samuel E. Dalton et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Umbralisib, a novel PI3Kδ and casein kinase-1ε inhibitor, in relapsed or refractory chronic lymphocytic leukaemia and lymphoma: an open-label, phase 1, dose-escalation, first-in-human study

(2018) Howard A Burris et al.   LANCET ONCOLOGY

19F-NMR based determination of the absorption, metabolism and excretion of the oral phosphatidylinositol-3-kinase (PI3K) delta inhibitor leniolisib (CDZ173) in healthy volunteers

(2018) David Pearson et al.   XENOBIOTICA

Targeting Cancer Cells and Tumor Microenvironment in Preclinical and Clinical Models of Hodgkin Lymphoma Using the Dual PI3Kδ/γ Inhibitor RP6530

(2018) Silvia L. Locatelli et al.   CLINICAL CANCER RESEARCH

Safety, Pharmacokinetics, and Pharmacodynamics of ME-401, an Oral, Potent, and Selective Inhibitor of Phosphatidylinositol 3-Kinase P110δ, Following Single Ascending Dose Administration to Healthy Volunteers

(2018) Ofir Moreno et al.   CLINICAL THERAPEUTICS

Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective

(2018) Aimie E. Garces et al.   JOURNAL OF MEDICINAL CHEMISTRY

Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases

(2018) Matthew W. D. Perry et al.   JOURNAL OF MEDICINAL CHEMISTRY

Duvelisib: a phosphoinositide-3 kinase δ/γ inhibitor for chronic lymphocytic leukemia

(2017) Hima V. Vangapandu et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Seletalisib: Characterization of a Novel, Potent, and Selective Inhibitor of PI3K δ

(2017) Rodger A. Allen et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

INCB040093 Is a Novel PI3KδInhibitor for the Treatment of B Cell Lymphoid Malignancies

(2017) Niu Shin et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties

(2016) Klemens Hoegenauer et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of Orally Efficacious Phosphoinositide 3-Kinase δ Inhibitors with Improved Metabolic Stability

(2016) Leena Patel et al.   JOURNAL OF MEDICINAL CHEMISTRY

Idelalisib

(2015) Arpita Shah et al.   ANNALS OF PHARMACOTHERAPY

PI3K signalling in inflammation

(2015) P.T. Hawkins et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Synthesis and SAR study of potent and selective PI3Kδ inhibitors

(2015) Minna Bui et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Idelalisib: First-in-Class PI3K Delta Inhibitor for the Treatment of Chronic Lymphocytic Leukemia, Small Lymphocytic Leukemia, and Follicular Lymphoma

(2015) Q. Yang et al.   CLINICAL CANCER RESEARCH

Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease

(2015) Kenneth Down et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting PI3Kδ: Emerging Therapy for Chronic Lymphocytic Leukemia and Beyond

(2015) Manman Wei et al.   MEDICINAL RESEARCH REVIEWS

Discovery and in Vivo Evaluation of (S)-N-(1-(7-Fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and Related PI3Kδ Inhibitors for Inflammation and Autoimmune Disease

(2014) Timothy D. Cushing et al.   JOURNAL OF MEDICINAL CHEMISTRY

Effects of Isoform-selective Phosphatidylinositol 3-Kinase Inhibitors on Osteoclasts

(2013) Ryan P. P. Shugg et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Selective PI3Kδ inhibitors, a review of the patent literature

(2011) Peter Norman   EXPERT OPINION ON THERAPEUTIC PATENTS

Class I PI3K in oncogenic cellular transformation

(2008) L Zhao et al.   ONCOGENE

PI3K pathway alterations in cancer: variations on a theme

(2008) T L Yuan et al.   ONCOGENE