Next Article in Journal
Medullary Thyroid Cancer and Pseudocirrhosis: Case Report and Literature Review
Previous Article in Journal
Fine-Needle Sspiration Biopsy versus Core-Needle Biopsy in Diagnosing Lung Cancer: A Systematic Review
 
 
Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
Journals
Current Oncology
Volume 19
Issue 1
10.3747/co.19.866
curroncol-logo
Submit to this Journal Review for this Journal Propose a Special Issue
► Article Menu

Article Menu

share Share announcement Help format_quote Cite question_answer Discuss in SciProfiles thumb_up
...
Endorse textsms
...
Comment
Current Oncology is published by MDPI from Volume 28 Issue 1 (2021). Previous articles were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence, and they are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Multimed Inc..
first_page
settings
Order Article Reprints
Font Type:
Arial Georgia Verdana
Font Size:
Aa Aa Aa
Line Spacing:
Column Width:
Background:
Article

Phase I Study of the Plk1 Inhibitor BI 2536 Administered Intravenously on Three Consecutive Days in Advanced Solid Tumours

by
A. Frost
1,
K. Mross
1,*,
S. Steinbild
1,
S. Hedbom
1,
C. Unger
1,
R. Kaiser
2,
D. Trommeshauser
2 and
G. Munzert
2
1
Klinik für Internistische Onkologie (KIO), Freiburg im Breisgau, Germany
2
Boehringer Ingelheim Pharma, Biberach an der Riss, Germany
*
Author to whom correspondence should be addressed.
Curr. Oncol. 2012, 19(1), 28-35; https://doi.org/10.3747/co.19.866
Submission received: 6 November 2011 / Revised: 4 December 2011 / Accepted: 2 January 2012 / Published: 1 February 2012

Abstract

Background: This open-label phase i study with an accelerated titration design was performed to determine the maximum tolerated dose of BI 2536, a potent, highly selective small-molecule polo-like kinase 1 (Plk1) inhibitor. Methods: Patients with advanced solid tumours received a single 60-minute intravenous infusion of BI 2536 (50–70 mg) on days 1–3 of each 21-day treatment course. Recipients without disease progression or untenable toxicity could receive additional treatment courses. The maximum tolerated dose was determined based on dose-limiting toxicities. Other assessments included safety, pharmacokinetic profile, and antitumour activity according to the Response Evaluation Criteria in Solid Tumors. Results: The study enrolled 21 patients. The maximum tolerated dose for BI 2536 was determined to be 60 mg for the study schedule. Dose-limiting toxicities included hematologic events, hypertension, elevated liver enzymes, and fatigue. The most frequently reported drug-related adverse events were mild-to-moderate fatigue, leukopenia, constipation, nausea, mucosal inflammation, anorexia, and alopecia. The pharmacokinetics of BI 2536 were linear within the dose range tested. Plasma concentration profiles exhibited multi-compartmental pharmacokinetic behaviour, with a terminal elimination half-life of 20–30 hours. Conclusions: In the present study, BI 2536 showed an acceptable safety profile warranting further investigation of Plk1 inhibitors in this patient population.
Keywords: polo-like kinase; Plk1 inhibitor; BI 2536; phase i; dose escalation; solid tumours polo-like kinase; Plk1 inhibitor; BI 2536; phase i; dose escalation; solid tumours

Share and Cite

MDPI and ACS Style

Frost, A.; Mross, K.; Steinbild, S.; Hedbom, S.; Unger, C.; Kaiser, R.; Trommeshauser, D.; Munzert, G. Phase I Study of the Plk1 Inhibitor BI 2536 Administered Intravenously on Three Consecutive Days in Advanced Solid Tumours. Curr. Oncol. 2012, 19, 28-35. https://doi.org/10.3747/co.19.866

AMA Style

Frost A, Mross K, Steinbild S, Hedbom S, Unger C, Kaiser R, Trommeshauser D, Munzert G. Phase I Study of the Plk1 Inhibitor BI 2536 Administered Intravenously on Three Consecutive Days in Advanced Solid Tumours. Current Oncology. 2012; 19(1):28-35. https://doi.org/10.3747/co.19.866

Chicago/Turabian Style

Frost, A., K. Mross, S. Steinbild, S. Hedbom, C. Unger, R. Kaiser, D. Trommeshauser, and G. Munzert. 2012. "Phase I Study of the Plk1 Inhibitor BI 2536 Administered Intravenously on Three Consecutive Days in Advanced Solid Tumours" Current Oncology 19, no. 1: 28-35. https://doi.org/10.3747/co.19.866

APA Style

Frost, A., Mross, K., Steinbild, S., Hedbom, S., Unger, C., Kaiser, R., Trommeshauser, D., & Munzert, G. (2012). Phase I Study of the Plk1 Inhibitor BI 2536 Administered Intravenously on Three Consecutive Days in Advanced Solid Tumours. Current Oncology, 19(1), 28-35. https://doi.org/10.3747/co.19.866

Article Metrics

Back to TopTop