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

Phosphatidylinositol 3-kinase δ blockade increases genomic instability in B cells

(2017) Mara Compagno et al.   NATURE

Idelalisib given front-line for treatment of chronic lymphocytic leukemia causes frequent immune-mediated hepatotoxicity

(2016) B. L. Lampson et al.   BLOOD

Cancer treatment and survivorship statistics, 2016

(2016) Kimberly D. Miller et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Discovery and SAR of Novel 2,3-Dihydroimidazo[1,2-c]quinazoline PI3K Inhibitors: Identification of Copanlisib (BAY 80-6946)

(2016) William J. Scott et al.   ChemMedChem

A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER + /HER2 − Metastatic Breast Cancer

(2016) Ingrid A. Mayer et al.   CLINICAL CANCER RESEARCH

Idelalisib Impacts Cell Growth through Inhibiting Translation-Regulatory Mechanisms in Mantle Cell Lymphoma

(2016) Qingshan Yang et al.   CLINICAL CANCER RESEARCH

Duvelisib treatment is associated with altered expression of apoptotic regulators that helps in sensitization of chronic lymphocytic leukemia cells to venetoclax (ABT-199)

(2016) V M Patel et al.   LEUKEMIA

Erratum: The pan phosphoinositide 3-kinase/mammalian target of rapamycin inhibitor SAR245409 (voxtalisib/XL765) blocks survival, adhesion and proliferation of primary chronic lymphocytic leukemia cells

(2016) R Thijssen et al.   LEUKEMIA

Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate

(2016) Catherine A. Evans et al.   ACS Medicinal Chemistry Letters

BKM-120 (Buparlisib): A Phosphatidyl-Inositol-3 Kinase Inhibitor with Anti-Invasive Properties in Glioblastoma

(2016) Maria-Carmela Speranza et al.   Scientific Reports

A phase 2 study of idelalisib plus rituximab in treatment-naive older patients with chronic lymphocytic leukemia

(2015) S. M. O'Brien et al.   BLOOD

Phase I Trial of the Pan-PI3K Inhibitor Pilaralisib (SAR245408/XL147) in Patients with Chronic Lymphocytic Leukemia (CLL) or Relapsed/Refractory Lymphoma

(2015) J. R. Brown et al.   CLINICAL CANCER RESEARCH

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

FDA Approval: Idelalisib Monotherapy for the Treatment of Patients with Follicular Lymphoma and Small Lymphocytic Lymphoma

(2015) B. W. Miller et al.   CLINICAL CANCER RESEARCH

Buparlisib, an oral pan-PI3K inhibitor for the treatment of breast cancer

(2015) Elena Geuna et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Phase II study of the PI3K inhibitor pilaralisib (SAR245408; XL147) in patients with advanced or recurrent endometrial carcinoma

(2015) Ursula Matulonis et al.   GYNECOLOGIC ONCOLOGY

Discovery of (R)-8-(1-(3,5-Difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): A Potent and Selective Inhibitor of PI3Kβ and PI3Kδ for the Treatment of PTEN-Deficient Cancers

(2015) Bernard Barlaam et al.   JOURNAL OF MEDICINAL CHEMISTRY

Safety and Efficacy of Buparlisib (BKM120) in Patients with PI3K Pathway-Activated Non-Small Cell Lung Cancer

(2015) Johan F. Vansteenkiste et al.   Journal of Thoracic Oncology

The phosphoinositide-3-kinase (PI3K)-delta and gamma inhibitor, IPI-145 (Duvelisib), overcomes signals from the PI3K/AKT/S6 pathway and promotes apoptosis in CLL

(2015) K Balakrishnan et al.   LEUKEMIA

Take (STAT)5: jazzing up T-cell leukemia

(2014) P. Porcu et al.   BLOOD

IPI-145 antagonizes intrinsic and extrinsic survival signals in chronic lymphocytic leukemia cells

(2014) S. Dong et al.   BLOOD

A preclinical evaluation of the PI3K alpha/delta dominant inhibitor BAY 80-6946 in HER2-positive breast cancer models with acquired resistance to the HER2-targeted therapies trastuzumab and lapatinib

(2014) N. Elster et al.   BREAST CANCER RESEARCH AND TREATMENT

Phase I dose-escalation study of buparlisib (BKM120), an oral pan-class I PI3K inhibitor, in Japanese patients with advanced solid tumors

(2014) Yuichi Ando et al.   CANCER SCIENCE

First-in-Human Phase I Study of Pictilisib (GDC-0941), a Potent Pan-Class I Phosphatidylinositol-3-Kinase (PI3K) Inhibitor, in Patients with Advanced Solid Tumors

(2014) D. Sarker et al.   CLINICAL CANCER RESEARCH

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

A Randomized, Phase 2 Trial of Docetaxel with or without PX-866, an Irreversible Oral Phosphatidylinositol 3-Kinase Inhibitor, in Patients with Relapsed or Metastatic Non–Small-Cell Lung Cancer

(2014) Benjamin Levy et al.   Journal of Thoracic Oncology

Inhibition of PI3K  Signaling with AZD8186 Inhibits Growth of PTEN-Deficient Breast and Prostate Tumors Alone and in Combination with Docetaxel

(2014) U. Hancox et al.   MOLECULAR CANCER THERAPEUTICS

Idelalisib and Rituximab in Relapsed Chronic Lymphocytic Leukemia

(2014) Richard R. Furman et al.   NEW ENGLAND JOURNAL OF MEDICINE

A multicenter phase 1 study of PX-866 in combination with docetaxel in patients with advanced solid tumours

(2013) D W Bowles et al.   BRITISH JOURNAL OF CANCER

PI3K-δ and PI3K-γ Inhibition by IPI-145 Abrogates Immune Responses and Suppresses Activity in Autoimmune and Inflammatory Disease Models

(2013) David G. Winkler et al.   CHEMISTRY & BIOLOGY

PI3K Pathway Dependencies in Endometrioid Endometrial Cancer Cell Lines

(2013) B. Weigelt et al.   CLINICAL CANCER RESEARCH

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

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

An educational infusion: more synergy between Blood and the American Society of Hematology

(2012) C. E. Dunbar   BLOOD

The B-cell receptor signaling pathway as a therapeutic target in CLL

(2012) J. A. Woyach et al.   BLOOD

Multiple roles for the p85α isoform in the regulation and function of PI3K signalling and receptor trafficking

(2011) Paul Mellor et al.   BIOCHEMICAL JOURNAL

PI3K  inhibitor, GS-1101 (CAL-101), attenuates pathway signaling, induces apoptosis, and overcomes signals from the microenvironment in cellular models of Hodgkin lymphoma

(2011) S. A. Meadows et al.   BLOOD

CAL-101, a p110  selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability

(2010) B. J. Lannutti et al.   BLOOD

Phosphatidylinositol 3-kinase-  inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals

(2010) S. E. M. Herman et al.   BLOOD

Coordinate suppression of B cell lymphoma by PTEN and SHIP phosphatases

(2010) Ana V. Miletic et al.   JOURNAL OF EXPERIMENTAL MEDICINE

The emerging mechanisms of isoform-specific PI3K signalling

(2010) Bart Vanhaesebroeck et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Effect of ZSTK474, a Novel Phosphatidylinositol 3-Kinase Inhibitor, on DNA-Dependent Protein Kinase

(2009) Dexin Kong et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

Antiangiogenic effect of ZSTK474, a novel phosphatidylinositol 3-kinase inhibitor

(2009) Dexin Kong et al.   EUROPEAN JOURNAL OF CANCER

Targeting the phosphoinositide 3-kinase pathway in cancer

(2009) Pixu Liu et al.   NATURE REVIEWS DRUG DISCOVERY

Phosphoinositide 3-Kinases γ and δ, Linkers of Coordinate C5a Receptor-Fcγ Receptor Activation and Immune Complex-induced Inflammation

(2008) Stephanie Konrad et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeting phosphoinositide 3-kinase—Moving towards therapy

(2007) Romina Marone et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS