Literature DB >> 23589525

Efatutazone, an oral PPAR-γ agonist, in combination with paclitaxel in anaplastic thyroid cancer: results of a multicenter phase 1 trial.

R C Smallridge1, J A Copland, M S Brose, J T Wadsworth, Y Houvras, M E Menefee, K C Bible, M H Shah, A W Gramza, J P Klopper, L A Marlow, M G Heckman, R Von Roemeling.   

Abstract

PURPOSE: A phase 1 study was initiated to determine the safety, potential effectiveness, and maximal tolerated dose and recommended phase 2 dose of efatutazone and paclitaxel in anaplastic thyroid cancer. EXPERIMENTAL
DESIGN: Patients received efatutazone (0.15, 0.3, or 0.5 mg) orally twice daily and then paclitaxel every 3 weeks. Patient tolerance and outcomes were assessed, as were serum efatutazone pharmacokinetics.
RESULTS: Ten of 15 patients were women. Median age was 59 years. Seven patients received 0.15 mg of efatutazone, 6 patients received 0.3 mg, and 2 patients received 0.5 mg. One patient receiving 0.3 mg of efatutazone had a partial response from day 69 to day 175; 7 patients attained stable disease. Median times to progression were 48 and 68 days in patients receiving 0.15 mg of efatutazone and 0.3 mg of efatutazone, respectively; corresponding median survival was 98 vs 138 days. The median peak efatutazone blood level was 8.6 ng/mL for 0.15-mg dosing vs 22.0 ng/mL for 0.3-mg twice daily dosing. Ten patients had grade 3 or greater adverse events (Common Terminology Criteria for Adverse Events), with 2 of these (anemia and edema) related to efatutazone. Thirteen events of edema were reported in 8 patients, with 2 of grade 3 or greater. Eight patients had ≥1 serious adverse event, with 1 of these (anemia) attributed to efatutazone and 1 (anaphylactic reaction) related to paclitaxel. The maximal tolerated dose was not achieved. Angiopoietin-like 4 was induced by efatutazone in tissue biopsy samples of 2 patients.
CONCLUSIONS: Efatutazone and paclitaxel in combination were safe and tolerated and had biologic activity.

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Year:  2013        PMID: 23589525      PMCID: PMC3667260          DOI: 10.1210/jc.2013-1106

Source DB:  PubMed          Journal:  J Clin Endocrinol Metab        ISSN: 0021-972X            Impact factor:   5.958


  21 in total

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Journal:  World J Surg       Date:  1999-09       Impact factor: 3.352

2.  Treatment of anaplastic thyroid carcinoma with paclitaxel: phase 2 trial using ninety-six-hour infusion. Collaborative Anaplastic Thyroid Cancer Health Intervention Trials (CATCHIT) Group.

Authors:  K B Ain; M J Egorin; P A DeSimone
Journal:  Thyroid       Date:  2000-07       Impact factor: 6.568

3.  Anaplastic carcinoma of the thyroid. A clinicopathologic study of 121 cases.

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Journal:  Cancer       Date:  1990-07-15       Impact factor: 6.860

Review 4.  Anaplastic thyroid carcinoma: pathogenesis and emerging therapies.

Authors:  R C Smallridge; J A Copland
Journal:  Clin Oncol (R Coll Radiol)       Date:  2010-04-24       Impact factor: 4.126

Review 5.  Peroxisome proliferator-activated receptor-gamma ligands as cell-cycle modulators.

Authors:  Stamos Theocharis; Alexandra Margeli; Philippe Vielh; Gregory Kouraklis
Journal:  Cancer Treat Rev       Date:  2004-10       Impact factor: 12.111

6.  Oncocytic, focally anaplastic, thyroid cancer responding to erlotinib.

Authors:  Thomas Hogan; H James Williams; Ramin Altaha
Journal:  J Oncol Pharm Pract       Date:  2009-03-10       Impact factor: 1.809

7.  A phase II trial of fosbretabulin in advanced anaplastic thyroid carcinoma and correlation of baseline serum-soluble intracellular adhesion molecule-1 with outcome.

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Journal:  Thyroid       Date:  2009-03       Impact factor: 6.568

Review 8.  Antineoplastic effects of peroxisome proliferator-activated receptor gamma agonists.

Authors:  Christian Grommes; Gary E Landreth; Michael T Heneka
Journal:  Lancet Oncol       Date:  2004-07       Impact factor: 41.316

9.  Anti-tumour activity of CS-7017, a selective peroxisome proliferator-activated receptor gamma agonist of thiazolidinedione class, in human tumour xenografts and a syngeneic tumour implant model.

Authors:  Naomi Shimazaki; Noriko Togashi; Masaharu Hanai; Takeshi Isoyama; Kunio Wada; Takashi Fujita; Kosaku Fujiwara; Shinichi Kurakata
Journal:  Eur J Cancer       Date:  2008-05-27       Impact factor: 9.162

10.  PPARγ Promotes Growth and Invasion of Thyroid Cancer Cells.

Authors:  William M Wood; Vibha Sharma; Kevin T Bauerle; Laura A Pike; Qiong Zhou; Deborah L Fretwell; Rebecca E Schweppe; Bryan R Haugen
Journal:  PPAR Res       Date:  2011-12-12       Impact factor: 4.964

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  35 in total

Review 1.  Exploration and Development of PPAR Modulators in Health and Disease: An Update of Clinical Evidence.

Authors:  Hong Sheng Cheng; Wei Ren Tan; Zun Siong Low; Charlie Marvalim; Justin Yin Hao Lee; Nguan Soon Tan
Journal:  Int J Mol Sci       Date:  2019-10-11       Impact factor: 5.923

Review 2.  Anaplastic thyroid carcinoma: from clinicopathology to genetics and advanced therapies.

Authors:  Eleonora Molinaro; Cristina Romei; Agnese Biagini; Elena Sabini; Laura Agate; Salvatore Mazzeo; Gabriele Materazzi; Stefano Sellari-Franceschini; Alessandro Ribechini; Liborio Torregrossa; Fulvio Basolo; Paolo Vitti; Rossella Elisei
Journal:  Nat Rev Endocrinol       Date:  2017-07-14       Impact factor: 43.330

Review 3.  Evolving molecularly targeted therapies for advanced-stage thyroid cancers.

Authors:  Keith C Bible; Mabel Ryder
Journal:  Nat Rev Clin Oncol       Date:  2016-03-01       Impact factor: 66.675

4.  Cell Cycle M-Phase Genes Are Highly Upregulated in Anaplastic Thyroid Carcinoma.

Authors:  Paul Weinberger; Sithara Raju Ponny; Hongyan Xu; Shan Bai; Robert Smallridge; John Copland; Ashok Sharma
Journal:  Thyroid       Date:  2016-12-15       Impact factor: 6.568

Review 5.  Peroxisome proliferator-activated receptor gamma and BRCA1.

Authors:  Priscilla A Furth
Journal:  Endocr Relat Cancer       Date:  2019-02       Impact factor: 5.678

6.  Peroxisome proliferator-activated receptor-γ agonist troglitazone suppresses transforming growth factor-β1 signalling through miR-92b upregulation-inhibited Axl expression in human keloid fibroblasts in vitro.

Authors:  Hua-Yu Zhu; Wen-Dong Bai; Jun Li; Ke Tao; Hong-Tao Wang; Xue-Kang Yang; Jia-Qi Liu; Yun-Chuan Wang; Ting He; Song-Tao Xie; Da-Hai Hu
Journal:  Am J Transl Res       Date:  2016-08-15       Impact factor: 4.060

Review 7.  Novel treatments for anaplastic thyroid carcinoma.

Authors:  Silvia Martina Ferrari; Giusy Elia; Francesca Ragusa; Ilaria Ruffilli; Concettina La Motta; Sabrina Rosaria Paparo; Armando Patrizio; Roberto Vita; Salvatore Benvenga; Gabriele Materazzi; Poupak Fallahi; Alessandro Antonelli
Journal:  Gland Surg       Date:  2020-01

8.  miR30a inhibits LOX expression and anaplastic thyroid cancer progression.

Authors:  Myriem Boufraqech; Naris Nilubol; Lisa Zhang; Sudheer Kumar Gara; Samira M Sadowski; Amit Mehta; Mei He; Sean Davis; Jennifer Dreiling; John A Copland; Robert C Smallridge; Martha M Quezado; Electron Kebebew
Journal:  Cancer Res       Date:  2014-12-08       Impact factor: 12.701

Review 9.  Update: the status of clinical trials with kinase inhibitors in thyroid cancer.

Authors:  Samuel A Wells; Massimo Santoro
Journal:  J Clin Endocrinol Metab       Date:  2014-01-13       Impact factor: 5.958

Review 10.  Targeting lipid metabolism for the treatment of anaplastic thyroid carcinoma.

Authors:  Christina A von Roemeling; John A Copland
Journal:  Expert Opin Ther Targets       Date:  2015-09-28       Impact factor: 6.902

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