Literature DB >> 14739661

Phase I trial of the polyamine analog N1,N14-diethylhomospermine (DEHSPM) in patients with advanced solid tumors.

George Wilding1, David King, Kendra Tutsch, Marcia Pomplun, Chris Feierabend, Dona Alberti, Rhoda Arzoomanian.   

Abstract

BACKGROUND: This phase I study was conducted to determine maximal tolerated dose (MTD) and dose-limiting toxicities (DLT) in patients with advanced solid tumors treated with the polyamine analog N1, N14-diethylhomospermine (DEHSPM).
METHODS: Patients were treated with DEHSPM administered as a subcutaneous (SC) injection daily for five consecutive days repeated every 4 weeks. Three dose levels were examined starting at 12.5 mg/m2/day, escalating to 37.5 mg/m2/day.
RESULTS: A total of 15 patients were enrolled. Dose limiting toxicities (grade 3 or 4) included nausea, vomiting, constipation, ileus, elevations of aspartate aminotransferase (AST) and alkaline phosphatase, hyperbilirubinemia, and ventricular bigeminy.
CONCLUSION: DEHSPM given as a SC injection is overall well tolerated at lower doses, but significant toxicities were observed at the 37.5mg/m2/day dose level. MTD was established at 25 mg/m2/day but further investigation with this study drug is not recommended secondary to the potential for neurotoxicities and hepatic damage as a result of cumulative doses.

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Year:  2004        PMID: 14739661     DOI: 10.1023/B:DRUG.0000011789.79368.ae

Source DB:  PubMed          Journal:  Invest New Drugs        ISSN: 0167-6997            Impact factor:   3.850


  34 in total

1.  Metabolically programmed polyamine analogue antidiarrheals.

Authors:  R J Bergeron; G W Yao; H Yao; W R Weimar; C A Sninsky; B Raisler; Y Feng; Q Wu; F Gao
Journal:  J Med Chem       Date:  1996-06-21       Impact factor: 7.446

Review 2.  Polyamines in rapid growth and cancer.

Authors:  J Jänne; H Pösö; A Raina
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3.  Correlations between polyamine analogue-induced increases in spermidine/spermine N1-acetyltransferase activity, polyamine pool depletion, and growth inhibition in human melanoma cell lines.

Authors:  C W Porter; B Ganis; P R Libby; R J Bergeron
Journal:  Cancer Res       Date:  1991-07-15       Impact factor: 12.701

4.  Polyamine analogue antidiarrheals: a structure-activity study.

Authors:  R J Bergeron; J Wiegand; J S McManis; W R Weimar; R E Smith; S E Algee; T L Fannin; M A Slusher; P S Snyder
Journal:  J Med Chem       Date:  2001-01-18       Impact factor: 7.446

5.  Phase I study of N(1),N(11)-diethylnorspermine in patients with non-small cell lung cancer.

Authors:  Hillary A Hahm; David S Ettinger; Kathy Bowling; Beth Hoker; Tian Ling Chen; Yelena Zabelina; Robert A Casero
Journal:  Clin Cancer Res       Date:  2002-03       Impact factor: 12.531

6.  Overexpression of ornithine decarboxylase enhances endothelial proliferation by suppressing endostatin expression.

Authors:  Takahiro Nemoto; Hisae Hori; Masataka Yoshimoto; Yousuke Seyama; Shunichiro Kubota
Journal:  Blood       Date:  2002-02-15       Impact factor: 22.113

7.  A randomized, placebo-controlled trial of low-dose alpha-difluoromethylornithine in individuals at risk for colorectal cancer.

Authors:  R R Love; R Jacoby; M A Newton; K D Tutsch; K Simon; M Pomplun; A K Verma
Journal:  Cancer Epidemiol Biomarkers Prev       Date:  1998-11       Impact factor: 4.254

8.  Role of the methylene backbone in the antiproliferative activity of polyamine analogues on L1210 cells.

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Journal:  Cancer Res       Date:  1989-06-01       Impact factor: 12.701

9.  Differential induction of spermidine/spermine N1-acetyltransferase activity in cisplatin-sensitive and -resistant ovarian cancer cells in response to N1,N12-bis(ethyl)spermine involves transcriptional and post-transcriptional regulation.

Authors:  G Marverti; S Bettuzzi; S Astancolle; C Pinna; M G Monti; M S Moruzzi
Journal:  Eur J Cancer       Date:  2001-01       Impact factor: 9.162

Review 10.  Polyamine metabolism and function.

Authors:  A E Pegg; P P McCann
Journal:  Am J Physiol       Date:  1982-11
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  5 in total

Review 1.  Recent advances in the development of polyamine analogues as antitumor agents.

Authors:  Robert A Casero; Patrick M Woster
Journal:  J Med Chem       Date:  2009-08-13       Impact factor: 7.446

2.  Herbacetin Is a Novel Allosteric Inhibitor of Ornithine Decarboxylase with Antitumor Activity.

Authors:  Dong Joon Kim; Eunmiri Roh; Mee-Hyun Lee; Naomi Oi; Do Young Lim; Myoung Ok Kim; Young-Yeon Cho; Angelo Pugliese; Jung-Hyun Shim; Hanyong Chen; Eun Jin Cho; Jong-Eun Kim; Sun Chul Kang; Souren Paul; Hee Eun Kang; Ji Won Jung; Sung-Young Lee; Sung-Hyun Kim; Kanamata Reddy; Young Il Yeom; Ann M Bode; Zigang Dong
Journal:  Cancer Res       Date:  2015-12-16       Impact factor: 12.701

3.  Polyamine analogues: potent inducers of nucleosomal array oligomerization and inhibitors of yeast cell growth.

Authors:  Lenny M Carruthers; Laurence J Marton; Craig L Peterson
Journal:  Biochem J       Date:  2007-08-01       Impact factor: 3.857

4.  Subcutaneous Toxicity of Agmatine in Rats.

Authors:  Tayfun Uzbay; Fatma Duygu Kaya Yertutanol; Ahmet Midi; Burcu Çevreli
Journal:  Turk J Pharm Sci       Date:  2017-08-15

Review 5.  Oil for the cancer engine: The cross-talk between oncogenic signaling and polyamine metabolism.

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Journal:  Sci Adv       Date:  2018-01-24       Impact factor: 14.136

  5 in total

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