The emerging role of PI3K inhibitors for solid tumour treatment and beyond

Phase II Study of Copanlisib in Patients With Tumors With PIK3CA Mutations: Results From the NCI-MATCH ECOG-ACRIN Trial (EAY131) Subprotocol Z1F

(2022) Senthil Damodaran et al.   JOURNAL OF CLINICAL ONCOLOGY

Molecular Glues: The Adhesive Connecting Targeted Protein Degradation to the Clinic

(2022) Janet M. Sasso et al.   BIOCHEMISTRY

33O A phase I study to evaluate safety, pharmacokinetics (PK), and preliminary efficacy of CYH33, a phosphatidylinositol 3-kinase α (PI3Kα) inhibitor, in patients (pts) with advanced solid tumours

(2021) X-L. Wei et al.   ANNALS OF ONCOLOGY

Alpelisib plus fulvestrant in PIK3CA-mutated, hormone receptor-positive advanced breast cancer after a CDK4/6 inhibitor (BYLieve): one cohort of a phase 2, multicentre, open-label, non-comparative study

(2021) Hope S Rugo et al.   LANCET ONCOLOGY

SO-10 An open-label, multi-centre, phase Ib/II study of PI3Kβ selective inhibitor GSK2636771 administered in combination with paclitaxel in patients with advanced gastric cancer having alterations in PI3K/Akt pathway

(2021) M. Jung et al.   ANNALS OF ONCOLOGY

Alpelisib in combination with everolimus ± exemestane in solid tumours: Phase Ib randomised, open-label, multicentre study

(2021) Giuseppe Curigliano et al.   EUROPEAN JOURNAL OF CANCER

Ipatasertib plus abiraterone and prednisolone in metastatic castration-resistant prostate cancer (IPATential150): a multicentre, randomised, double-blind, phase 3 trial

(2021) Christopher Sweeney et al.   LANCET

Outcome and molecular landscape of patients with PIK3CA-mutated metastatic breast cancer

(2020) F. Mosele et al.   ANNALS OF ONCOLOGY

The evolutionary history of 2,658 cancers

(2020) Moritz Gerstung et al.   NATURE

Immunomodulation by targeted anticancer agents

(2020) Giulia Petroni et al.   CANCER CELL

Phase III randomized study of taselisib or placebo with fulvestrant in estrogen receptor-positive, PIK3CA-mutant, HER2-negative, advanced breast cancer: the SANDPIPER trial

(2020) S. Dent et al.   ANNALS OF ONCOLOGY

Alpelisib plus fulvestrant for PIK3CA-mutated, hormone receptor-positive, human epidermal growth factor receptor-2–negative advanced breast cancer: final overall survival results from SOLAR-1

(2020) F. André et al.   ANNALS OF ONCOLOGY

1ODouble PIK3CA mutations in cis enhance PI3Kα oncogene activation and sensitivity to PI3Kα inhibitors in breast cancer

(2019) N Vasan et al.   ANNALS OF ONCOLOGY

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

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

PI3K Inhibition Activates SGK1 via a Feedback Loop to Promote Chromatin-Based Regulation of ER-Dependent Gene Expression

(2019) Eneda Toska et al.   Cell Reports

Capivasertib Plus Paclitaxel Versus Placebo Plus Paclitaxel As First-Line Therapy for Metastatic Triple-Negative Breast Cancer: The PAKT Trial

(2019) Peter Schmid 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

Targeting the PI3K pathway in cancer: are we making headway?

(2018) Filip Janku et al.   Nature Reviews Clinical Oncology

Suppression of insulin feedback enhances the efficacy of PI3K inhibitors

(2018) Benjamin D. Hopkins et al.   NATURE

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

Buparlisib and paclitaxel in patients with platinum-pretreated recurrent or metastatic squamous cell carcinoma of the head and neck (BERIL-1): a randomised, double-blind, placebo-controlled phase 2 trial

(2017) Denis Soulières et al.   LANCET ONCOLOGY

Mutational landscape of metastatic cancer revealed from prospective clinical sequencing of 10,000 patients

(2017) Ahmet Zehir et al.   NATURE MEDICINE

PI3K pathway regulates ER-dependent transcription in breast cancer through the epigenetic regulator KMT2D

(2017) Eneda Toska et al.   SCIENCE

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

(2017) Dejan Juric et al.   Cancer Discovery

A randomized adaptive phase II/III study of buparlisib, a pan-class I PI3K inhibitor, combined with paclitaxel for the treatment of HER2− advanced breast cancer (BELLE-4)

(2016) M. Martín 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

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

Everolimus for the treatment of advanced, non-functional neuroendocrine tumours of the lung or gastrointestinal tract (RADIANT-4): a randomised, placebo-controlled, phase 3 study

(2016) James C Yao et al.   LANCET

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

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

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 head and neck squamous cell cancer

(2015) Antonio Jimeno et al.   ORAL ONCOLOGY

PI3K inhibition results in enhanced estrogen receptor function and dependence in hormone receptor–positive breast cancer

(2015) Ana Bosch et al.   Science Translational Medicine

Clinical delineation and natural history of thePIK3CA-related overgrowth spectrum

(2014) Kim M. Keppler-Noreuil et al.   AMERICAN JOURNAL OF MEDICAL GENETICS PART A

Systematic review/Meta-analysis Anti-epidermal growth factor receptor monoclonal antibody-based therapy for metastatic colorectal cancer: a meta-analysis of the effect of PIK3CA mutations in KRAS wild-type patients

(2014) Lulu Huang et al.   Archives of Medical Science

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

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

(2014) Dejan Juric et al.   NATURE

Idelalisib and Rituximab in Relapsed Chronic Lymphocytic Leukemia

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

The landscape of kinase fusions in cancer

(2014) Nicolas Stransky et al.   Nature Communications

Inhibition of p85, the non-catalytic subunit of phosphatidylinositol 3-kinase, exerts potent antitumor activity in human breast cancer cells

(2012) V Folgiero et al.   Cell Death & Disease

PIK3CA exon 20 mutations as a potential biomarker for resistance to anti-EGFR monoclonal antibodies in KRAS wild-type metastatic colorectal cancer: a systematic review and meta-analysis

(2011) C. Mao et al.   ANNALS OF ONCOLOGY

Everolimus for Advanced Pancreatic Neuroendocrine Tumors

(2011) James C. Yao et al.   NEW ENGLAND JOURNAL OF MEDICINE

Everolimus in Postmenopausal Hormone-Receptor–Positive Advanced Breast Cancer

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

Pertuzumab plus Trastuzumab plus Docetaxel for Metastatic Breast Cancer

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

Effects of KRAS, BRAF, NRAS, and PIK3CA mutations on the efficacy of cetuximab plus chemotherapy in chemotherapy-refractory metastatic colorectal cancer: a retrospective consortium analysis

(2010) Wendy De Roock et al.   LANCET ONCOLOGY

The emerging mechanisms of isoform-specific PI3K signalling

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

Somatic Mutations in p85α Promote Tumorigenesis through Class IA PI3K Activation

(2009) Bijay S. Jaiswal et al.   CANCER CELL

PIK3CAMutation Is Associated With Poor Prognosis Among Patients With Curatively Resected Colon Cancer

(2009) Shuji Ogino et al.   JOURNAL OF CLINICAL ONCOLOGY

Targeting the phosphoinositide 3-kinase pathway in cancer

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

Efficacy of everolimus in advanced renal cell carcinoma: a double-blind, randomised, placebo-controlled phase III trial

(2008) Robert J Motzer et al.   LANCET