Development of PI3K inhibitors: lessons learned from early clinical trials (Q38080710)

28 August 2017

Development of PI3K inhibitors: lessons learned from early clinical trials (English)

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28 August 2017

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3

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28 August 2017

Josep Tabernero Caturla

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28 August 2017

Jordi Rodon

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28 August 2017

Rodrigo Dienstmann

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2

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28 August 2017

language of work or name

English

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publication date

12 February 2013

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Nature Reviews Clinical Oncology

28 August 2017

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28 August 2017

10

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28 August 2017

3

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28 August 2017

143-153

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The PI3K pathway as drug target in human cancer

28 August 2017

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https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

PI3K: a potential therapeutic target for cancer

31 March 2020

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Temsirolimus, interferon alfa, or both for advanced renal-cell carcinoma

31 March 2020

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Everolimus in postmenopausal hormone-receptor-positive advanced breast cancer

31 March 2020

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Phase 3 trial of everolimus for metastatic renal cell carcinoma : final results and analysis of prognostic factors

31 March 2020

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Everolimus for advanced pancreatic neuroendocrine tumors.

31 March 2020

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Phase I, dose-escalation study of BKM120, an oral pan-Class I PI3K inhibitor, in patients with advanced solid tumors

31 March 2020

1 reference

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First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors

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Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors

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Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma

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Improved survival with vemurafenib in melanoma with BRAF V600E mutation

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https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism

31 March 2020

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https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Reciprocal feedback regulation of PI3K and androgen receptor signaling in PTEN-deficient prostate cancer

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers

31 March 2020

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Helical domain and kinase domain mutations in p110alpha of phosphatidylinositol 3-kinase induce gain of function by different mechanisms

31 March 2020

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Sequence analysis of mutations and translocations across breast cancer subtypes

31 March 2020

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Next-generation mTOR inhibitors in clinical oncology: how pathway complexity informs therapeutic strategy

31 March 2020

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Phase III study to evaluate temsirolimus compared with investigator's choice therapy for the treatment of relapsed or refractory mantle cell lymphoma

31 March 2020

1 reference

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mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates Akt

31 March 2020

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Mutations in the phosphatidylinositol 3-kinase pathway: role in tumor progression and therapeutic implications in breast cancer

31 March 2020

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Rapamycin differentially inhibits S6Ks and 4E-BP1 to mediate cell-type-specific repression of mRNA translation

31 March 2020

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Multiple mechanisms control phosphorylation of PHAS-I in five (S/T)P sites that govern translational repression

31 March 2020

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https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Should individual PI3 kinase isoforms be targeted in cancer?

31 March 2020

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https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

PTEN-deficient cancers depend on PIK3CB.

31 March 2020

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https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity

31 March 2020

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AKT-independent signaling downstream of oncogenic PIK3CA mutations in human cancer

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Toxicity as a biomarker of efficacy of molecular targeted therapies: focus on EGFR and VEGF inhibiting anticancer drugs

31 March 2020

1 reference

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Intrapatient cetuximab dose escalation in metastatic colorectal cancer according to the grade of early skin reactions: the randomized EVEREST study

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Management of metabolic effects associated with anticancer agents targeting the PI3K-Akt-mTOR pathway

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Critical role for the p110alpha phosphoinositide-3-OH kinase in growth and metabolic regulation

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Safety of multi-targeted kinase inhibitors as monotherapy treatment of cancer: a systematic review of the literature

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

89 POSTER Evaluation of peripheral blood cells and hair as surrogate tissues for clinical trial pharmacodynamic assessment of XL147 and XL765, inhibitors of the PI3K signaling pathway

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

The skin and hair as surrogate tissues for measuring the target effect of inhibitors of phosphoinositide-3-kinase signaling

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

AKT/PKB signaling: navigating downstream

31 March 2020

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https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Understanding the Warburg effect: the metabolic requirements of cell proliferation

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

[18F]fluorodeoxyglucose positron emission tomography correlates with Akt pathway activity but is not predictive of clinical outcome during mTOR inhibitor therapy.

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

18FDG-PET predicts pharmacodynamic response to OSI-906, a dual IGF-1R/IR inhibitor, in preclinical mouse models of lung cancer

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Clinical development of phosphatidylinositol 3-kinase inhibitors for cancer treatment

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Specific apoptosis induction by the dual PI3K/mTor inhibitor NVP-BEZ235 in HER2 amplified and PIK3CA mutant breast cancer cells

31 March 2020

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https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Predictive biomarkers of sensitivity to the phosphatidylinositol 3' kinase inhibitor GDC-0941 in breast cancer preclinical models

31 March 2020

1 reference

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The dual PI3K/mTOR inhibitor NVP-BEZ235 induces tumor regression in a genetically engineered mouse model of PIK3CA wild-type colorectal cancer

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

PIK3CA mutation, but not PTEN loss of function, determines the sensitivity of breast cancer cells to mTOR inhibitory drugs

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

PIK3CA mutations in patients with advanced cancers treated with PI3K/AKT/mTOR axis inhibitors

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

RAF/MEK dependence of KRAS-mutant pancreatic ductal adenocarcinomas

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer

31 March 2020

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https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

A chemical screen in diverse breast cancer cell lines reveals genetic enhancers and suppressors of sensitivity to PI3K isoform-selective inhibition.

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

GDC-0941, a novel class I selective PI3K inhibitor, enhances the efficacy of docetaxel in human breast cancer models by increasing cell death in vitro and in vivo

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Isoform-specific phosphoinositide 3-kinase inhibitors exert distinct effects in solid tumors

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Comparison of phosphatidylinositol-3-kinase signalling within a panel of human colorectal cancer cell lines with mutant or wild-type PIK3CA.

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Genomic complexity and AKT dependence in serous ovarian cancer

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

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

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

AKT inhibition relieves feedback suppression of receptor tyrosine kinase expression and activity

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

mTOR kinase inhibition causes feedback-dependent biphasic regulation of AKT signaling

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

PI3K-targeted therapy can be evaded by gene amplification along the MYC-eukaryotic translation initiation factor 4E (eIF4E) axis

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Oncogenic PIK3CA-driven mammary tumors frequently recur via PI3K pathway-dependent and PI3K pathway-independent mechanisms

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

A chemical-genetic screen reveals a mechanism of resistance to PI3K inhibitors in cancer.

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

β-catenin confers resistance to PI3K and AKT inhibitors and subverts FOXO3a to promote metastasis in colon cancer

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

The clinical effect of the dual-targeting strategy involving PI3K/AKT/mTOR and RAS/MEK/ERK pathways in patients with advanced cancer.

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

PIK3CA and PIK3CB inhibition produce synthetic lethality when combined with estrogen deprivation in estrogen receptor-positive breast cancer

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

PKBalpha/Akt1 acts downstream of DNA-PK in the DNA double-strand break response and promotes survival

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

The efficacy of a novel, dual PI3K/mTOR inhibitor NVP-BEZ235 to enhance chemotherapy and antiangiogenic response in pancreatic cancer

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Tumor genetic testing for patient selection in phase I clinical trials: the case of PI3K inhibitors.

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Phase II randomized study of neoadjuvant everolimus plus letrozole compared with placebo plus letrozole in patients with estrogen receptor-positive breast cancer

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Dissecting "PI3Kness": the complexity of personalized therapy for ovarian cancer

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Detection of tumor PIK3CA status in metastatic breast cancer using peripheral blood

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Molecular prescreening to select patient population in early clinical trials

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Comprehensive molecular characterization of human colon and rectal cancer

31 March 2020

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https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Comprehensive genomic characterization defines human glioblastoma genes and core pathways

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Integrated genomic analyses of ovarian carcinoma

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Regulation of cancer cell metabolism

31 March 2020

1 reference

https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

INPP4B: the new kid on the PI3K block

31 March 2020

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https://api.crossref.org/works/10.1038%2FNRCLINONC.2013.10

Effect of PI3K/Akt pathway inhibition-mediated G1 arrest on chemosensitization in ovarian cancer cells

31 March 2020

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12 December 2020

Perifosine, a novel alkylphospholipid, inhibits protein kinase B activation

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12 December 2020

Gene alterations in the PI3K/PTEN/AKT pathway as a mechanism of drug-resistance (review).

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12 December 2020

Inhibition of mTORC1 leads to MAPK pathway activation through a PI3K-dependent feedback loop in human cancer

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12 December 2020

A phase Ib dose-escalation study of the oral pan-PI3K inhibitor buparlisib (BKM120) in combination with the oral MEK1/2 inhibitor trametinib (GSK1120212) in patients with selected advanced solid tumors

1 reference

12 December 2020

Clinical development of phosphatidylinositol-3 kinase pathway inhibitors

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12 December 2020

Inhibition of phosphatidylinositol 3'-kinase increases efficacy of paclitaxel in in vitro and in vivo ovarian cancer models.

1 reference

12 December 2020

10.1038/NRCLINONC.2013.10

Identifiers

DOI

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28 August 2017

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