Phase II trial of RAD001 and bicalutamide for castration‐resistant prostate cancer

Study Type – Therapy (cohort)

[1]  C. Porta,et al.  Management of adverse events associated with the use of everolimus in patients with advanced renal cell carcinoma. , 2011, European journal of cancer.

[2]  S. Balk,et al.  Intratumoral androgen biosynthesis in prostate cancer pathogenesis and response to therapy. , 2011, Endocrine-related cancer.

[3]  H. Lane,et al.  mTOR Inhibitor RAD 001 ( Everolimus ) Has Antiangiogenic / Vascular Properties Distinct from a VEGFR Tyrosine Kinase Inhibitor , 2009 .

[4]  H. Lane,et al.  Increased AKT S473 phosphorylation after mTORC1 inhibition is rictor dependent and does not predict tumor cell response to PI3K/mTOR inhibition , 2009, Molecular Cancer Therapeutics.

[5]  W. Friedrichs,et al.  Reduced PTEN expression in breast cancer cells confers susceptibility to inhibitors of the PI3 kinase/Akt pathway. , 2004, Annals of oncology : official journal of the European Society for Medical Oncology.

[6]  H. Lane,et al.  Increased AKT S 473 phosphorylation after mTORC 1 inhibition is rictor dependent and does not predict tumor cell response to PI 3 K / mTOR inhibition , 2009 .

[7]  L. Cantley,et al.  Targeting the PI3K-Akt pathway in human cancer: rationale and promise. , 2003, Cancer cell.

[8]  D. Guertin,et al.  Phosphorylation and Regulation of Akt/PKB by the Rictor-mTOR Complex , 2005, Science.

[9]  P. Kantoff,et al.  Secondary hormonal therapy in men with castration-resistant prostate cancer. , 2011, Clinical genitourinary cancer.

[10]  P. Nelson,et al.  Maintenance of intratumoral androgens in metastatic prostate cancer: a mechanism for castration-resistant tumor growth. , 2008, Cancer research.

[11]  P. Pandolfi,et al.  Inhibition of mTORC1 leads to MAPK pathway activation through a PI3K-dependent feedback loop in human cancer. , 2008, The Journal of clinical investigation.

[12]  J. Blenis,et al.  Mammalian cell size is controlled by mTOR and its downstream targets S6K1 and 4EBP1/eIF4E. , 2002, Genes & development.

[13]  W. K. Alfred Yung,et al.  Identification of a candidate tumour suppressor gene, MMAC1, at chromosome 10q23.3 that is mutated in multiple advanced cancers , 1997, Nature Genetics.

[14]  W. Friedrichs,et al.  Inhibitors of mTOR reverse doxorubicin resistance conferred by PTEN status in prostate cancer cells. , 2002, Cancer research.

[15]  G. Bubley,et al.  High dose bicalutamide for androgen independent prostate cancer: effect of prior hormonal therapy. , 1998, The Journal of urology.

[16]  P. Kantoff,et al.  Androgen receptor mutations in androgen-independent prostate cancer: Cancer and Leukemia Group B Study 9663. , 2003, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[17]  L. Schwartz,et al.  Bicalutamide for advanced prostate cancer: the natural versus treated history of disease. , 1997, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[18]  M Van Glabbeke,et al.  New guidelines to evaluate the response to treatment in solid tumors. European Organization for Research and Treatment of Cancer, National Cancer Institute of the United States, National Cancer Institute of Canada. , 2000, Journal of the National Cancer Institute.

[19]  A. De Benedetti,et al.  Post-transcriptional regulation of the androgen receptor by Mammalian target of rapamycin. , 2005, Cancer research.

[20]  C. Porta,et al.  Effi cacy of everolimus in advanced renal cell carcinoma : a double-blind , randomised , placebo-controlled phase III trial , 2008 .

[21]  H. Lane,et al.  mTOR Inhibitor RAD001 (Everolimus) Has Antiangiogenic/Vascular Properties Distinct from a VEGFR Tyrosine Kinase Inhibitor , 2009, Clinical Cancer Research.

[22]  L. Cantley,et al.  Ras, PI(3)K and mTOR signalling controls tumour cell growth , 2006, Nature.

[23]  C. Moinpour,et al.  Phase II trial of bicalutamide in patients with advanced prostate cancer in whom conventional hormonal therapy failed: a Southwest Oncology Group study (SWOG 9235). , 2001, Urology.

[24]  T. Golub,et al.  mTOR inhibition reverses Akt-dependent prostate intraepithelial neoplasia through regulation of apoptotic and HIF-1-dependent pathways , 2004, Nature Medicine.

[25]  Gordon B Mills,et al.  mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates Akt. , 2006, Cancer research.

[26]  L. Morel,et al.  Androgen receptor expression is regulated by the phosphoinositide 3-kinase/Akt pathway in normal and tumoral epithelial cells. , 2002, The Biochemical journal.

[27]  Hong Wu,et al.  Enhanced sensitivity of PTEN-deficient tumors to inhibition of FRAP/mTOR , 2001, Proceedings of the National Academy of Sciences of the United States of America.

[28]  R. Vessella,et al.  Molecular determinants of resistance to antiandrogen therapy , 2004, Nature Medicine.

[29]  Sarat Chandarlapaty,et al.  Reciprocal feedback regulation of PI3K and androgen receptor signaling in PTEN-deficient prostate cancer. , 2011, Cancer cell.

[30]  M. Taplin Drug Insight: role of the androgen receptor in the development and progression of prostate cancer , 2007, Nature Clinical Practice Oncology.

[31]  David M Sabatini,et al.  Defining the role of mTOR in cancer. , 2007, Cancer cell.

[32]  P. Nelson,et al.  Intratumoral de novo steroid synthesis activates androgen receptor in castration-resistant prostate cancer and is upregulated by treatment with CYP17A1 inhibitors. , 2011, Cancer research.

[33]  M. Broggini,et al.  Combination of PI3K/mTOR inhibitors: antitumor activity and molecular correlates. , 2011, Cancer research.

[34]  E. Small,et al.  Selection for androgen receptor mutations in prostate cancers treated with androgen antagonist. , 1999, Cancer research.

[35]  M. Wigler,et al.  PTEN, a Putative Protein Tyrosine Phosphatase Gene Mutated in Human Brain, Breast, and Prostate Cancer , 1997, Science.

[36]  Kenneth N Ross,et al.  Androgens induce prostate cancer cell proliferation through mammalian target of rapamycin activation and post-transcriptional increases in cyclin D proteins. , 2006, Cancer research.

[37]  M. Hall,et al.  Rapamycin passes the torch: a new generation of mTOR inhibitors , 2011, Nature Reviews Drug Discovery.

[38]  R. Motzer,et al.  Efficacy of everolimus in advanced renal cell carcinoma: a double-blind, randomised, placebo-controlled phase III trial , 2008, The Lancet.

[39]  T. Golub,et al.  Increased expression of genes converting adrenal androgens to testosterone in androgen-independent prostate cancer. , 2006, Cancer research.

[40]  L. Cantley,et al.  New insights into tumor suppression: PTEN suppresses tumor formation by restraining the phosphoinositide 3-kinase/AKT pathway. , 1999, Proceedings of the National Academy of Sciences of the United States of America.

[41]  Norbert Hollaender,et al.  Phase 3 trial of everolimus for metastatic renal cell carcinoma , 2010, Cancer.

[42]  D. Tindall,et al.  The role of PTEN in the progression and survival of prostate cancer. , 2003, Minerva endocrinologica.

[43]  V. Njar,et al.  Prolonging hormone sensitivity in prostate cancer xenografts through dual inhibition of AR and mTOR , 2010, British Journal of Cancer.

[44]  P. Majumder,et al.  Inhibition of tumor growth progression by antiandrogens and mTOR inhibitor in a Pten-deficient mouse model of prostate cancer. , 2009, Cancer research.

[45]  C. Sander,et al.  Integrative genomic profiling of human prostate cancer. , 2010, Cancer cell.

[46]  Suzanne F. Jones,et al.  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, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[47]  G. Bubley,et al.  Mutation of the androgen-receptor gene in metastatic androgen-independent prostate cancer. , 1995, The New England journal of medicine.

[48]  Susan Halabi,et al.  Design and end points of clinical trials for patients with progressive prostate cancer and castrate levels of testosterone: recommendations of the Prostate Cancer Clinical Trials Working Group. , 2008, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[49]  J. Blenis,et al.  An inhibitor of mTOR reduces neoplasia and normalizes p70/S6 kinase activity in Pten+/− mice , 2001, Proceedings of the National Academy of Sciences of the United States of America.

[50]  M. van Glabbeke,et al.  New guidelines to evaluate the response to treatment in solid tumors , 2000, Journal of the National Cancer Institute.

[51]  M. Bjornsti,et al.  The tor pathway: a target for cancer therapy , 2004, Nature Reviews Cancer.

[52]  David McDermott,et al.  Temsirolimus, interferon alfa, or both for advanced renal-cell carcinoma. , 2007, The New England journal of medicine.

[53]  B. Weigelt,et al.  PIK3CA mutation, but not PTEN loss of function, determines the sensitivity of breast cancer cells to mTOR inhibitory drugs , 2011, Oncogene.

[54]  D. Guertin,et al.  Rictor, a Novel Binding Partner of mTOR, Defines a Rapamycin-Insensitive and Raptor-Independent Pathway that Regulates the Cytoskeleton , 2004, Current Biology.

[55]  Y. Wang,et al.  Regulation of androgen receptor transcriptional activity by rapamycin in prostate cancer cell proliferation and survival , 2008, Oncogene.