Efficacy of PI3K inhibitors in advanced breast cancer

Navigating metabolic pathways to enhance antitumour immunity and immunotherapy

(2019) Xiaoyun Li et al.   Nature Reviews Clinical Oncology

A Phase II Randomized Study of Neoadjuvant Letrozole Plus Alpelisib for Hormone Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Breast Cancer (NEO-ORB)

(2019) Ingrid A. Mayer et al.   CLINICAL CANCER RESEARCH

149OOutcome and mutational landscape of patients with PIK3CA-mutated metastatic breast cancer (mBC)

(2019) M F Mosele et al.   ANNALS OF ONCOLOGY

Molecular profiling of ER+ metastatic breast cancers to reveal association of genomic alterations with acquired resistance to CDK4/6 inhibitors.

(2019) Pedram Razavi et al.   JOURNAL OF CLINICAL ONCOLOGY

Genomic characterization of metastatic breast cancers

(2019) François Bertucci et al.   NATURE

Alpelisib for PIK3CA-Mutated, Hormone Receptor–Positive Advanced Breast Cancer

(2019) Fabrice André et al.   NEW ENGLAND JOURNAL OF MEDICINE

Overall Survival with Ribociclib plus Endocrine Therapy in Breast Cancer

(2019) Seock-Ah Im et al.   NEW ENGLAND JOURNAL OF MEDICINE

Neoadjuvant letrozole plus taselisib versus letrozole plus placebo in postmenopausal women with oestrogen receptor-positive, HER2-negative, early-stage breast cancer (LORELEI): a multicentre, randomised, double-blind, placebo-controlled, phase 2 trial

(2019) Cristina Saura et al.   LANCET ONCOLOGY

1938PCharacterization of the mechanism of action and efficacy of MEN1611 (PA799), a novel PI3K inhibitor, in breast cancer preclinical models

(2019) A Fiascarelli et al.   ANNALS OF ONCOLOGY

Phase I study of alpelisib (BYL-719) and trastuzumab emtansine (T-DM1) in HER2-positive metastatic breast cancer (MBC) after trastuzumab and taxane therapy

(2018) Sarika Jain et al.   BREAST CANCER RESEARCH AND TREATMENT

Phosphatidylinositol 3-Kinase α–Selective Inhibition With Alpelisib (BYL719) in PIK3CA-Altered Solid Tumors: Results From the First-in-Human Study

(2018) Dejan Juric et al.   JOURNAL OF CLINICAL ONCOLOGY

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

CDK4/6 Inhibition in Cancer: Beyond Cell Cycle Arrest

(2018) Shom Goel et al.   TRENDS IN CELL BIOLOGY

Spotlight on copanlisib and its potential in the treatment of relapsed/refractory follicular lymphoma: evidence to date

(2018) Felix Mensah et al.   OncoTargets and Therapy

The genetic landscape and clonal evolution of breast cancer resistance to palbociclib plus fulvestrant in the PALOMA-3 trial

(2018) Ben O'Leary et al.   Cancer Discovery

Neoadjuvant buparlisib plus trastuzumab and paclitaxel for women with HER2+ primary breast cancer: A randomised, double-blind, placebo-controlled phase II trial (NeoPHOEBE)

(2017) Sibylle Loibl et al.   EUROPEAN JOURNAL OF CANCER

MONARCH 3: Abemaciclib As Initial Therapy for Advanced Breast Cancer

(2017) Matthew P. Goetz et al.   JOURNAL OF CLINICAL ONCOLOGY

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

Phase I Dose-Escalation Study of Taselisib, an Oral PI3K Inhibitor, in Patients with Advanced Solid Tumors

(2017) Dejan Juric et al.   Cancer Discovery

PIK3CAmutations are associated with reduced pathological complete response rates in primary HER2-positive breast cancer: pooled analysis of 967 patients from five prospective trials investigating lapatinib and trastuzumab

(2016) S. Loibl et al.   ANNALS OF ONCOLOGY

Consensus on precision medicine for metastatic cancers: a report from the MAP conference: Table 1.

(2016) C. Swanton et al.   ANNALS OF ONCOLOGY

Pictilisib PI3Kinase inhibitor (a phosphatidylinositol 3-kinase [PI3K] inhibitor) plus paclitaxel for the treatment of hormone receptor-positive, HER2-negative, locally recurrent, or metastatic breast cancer: interim analysis of the multicentre, placebo-controlled, phase II randomised PEGGY study

(2016) P. Vuylsteke et al.   ANNALS OF ONCOLOGY

Early Adaptation and Acquired Resistance to CDK4/6 Inhibition in Estrogen Receptor–Positive Breast Cancer

(2016) Maria Teresa Herrera-Abreu et al.   CANCER RESEARCH

New insights on PI3K/AKT pathway alterations and clinical outcomes in breast cancer

(2016) Sherry X. Yang et al.   CANCER TREATMENT REVIEWS

Relationship between Tumor Biomarkers and Efficacy in EMILIA, a Phase III Study of Trastuzumab Emtansine in HER2-Positive Metastatic Breast Cancer

(2016) J. Baselga et al.   CLINICAL CANCER RESEARCH

Pictilisib for oestrogen receptor-positive, aromatase inhibitor-resistant, advanced or metastatic breast cancer (FERGI): a randomised, double-blind, placebo-controlled, phase 2 trial

(2016) Ian E Krop et al.   LANCET ONCOLOGY

Fulvestrant plus palbociclib versus fulvestrant plus placebo for treatment of hormone-receptor-positive, HER2-negative metastatic breast cancer that progressed on previous endocrine therapy (PALOMA-3): final analysis of the multicentre, double-blind, phase 3 randomised controlled trial

(2016) Massimo Cristofanilli et al.   LANCET ONCOLOGY

Palbociclib and Letrozole in Advanced Breast Cancer

(2016) Richard S. Finn et al.   NEW ENGLAND JOURNAL OF MEDICINE

Neoadjuvant Endocrine Therapy for Estrogen Receptor–Positive Breast Cancer

(2016) Laura M. Spring et al.   JAMA Oncology

A Phase I Trial of BKM120 (Buparlisib) in Combination with Fulvestrant in Postmenopausal Women with Estrogen Receptor-Positive Metastatic Breast Cancer

(2015) C. X. Ma 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

CDK 4/6 Inhibitors Sensitize PIK3CA Mutant Breast Cancer to PI3K Inhibitors

(2014) Sadhna R. Vora et al.   CANCER CELL

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

Stand Up to Cancer Phase Ib Study of Pan-Phosphoinositide-3-Kinase Inhibitor Buparlisib With Letrozole in Estrogen Receptor-Positive/Human Epidermal Growth Factor Receptor 2-Negative Metastatic Breast Cancer

(2014) Ingrid A. Mayer et al.   JOURNAL OF CLINICAL ONCOLOGY

Biomarker Analyses in CLEOPATRA: A Phase III, Placebo-Controlled Study of Pertuzumab in Human Epidermal Growth Factor Receptor 2–Positive, First-Line Metastatic Breast Cancer

(2014) José Baselga et al.   JOURNAL OF CLINICAL ONCOLOGY

Double-Blind, Placebo-Controlled, Multicenter, Randomized, Phase IIB Neoadjuvant Study of Letrozole-Lapatinib in Postmenopausal Hormone Receptor–Positive, Human Epidermal Growth Factor Receptor 2–Negative, Operable Breast Cancer

(2014) Valentina Guarneri et al.   JOURNAL OF CLINICAL ONCOLOGY

Picking the Point of Inhibition: A Comparative Review of PI3K/AKT/mTOR Pathway Inhibitors

(2014) R. Dienstmann et al.   MOLECULAR CANCER THERAPEUTICS

Characterization of the Novel and Specific PI3K  Inhibitor NVP-BYL719 and Development of the Patient Stratification Strategy for Clinical Trials

(2014) C. Fritsch et al.   MOLECULAR CANCER THERAPEUTICS

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

(2014) Dejan Juric et al.   NATURE

Prognostic role of PIK3CA mutations and their association with hormone receptor expression in breast cancer: a meta-analysis

(2014) Bo Pang et al.   Scientific Reports

Increased pathological complete response rate after a long-term neoadjuvant letrozole treatment in postmenopausal oestrogen and/or progesterone receptor-positive breast cancer

(2013) G Allevi et al.   BRITISH JOURNAL OF CANCER

Discovery of 2-{3-[2-(1-Isopropyl-3-methyl-1H-1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β-Sparing Phosphoinositide 3-Kinase Inhibitor with High Unbound Exposure and Robust in Vivo Antitumor Activity

(2013) Chudi O. Ndubaku et al.   JOURNAL OF MEDICINAL CHEMISTRY

Mutant PIK3CA accelerates HER2-driven transgenic mammary tumors and induces resistance to combinations of anti-HER2 therapies

(2013) A. B. Hanker et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Detection of Tumor PIK3CA Status in Metastatic Breast Cancer Using Peripheral Blood

(2012) M. J. Higgins et al.   CLINICAL CANCER RESEARCH

Comprehensive molecular portraits of human breast tumours

(2012) Daniel C. Koboldt et al.   NATURE

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

(2012) Ashish Juvekar et al.   Cancer Discovery

PIK3CA mutations, PTEN, and pHER2 expression and impact on outcome in HER2-positive early-stage breast cancer patients treated with adjuvant chemotherapy and trastuzumab

(2011) J. D. Jensen et al.   ANNALS OF ONCOLOGY

Identification and Characterization of NVP-BKM120, an Orally Available Pan-Class I PI3-Kinase Inhibitor

(2011) S.-M. Maira et al.   MOLECULAR CANCER THERAPEUTICS

Specific Roles of the p110α Isoform of Phosphatidylinsositol 3-Kinase in Hepatic Insulin Signaling and Metabolic Regulation

(2010) Victoria Rotter Sopasakis et al.   Cell Metabolism

Hyperactivation of phosphatidylinositol-3 kinase promotes escape from hormone dependence in estrogen receptor–positive human breast cancer

(2010) Todd W. Miller et al.   JOURNAL OF CLINICAL INVESTIGATION

The emerging mechanisms of isoform-specific PI3K signalling

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

Phosphatidyl-inositol-3-kinase alpha catalytic subunit mutation and response to neoadjuvant endocrine therapy for estrogen receptor positive breast cancer

(2009) Matthew J. Ellis et al.   BREAST CANCER RESEARCH AND TREATMENT

PIK3CA Mutation Associates with Improved Outcome in Breast Cancer

(2009) K. Kalinsky et al.   CLINICAL CANCER RESEARCH

PI3K pathway activation in breast cancer is associated with the basal-like phenotype and cancer-specific mortality

(2009) Elena López-Knowles et al.   INTERNATIONAL JOURNAL OF CANCER

An Integrative Genomic and Proteomic Analysis of PIK3CA, PTEN, and AKT Mutations in Breast Cancer

(2008) K. Stemke-Hale et al.   CANCER RESEARCH

The Identification of 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer†

(2008) Adrian J. Folkes et al.   JOURNAL OF MEDICINAL CHEMISTRY

Angiogenesis selectively requires the p110α isoform of PI3K to control endothelial cell migration

(2008) Mariona Graupera et al.   NATURE

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

(2008) Shidong Jia et al.   NATURE

Phosphoinositide 3-Kinase p110  Activity: Key Role in Metabolism and Mammary Gland Cancer but Not Development

(2008) E. Ciraolo et al.   Science Signaling