Current and future directions in mammalian target of rapamycin inhibitors development

A phase I dose-escalation study of the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of a novel PI3K inhibitor, XL765, administered orally to patients (pts) with advanced solid tumors

(2017) K. P. Papadopoulos et al.   JOURNAL OF CLINICAL ONCOLOGY

Pharmacokinetics of oral deforolimus (AP23573, MK-8669)

(2017) G. J. Fetterly et al.   JOURNAL OF CLINICAL ONCOLOGY

First-in-human phase I study exploring three schedules of OSI-027, a novel small molecule TORC1/TORC2 inhibitor, in patients with advanced solid tumors and lymphoma.

(2017) D. S. Tan et al.   JOURNAL OF CLINICAL ONCOLOGY

A phase I dose-escalation study of the safety, pharmacokinetics (PK), and pharmacodynamics of XL765 (SAR245409), a PI3K/TORC1/TORC2 inhibitor administered orally to patients (pts) with advanced malignancies.

(2017) I. Brana et al.   JOURNAL OF CLINICAL ONCOLOGY

A first-in-human, phase l study to evaluate the dual PI3K/mTOR inhibitor GDC-0980 administered QD in patients with advanced solid tumors or non-Hodgkin's lymphoma.

(2017) S. Dolly et al.   JOURNAL OF CLINICAL ONCOLOGY

A phase I safety and pharmacokinetic study of XL765 (SAR245409), a novel PI3K/TORC1/TORC2 inhibitor, in combination with temozolomide (TMZ) in patients (pts) with newly diagnosed malignant glioma.

(2017) P. L. Nghiemphu et al.   JOURNAL OF CLINICAL ONCOLOGY

First-in-human phase I study of the oral PI3K inhibitor BEZ235 in patients (pts) with advanced solid tumors.

(2017) H. Burris et al.   JOURNAL OF CLINICAL ONCOLOGY

Targeting TOR dependence in cancer

(2015)   Oncotarget

Targeting mTOR globally in cancer: Thinking beyond rapamycin

(2011) Boris Shor et al.   CELL CYCLE

Beyond Rapalog Therapy: Preclinical Pharmacology and Antitumor Activity of WYE-125132, an ATP-Competitive and Specific Inhibitor of mTORC1 and mTORC2

(2010) K. Yu et al.   CANCER RESEARCH

Not all substrates are treated equally: Implications for mTOR, rapamycin-resistance, and cancer therapy

(2010) Andrew Y. Choo et al.   CELL CYCLE

Deregulation of the PI3K and KRAS signaling pathways in human cancer cells determines their response to everolimus

(2010) Federica Di Nicolantonio et al.   JOURNAL OF CLINICAL INVESTIGATION

Phase I and Pharmacologic Study of SNS-032, a Potent and Selective Cdk2, 7, and 9 Inhibitor, in Patients With Advanced Chronic Lymphocytic Leukemia and Multiple Myeloma

(2010) Wei-Gang Tong et al.   JOURNAL OF CLINICAL ONCOLOGY

The PI3K Pathway As Drug Target in Human Cancer

(2010) Kevin D. Courtney et al.   JOURNAL OF CLINICAL ONCOLOGY

Bis(morpholino-1,3,5-triazine) Derivatives: Potent Adenosine 5′-Triphosphate Competitive Phosphatidylinositol-3-kinase/Mammalian Target of Rapamycin Inhibitors: Discovery of Compound26(PKI-587), a Highly Efficacious Dual Inhibitor

(2010) Aranapakam M. Venkatesan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Kinase targets in renal-cell carcinomas: reassessing the old and discovering the new

(2010) Kyle A Furge et al.   LANCET ONCOLOGY

mTOR signaling and drug development in cancer

(2010) Janet Dancey   Nature Reviews Clinical Oncology

Discovery of the highly potent PI3K/mTOR dual inhibitor PF-04691502 through structure based drug design

(2010) Hengmiao Cheng et al.   MedChemComm

Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin

(2010) Steven D. Knight et al.   ACS Medicinal Chemistry Letters

A phase 2 study with a daily regimen of the oral mTOR inhibitor RAD001 (everolimus) in patients with metastatic clear cell renal cell cancer

(2009) Robert J. Amato et al.   CANCER

AZD8055 Is a Potent, Selective, and Orally Bioavailable ATP-Competitive Mammalian Target of Rapamycin Kinase Inhibitor with In vitro and In vivo Antitumor Activity

(2009) C. M. Chresta et al.   CANCER RESEARCH

Biochemical, Cellular, and In vivo Activity of Novel ATP-Competitive and Selective Inhibitors of the Mammalian Target of Rapamycin

(2009) K. Yu et al.   CANCER RESEARCH

PI3K and mTOR inhibitors—a new generation of targeted anticancer agents

(2009) Saskia Brachmann et al.   CURRENT OPINION IN CELL BIOLOGY

EORTC-GU group expert opinion on metastatic renal cell cancer

(2009) Theo M. de Reijke et al.   EUROPEAN JOURNAL OF CANCER

Phase III Study to Evaluate Temsirolimus Compared With Investigator's Choice Therapy for the Treatment of Relapsed or Refractory Mantle Cell Lymphoma

(2009) Georg Hess et al.   JOURNAL OF CLINICAL ONCOLOGY

Oropharyngeal Cancer, Human Papilloma Virus, and Clinical Trials

(2009) Danny Rischin   JOURNAL OF CLINICAL ONCOLOGY

Targeting tumorigenesis: development and use of mTOR inhibitors in cancer therapy

(2009) RuiRong Yuan et al.   Journal of Hematology & Oncology

The Pharmacology of mTOR Inhibition

(2009) D. A. Guertin et al.   Science Signaling

Active-Site Inhibitors of mTOR Target Rapamycin-Resistant Outputs of mTORC1 and mTORC2

(2009) Morris E Feldman et al.   PLOS BIOLOGY

Distinct functional significance of Akt and mTOR constitutive activation in mantle cell lymphoma

(2008) J. Dal Col et al.   BLOOD

Low-dose, single-agent temsirolimus for relapsed mantle cell lymphoma

(2008) Stephen M. Ansell et al.   CANCER

A Vascular Targeted Pan Phosphoinositide 3-Kinase Inhibitor Prodrug, SF1126, with Antitumor and Antiangiogenic Activity

(2008) J. R. Garlich et al.   CANCER RESEARCH

NVP-BEZ235, a Dual PI3K/mTOR Inhibitor, Prevents PI3K Signaling and Inhibits the Growth of Cancer Cells with Activating PI3K Mutations

(2008) V. Serra et al.   CANCER RESEARCH

The role of mTOR in the management of solid tumors: An overview

(2008) Alex S. Strimpakos et al.   CANCER TREATMENT REVIEWS

Improved Identification of von Hippel-Lindau Gene Alterations in Clear Cell Renal Tumors

(2008) M. L. Nickerson et al.   CLINICAL CANCER RESEARCH

mTOR inhibitors in the treatment of cancer

(2008) Angelica Fasolo et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Identifying Optimal Biologic Doses of Everolimus (RAD001) in Patients With Cancer Based on the Modeling of Preclinical and Clinical Pharmacokinetic and Pharmacodynamic Data

(2008) Chiaki Tanaka et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase I Trial of the Novel Mammalian Target of Rapamycin Inhibitor Deforolimus (AP23573; MK-8669) Administered Intravenously Daily for 5 Days Every 2 Weeks to Patients With Advanced Malignancies

(2008) Monica M. Mita et al.   JOURNAL OF CLINICAL ONCOLOGY

Dose Selection in Phase I Studies: Why We Should Always Go for the Top

(2008) Stefan Sleijfer et al.   JOURNAL OF CLINICAL ONCOLOGY

Dose- and Schedule-Dependent Inhibition of the Mammalian Target of Rapamycin Pathway With Everolimus: A Phase I Tumor Pharmacodynamic Study in Patients With Advanced Solid Tumors

(2008) Josep Tabernero et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase I Pharmacokinetic and Pharmacodynamic Study of the Oral Mammalian Target of Rapamycin Inhibitor Everolimus in Patients With Advanced Solid Tumors

(2008) Anne O'Donnell et al.   JOURNAL OF CLINICAL ONCOLOGY

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

(2008) Robert J Motzer et al.   LANCET

Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity

(2008) S.-M. Maira et al.   MOLECULAR CANCER THERAPEUTICS

The PTEN–PI3K pathway: of feedbacks and cross-talks

(2008) A Carracedo et al.   ONCOGENE

Drug discovery approaches targeting the PI3K/Akt pathway in cancer

(2008) C Garcia-Echeverria et al.   ONCOGENE