Literature DB >> 24393852

Randomized phase II trial of the cyclin-dependent kinase inhibitor dinaciclib (MK-7965) versus capecitabine in patients with advanced breast cancer.

Monica M Mita1, Anil A Joy2, Alain Mita3, Kamalesh Sankhala3, Ying-Ming Jou4, Da Zhang4, Paul Statkevich4, Yali Zhu4, Siu-Long Yao4, Karen Small4, Rajat Bannerji4, Charles L Shapiro5.   

Abstract

INTRODUCTION: Effective therapies after failure of treatment with anthracyclines and taxanes are needed for patients with metastatic breast cancer. Dinaciclib (MK-7965, formerly SCH727965), a small-molecule cyclin-dependent kinase inhibitor, has demonstrated antitumor activity in phase I studies with solid-tumor patients. This phase II trial was designed to assess the efficacy and safety of dinaciclib compared with that of capecitabine in women with previously treated advanced breast cancer. PATIENTS AND METHODS: Patients were randomized to receive either dinaciclib at 50 mg/m(2), administered as a 2-hour infusion every 21 days, or 1250 mg/m(2) capecitabine, administered orally twice daily in 21-day cycles.
RESULTS: An unplanned interim analysis showed that the time to disease progression was inferior with dinaciclib treatment compared with capecitabine treatment; therefore, the trial was stopped after 30 patients were randomized. Dinaciclib treatment demonstrated antitumor activity in 2 of 7 patients with estrogen receptor-positive and human epidermal growth factor receptor 2-negative metastatic breast cancer (1 confirmed and 1 unconfirmed partial response), as well as acceptable safety and tolerability. Grade 3 or 4 treatment-related adverse events were common and included neutropenia, leukopenia, increase in aspartate aminotransferase, and febrile neutropenia. Population pharmacokinetic model-predicted mean dinaciclib exposure (area under the concentration-time curve extrapolated to infinity [AUC[I]]) at 50 mg/m(2) was similar to that observed in a previous phase I trial, and no drug accumulation was observed after multiple-dose administration.
CONCLUSION: Although dinaciclib monotherapy demonstrated some antitumor activity and was generally tolerated, efficacy was not superior to capecitabine. Future studies may be considered to evaluate dinaciclib in select patient populations with metastatic breast cancer and in combination with other agents.
Copyright © 2014 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Efficacy; Monotherapy; Safety; Small-molecule inhibitor; Solid tumors

Mesh:

Substances:

Year:  2013        PMID: 24393852     DOI: 10.1016/j.clbc.2013.10.016

Source DB:  PubMed          Journal:  Clin Breast Cancer        ISSN: 1526-8209            Impact factor:   3.225


  58 in total

1.  Inhibition of CDK2 reduces EZH2 phosphorylation and reactivates ERα expression in high-grade serous ovarian carcinoma.

Authors:  Ye Han; Yongkun Wei; Jun Yao; Yu-Yi Chu; Chia-Wei Li; Jennifer L Hsu; Lei Nie; Mien-Chie Hung
Journal:  Am J Cancer Res       Date:  2020-04-01       Impact factor: 6.166

Review 2.  The history and future of targeting cyclin-dependent kinases in cancer therapy.

Authors:  Uzma Asghar; Agnieszka K Witkiewicz; Nicholas C Turner; Erik S Knudsen
Journal:  Nat Rev Drug Discov       Date:  2015-02       Impact factor: 84.694

Review 3.  Synthetic Lethality through the Lens of Medicinal Chemistry.

Authors:  Samuel H Myers; Jose Antonio Ortega; Andrea Cavalli
Journal:  J Med Chem       Date:  2020-11-02       Impact factor: 7.446

4.  CDK12 Inhibition Reverses De Novo and Acquired PARP Inhibitor Resistance in BRCA Wild-Type and Mutated Models of Triple-Negative Breast Cancer.

Authors:  Shawn F Johnson; Cristina Cruz; Ann Katrin Greifenberg; Sofia Dust; Daniel G Stover; David Chi; Benjamin Primack; Shiliang Cao; Andrea J Bernhardy; Rhiannon Coulson; Jean-Bernard Lazaro; Bose Kochupurakkal; Heather Sun; Christine Unitt; Lisa A Moreau; Kristopher A Sarosiek; Maurizio Scaltriti; Dejan Juric; José Baselga; Andrea L Richardson; Scott J Rodig; Alan D D'Andrea; Judith Balmaña; Neil Johnson; Matthias Geyer; Violeta Serra; Elgene Lim; Geoffrey I Shapiro
Journal:  Cell Rep       Date:  2016-11-22       Impact factor: 9.423

Review 5.  A comparison of toxicity profiles between the lower and standard dose capecitabine in breast cancer: a systematic review and meta-analysis.

Authors:  Tomohiro F Nishijima; Maya Suzuki; Hyman B Muss
Journal:  Breast Cancer Res Treat       Date:  2016-03-17       Impact factor: 4.872

6.  A phase 1 study with dose expansion of the CDK inhibitor dinaciclib (SCH 727965) in combination with epirubicin in patients with metastatic triple negative breast cancer.

Authors:  Zahi Mitri; Cansu Karakas; Caimiao Wei; Brian Briones; Holly Simmons; Nuhad Ibrahim; Ricardo Alvarez; James L Murray; Khandan Keyomarsi; Stacy Moulder
Journal:  Invest New Drugs       Date:  2015-05-07       Impact factor: 3.850

Review 7.  Ribociclib (LEE011): Mechanism of Action and Clinical Impact of This Selective Cyclin-Dependent Kinase 4/6 Inhibitor in Various Solid Tumors.

Authors:  Debu Tripathy; Aditya Bardia; William R Sellers
Journal:  Clin Cancer Res       Date:  2017-03-28       Impact factor: 12.531

Review 8.  Inhibiting CDK in Cancer Therapy: Current Evidence and Future Directions.

Authors:  Smruthi Vijayaraghavan; Stacy Moulder; Khandan Keyomarsi; Rachel M Layman
Journal:  Target Oncol       Date:  2018-02       Impact factor: 4.493

9.  Dinaciclib prolongs survival in the LSL-KrasG12D/+ ; LSL-Trp53R172H/+ ; Pdx-1-Cre (KPC) transgenic murine models of pancreatic ductal adenocarcinoma.

Authors:  Jia Yang; Su Hu; Junjie Shangguan; Aydin Eresen; Yu Li; Quanhong Ma; Vahid Yaghmai; Al B Benson Iii; Zhuoli Zhang
Journal:  Am J Transl Res       Date:  2020-03-15       Impact factor: 4.060

10.  Mitochondrial dysfunction RAD51, and Ku80 proteolysis promote apoptotic effects of Dinaciclib in Bcl-xL silenced cells.

Authors:  Daniel R Premkumar; Esther P Jane; Swetha Thambireddy; Philip A Sutera; Jonathon M Cavaleri; Ian F Pollack
Journal:  Mol Carcinog       Date:  2017-12-30       Impact factor: 4.784

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