Targeting the PI3-kinase pathway in triple-negative breast cancer

BEECH: A dose-finding run-in followed by a randomised phase 2 study assessing the efficacy of AKT inhibitor capivasertib (AZD5363) combined with paclitaxel in patients with oestrogen receptor-positive advanced or metastatic breast cancer, and in a PIK3CA mutant sub-population

(2019) N C Turner et al.   ANNALS OF ONCOLOGY

Unravelling triple-negative breast cancer molecular heterogeneity using an integrative multiomic analysis

(2018) Y Bareche et al.   ANNALS OF ONCOLOGY

First-in human, phase 1, dose-escalation pharmacokinetic and pharmacodynamic study of the oral dual PI3K and mTORC1/2 inhibitor PQR309 in patients with advanced solid tumors (SAKK 67/13)

(2018) Andreas Wicki et al.   EUROPEAN JOURNAL OF CANCER

Phase III study of taselisib (GDC-0032) + fulvestrant (FULV) v FULV in patients (pts) with estrogen receptor (ER)-positive, PIK3CA-mutant (MUT), locally advanced or metastatic breast cancer (MBC): Primary analysis from SANDPIPER.

(2018) Jose Baselga et al.   JOURNAL OF CLINICAL ONCOLOGY

Buparlisib plus fulvestrant in postmenopausal women with hormone-receptor-positive, HER2-negative, advanced breast cancer progressing on or after mTOR inhibition (BELLE-3): a randomised, double-blind, placebo-controlled, phase 3 trial

(2018) Angelo Di Leo et al.   LANCET ONCOLOGY

Carboplatin in BRCA1/2-mutated and triple-negative breast cancer BRCAness subgroups: the TNT Trial

(2018) Andrew Tutt et al.   NATURE MEDICINE

The functions and regulation of the PTEN tumour suppressor: new modes and prospects

(2018) Yu-Ru Lee et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

IPATunity130: A pivotal randomized phase III trial evaluating ipatasertib (IPAT) + paclitaxel (PAC) for PIK3CA/AKT1/PTEN-altered advanced triple-negative (TN) or hormone receptor-positive HER2-negative (HR+/HER2–) breast cancer (BC).

(2018) Rebecca Dent et al.   JOURNAL OF CLINICAL ONCOLOGY

AZD5363 plus paclitaxel versus placebo plus paclitaxel as first-line therapy for metastatic triple-negative breast cancer (PAKT): A randomised, double-blind, placebo-controlled, phase II trial.

(2018) Peter Schmid et al.   JOURNAL OF CLINICAL ONCOLOGY

Talazoparib in Patients with Advanced Breast Cancer and a Germline BRCA Mutation

(2018) Jennifer K. Litton et al.   NEW ENGLAND JOURNAL OF MEDICINE

Long-term Clinical Outcomes and Biomarker Analyses of Atezolizumab Therapy for Patients With Metastatic Triple-Negative Breast Cancer

(2018) Leisha A. Emens et al.   JAMA Oncology

Atezolizumab and Nab-Paclitaxel in Advanced Triple-Negative Breast Cancer

(2018) Peter Schmid et al.   NEW ENGLAND JOURNAL OF MEDICINE

Randomized Phase II Study Evaluating Akt Blockade with Ipatasertib, in Combination with Abiraterone, in Patients with Metastatic Prostate Cancer with and without PTEN Loss

(2018) Johann S. de Bono et al.   CLINICAL CANCER RESEARCH

Loss of PTEN Is Associated with Resistance to Anti-PD-1 Checkpoint Blockade Therapy in Metastatic Uterine Leiomyosarcoma

(2017) Suzanne George et al.   IMMUNITY

Buparlisib plus fulvestrant versus placebo plus fulvestrant in postmenopausal, hormone receptor-positive, HER2-negative, advanced breast cancer (BELLE-2): a randomised, double-blind, placebo-controlled, phase 3 trial

(2017) José Baselga et al.   LANCET ONCOLOGY

Ipatasertib plus paclitaxel versus placebo plus paclitaxel as first-line therapy for metastatic triple-negative breast cancer (LOTUS): a multicentre, randomised, double-blind, placebo-controlled, phase 2 trial

(2017) Sung-Bae Kim et al.   LANCET ONCOLOGY

Olaparib for Metastatic Breast Cancer in Patients with a Germline BRCA Mutation

(2017) Mark Robson et al.   NEW ENGLAND JOURNAL OF MEDICINE

Accelerating Discovery of Functional Mutant Alleles in Cancer

(2017) Matthew T. Chang et al.   Cancer Discovery

Loss of PTEN expression in breast cancer: association with clinicopathological characteristics and prognosis

(2017) Shuting Li et al.   Oncotarget

Targeting the PI3K/AKT/mTOR Pathway for the Treatment of Mesenchymal Triple-Negative Breast Cancer

(2017) Reva K. Basho et al.   JAMA Oncology

AKT1 and AKT2 isoforms play distinct roles during breast cancer progression through the regulation of specific downstream proteins

(2017) Marina Riggio et al.   Scientific Reports

Phase I Study of Apitolisib (GDC-0980), Dual Phosphatidylinositol-3-Kinase and Mammalian Target of Rapamycin Kinase Inhibitor, in Patients with Advanced Solid Tumors

(2016) S. O. Dolly et al.   CLINICAL CANCER RESEARCH

Molecular Alterations and Everolimus Efficacy in Human Epidermal Growth Factor Receptor 2–Overexpressing Metastatic Breast Cancers: Combined Exploratory Biomarker Analysis From BOLERO-1 and BOLERO-3

(2016) Fabrice André et al.   JOURNAL OF CLINICAL ONCOLOGY

Pembrolizumab in Patients With Advanced Triple-Negative Breast Cancer: Phase Ib KEYNOTE-012 Study

(2016) Rita Nanda et al.   JOURNAL OF CLINICAL ONCOLOGY

Inhibition of the PI3K/AKT/mTOR Pathway in Solid Tumors

(2016) Patricia Mucci LoRusso   JOURNAL OF CLINICAL ONCOLOGY

The somatic mutation profiles of 2,433 breast cancers refines their genomic and transcriptomic landscapes

(2016) Bernard Pereira et al.   Nature Communications

A First-in-Human Phase I Study of the ATP-Competitive AKT Inhibitor Ipatasertib Demonstrates Robust and Safe Targeting of AKT in Patients with Solid Tumors

(2016) Cristina Saura et al.   Cancer Discovery

Loss of PTEN expression is associated with aggressive behavior and poor prognosis in Middle Eastern triple-negative breast cancer

(2015) Shaham Beg et al.   BREAST CANCER RESEARCH AND TREATMENT

First-in-Human Study of PF-05212384 (PKI-587), a Small-Molecule, Intravenous, Dual Inhibitor of PI3K and mTOR in Patients with Advanced Cancer

(2015) G. I. Shapiro et al.   CLINICAL CANCER RESEARCH

Combination of everolimus with trastuzumab plus paclitaxel as first-line treatment for patients with HER2-positive advanced breast cancer (BOLERO-1): a phase 3, randomised, double-blind, multicentre trial

(2015) Sara A Hurvitz et al.   LANCET ONCOLOGY

INPP4B Is a PtdIns(3,4,5)P3 Phosphatase That Can Act as a Tumor Suppressor

(2015) S. Kofuji et al.   Cancer Discovery

Loss of PTEN Promotes Resistance to T Cell-Mediated Immunotherapy

(2015) W. Peng et al.   Cancer Discovery

Recurrent AKT mutations in human cancers: functional consequences and effects on drug sensitivity

(2015) Kyung H. Yi et al.   Oncotarget

Trastuzumab resistance induces EMT to transform HER2+ PTEN− to a triple negative breast cancer that requires unique treatment options

(2015) Joseph P. Burnett et al.   Scientific Reports

Cancer-Associated PTEN Mutants Act in a Dominant-Negative Manner to Suppress PTEN Protein Function

(2014) Antonella Papa et al.   CELL

Convergent loss of PTEN leads to clinical resistance to a PI(3)Kα inhibitor

(2014) Dejan Juric et al.   NATURE

PD-L1 Expression in Triple-Negative Breast Cancer

(2014) E. A. Mittendorf et al.   Cancer Immunology Research

Targeting Akt3 Signaling in Triple-Negative Breast Cancer

(2013) Y. R. Chin et al.   CANCER RESEARCH

Targeting Activated Akt with GDC-0068, a Novel Selective Akt Inhibitor That Is Efficacious in Multiple Tumor Models

(2013) J. Lin et al.   CLINICAL CANCER RESEARCH

A survey of immunohistochemical biomarkers for basal-like breast cancer against a gene expression profile gold standard

(2013) Jennifer R Won et al.   MODERN PATHOLOGY

Combined Targeting of mTOR and AKT Is an Effective Strategy for Basal-like Breast Cancer in Patient-Derived Xenograft Models

(2013) S. Xu et al.   MOLECULAR CANCER THERAPEUTICS

Triple Negative Breast Tumors in African-American and Hispanic/Latina Women Are High in CD44+, Low in CD24+, and Have Loss of PTEN

(2013) Yanyuan Wu et al.   PLoS One

Optimal strategies for the treatment of metastatic triple-negative breast cancer with currently approved agents

(2012) F. Andre et al.   ANNALS OF ONCOLOGY

The clonal and mutational evolution spectrum of primary triple-negative breast cancers

(2012) Sohrab P. Shah et al.   NATURE

Comprehensive molecular portraits of human breast tumours

(2012) Daniel C. Koboldt et al.   NATURE

The functions and regulation of the PTEN tumour suppressor

(2012) Min Sup Song et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

PI3K Inhibition Impairs BRCA1/2 Expression and Sensitizes BRCA-Proficient Triple-Negative Breast Cancer to PARP Inhibition

(2012) Yasir H. Ibrahim et al.   Cancer Discovery

Combining a PI3K Inhibitor with a PARP Inhibitor Provides an Effective Therapy for BRCA1-Related Breast Cancer

(2012) Ashish Juvekar et al.   Cancer Discovery

AKT Inhibition Relieves Feedback Suppression of Receptor Tyrosine Kinase Expression and Activity

(2011) Sarat Chandarlapaty et al.   CANCER CELL

Identification of human triple-negative breast cancer subtypes and preclinical models for selection of targeted therapies

(2011) Brian D. Lehmann et al.   JOURNAL OF CLINICAL INVESTIGATION

Eribulin monotherapy versus treatment of physician's choice in patients with metastatic breast cancer (EMBRACE): a phase 3 open-label randomised study

(2011) Javier Cortes et al.   LANCET

Everolimus in Postmenopausal Hormone-Receptor–Positive Advanced Breast Cancer

(2011) José Baselga et al.   NEW ENGLAND JOURNAL OF MEDICINE

PI3K inhibition results in enhanced HER signaling and acquired ERK dependency in HER2-overexpressing breast cancer

(2011) V Serra et al.   ONCOGENE

Targeting the Phosphoinositide-3 (PI3) Kinase Pathway in Breast Cancer

(2011) J. Baselga   ONCOLOGIST

An Activating Mutation of AKT2 and Human Hypoglycemia

(2011) K. Hussain et al.   SCIENCE

The Ras-ERK and PI3K-mTOR pathways: cross-talk and compensation

(2011) Michelle C. Mendoza et al.   TRENDS IN BIOCHEMICAL SCIENCES

Inositol polyphosphate 4-phosphatase II regulates PI3K/Akt signaling and is lost in human basal-like breast cancers

(2010) C. G. Fedele et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Evidence that Inositol Polyphosphate 4-Phosphatase Type II Is a Tumor Suppressor that Inhibits PI3K Signaling

(2009) Christina Gewinner et al.   CANCER CELL

Differential Expression of PTEN-Targeting MicroRNAs miR-19a and miR-21 in Cowden Syndrome

(2008) Marcus G. Pezzolesi et al.   AMERICAN JOURNAL OF HUMAN GENETICS

A novel AKT3 mutation in melanoma tumours and cell lines

(2008) M A Davies et al.   BRITISH JOURNAL OF CANCER

The TSC1-TSC2 Complex Is Required for Proper Activation of mTOR Complex 2

(2008) J. Huang et al.   MOLECULAR AND CELLULAR BIOLOGY

Essential roles of PI(3)K–p110β in cell growth, metabolism and tumorigenesis

(2008) Shidong Jia et al.   NATURE

PTEN-deficient cancers depend on PIK3CB

(2008) S. Wee et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA