Literature DB >> 19844661

Phase II trial of pyrazoloacridine (NSC#366140) in patients with metastatic breast cancer.

Bhuvaneswari Ramaswamy1, Ewa Mrozek, John Philip Kuebler, Tanios Bekaii-Saab, Eric H Kraut.   

Abstract

PURPOSE: Pyrazoloacridine (PZA) is an investigational nucleic acid binding agent that inhibits the activity of topoisomerases 1 and 2. We conducted a phase II clinical study to determine the efficacy and toxicities of PZA in patients with metastatic breast cancer (MBC). EXPERIMENTAL
DESIGN: In this phase II multicenter study, patients who were treated with no more than one prior chemotherapy for MBC were treated with 750 mg/m² of PZA given as a 3-hour intravenous infusion every 3 weeks. Treatment cycles were continued until disease progression or unacceptable toxicities. The study was designed to distinguish between a response rate of < 15% vs > 30% (alpha = 0.10, beta = 0.10) using Simons optimal 2-stage design. At least 2 responses were required in the first 12 patients in the 1st stage and 6 of 35 in the 2nd stage to recommend the agent for further study.
RESULTS: Two patients in the first stage had a response allowing accrual to second stage. A total of 15 patients (out of 35 planned) were treated on the study prior to premature closure. Three patients had a partial response (20%) lasting 4.5-6 months. Two patients had stable disease for 3 and 5 months. The dose limiting toxicity was granulocytopenia with ten patients requiring dose reduction or dose delay for grade 4 neutropenia. Other grade 3 and 4 toxicities include vomiting (n = 2), nausea (n = 2), neurotoxicity (n = 1), fatigue (n = 1), anemia (n = 1), dyspnea 9n = 1) and renal (n = 1).
CONCLUSIONS: Pyrazoloacridine demonstrated modest activity in patients with metastatic breast cancer.

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Year:  2009        PMID: 19844661      PMCID: PMC3486428          DOI: 10.1007/s10637-009-9338-1

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


  19 in total

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Authors:  R C Jackson; J S Sebolt; J L Shillis; W R Leopold
Journal:  Cancer Invest       Date:  1990       Impact factor: 2.176

2.  Phase II study of pyrazoloacridine in patients with advanced colorectal carcinoma.

Authors:  M M Zalupski; P A Philip; P LoRusso; A F Shields
Journal:  Cancer Chemother Pharmacol       Date:  1997       Impact factor: 3.333

3.  Phase II trial of pyrazoloacridine in patients with cisplatin-refractory germ cell tumors.

Authors:  J Vuky; J McCaffrey; M Ginsberg; T Mariani; D F Bajorin; G J Bosl; R J Motzer
Journal:  Invest New Drugs       Date:  2000-08       Impact factor: 3.850

4.  Phase II trial of pyrazoloacridine as second-line therapy for patients with unresectable or metastatic transitional cell carcinoma.

Authors:  P M Dodd; J A McCaffrey; M Mazumdar; E Icasiano; G Higgins; H Herr; D F Bajorin
Journal:  Invest New Drugs       Date:  2000-08       Impact factor: 3.850

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Journal:  Clin Cancer Res       Date:  1998-03       Impact factor: 12.531

6.  Cytotoxicity and DNA damage associated with pyrazoloacridine in MCF-7 breast cancer cells.

Authors:  J L Grem; P M Politi; S L Berg; N M Benchekroun; M Patel; F M Balis; B K Sinha; W Dahut; C J Allegra
Journal:  Biochem Pharmacol       Date:  1996-06-28       Impact factor: 5.858

7.  Activity of the pyrazoloacridines against multidrug-resistant tumor cells.

Authors:  J Sebolt; M Havlick; K Hamelehle; J Nelson; W Leopold; R Jackson
Journal:  Cancer Chemother Pharmacol       Date:  1989       Impact factor: 3.333

8.  Pyrazoloacridine for the treatment of hormone-refractory prostate cancer.

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Journal:  Cancer Invest       Date:  1998       Impact factor: 2.176

9.  Phase I clinical trial of pyrazoloacridine NSC366140 (PD115934).

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Journal:  Clin Cancer Res       Date:  1995-12       Impact factor: 12.531

10.  Phase I and pharmacologic studies of pyrazoloacridine, a novel DNA intercalating agent, on single-dosing and multiple-dosing schedules.

Authors:  E K Rowinsky; D A Noe; L B Grochow; S E Sartorious; M K Bowling; T L Chen; B G Lubejko; S H Kaufmann; R C Donehower
Journal:  J Clin Oncol       Date:  1995-08       Impact factor: 44.544

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  5 in total

1.  Synthesis and Evaluation of New Pyrazoline Derivatives as Potential Anticancer Agents in HepG-2 Cell Line.

Authors:  Weijie Xu; Ying Pan; Hong Wang; Haiyan Li; Qing Peng; Duncan Wei; Cheng Chen; Jinhong Zheng
Journal:  Molecules       Date:  2017-03-16       Impact factor: 4.411

2.  CCNA2 as an Immunological Biomarker Encompassing Tumor Microenvironment and Therapeutic Response in Multiple Cancer Types.

Authors:  Aimin Jiang; Ye Zhou; Wenliang Gong; Xin Pan; Xinxin Gan; Zhenjie Wu; Bing Liu; Le Qu; Linhui Wang
Journal:  Oxid Med Cell Longev       Date:  2022-03-31       Impact factor: 6.543

3.  A New Series of Cytotoxic Pyrazoline Derivatives as Potential Anticancer Agents that Induce Cell Cycle Arrest and Apoptosis.

Authors:  Hong Wang; Jinhong Zheng; Weijie Xu; Cheng Chen; Duncan Wei; Wenxiu Ni; Ying Pan
Journal:  Molecules       Date:  2017-09-29       Impact factor: 4.411

4.  The Aza-Analogous Benzo[c]phenanthridine P8-D6 Acts as a Dual Topoisomerase I and II Poison, thus Exhibiting Potent Genotoxic Properties.

Authors:  Georg Aichinger; Falk-Bach Lichtenberger; Tamara N Steinhauer; Inken Flörkemeier; Giorgia Del Favero; Bernd Clement; Doris Marko
Journal:  Molecules       Date:  2020-03-27       Impact factor: 4.411

5.  Synthesis, Biological Evaluation and Stability Studies of Some Novel Aza-Acridine Aminoderivatives.

Authors:  Maria Karelou; Vasileios Kourafalos; Athanasia P Tragomalou; Panagiotis Marakos; Nicole Pouli; Ourania E Tsitsilonis; Evangelos Gikas; Ioannis K Kostakis
Journal:  Molecules       Date:  2020-10-08       Impact factor: 4.411

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