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Spotlight on Volasertib: Preclinical and Clinical Evaluation of a Promising Plk1 Inhibitor
J Van den Bossche1, F Lardon1, V Deschoolmeester1,2
1Center for Oncological Research (CORE) Antwerp, University of Antwerp, Antwerp, Belgium.
Abstract:
Considering the important side effects of conventional microtubule targeting agents, more and more research focuses on regulatory proteins for the development of mitosis-specific agents. Polo-like kinase 1 (Plk1), a master regulator of several cell cycle events, has arisen as an intriguing target in this research field. The observed overexpression of Plk1 in a broad range of human malignancies has given rise to the development of several potent and specific small molecule inhibitors targeting the kinase. In this review, we focus on volasertib (BI6727), the lead agent in category of Plk1 inhibitors at the moment. Numerous preclinical experiments have demonstrated that BI6727 is highly active across a variety of carcinoma cell lines, and the inhibitor has been reported to induce tumor regression in several xenograft models. Moreover, volasertib has shown clinical efficacy in multiple tumor types. As a result, Food and Drug Administration (FDA) has recently awarded volasertib the Breakthrough Therapy status after significant benefit was observed in acute myeloid leukemia (AML) patients treated with the Plk1 inhibitor. Here, we discuss both preclinical and clinical data available for volasertib administered as monotherapy or in combination with other anticancer therapies in a broad range of tumor types.
Insights
Volasertib (BI6727), a Polo-like kinase 1 (Plk1) inhibitor, shows promise as a mitosis-specific cancer therapy. It demonstrates efficacy in preclinical models and clinical trials, including for acute myeloid leukemia (AML).
Area of Science:
- Oncology
- Cell Biology
- Pharmacology
Background:
- Conventional microtubule targeting agents have significant side effects.
- Polo-like kinase 1 (Plk1) is a key regulator of cell division and is overexpressed in many cancers.
- Targeting Plk1 offers a strategy for developing mitosis-specific anti-cancer agents.
Purpose of the Study:
- To review preclinical and clinical data for volasertib (BI6727), a Plk1 inhibitor.
- To assess volasertib's efficacy as monotherapy and in combination treatments.
- To highlight volasertib's potential in various tumor types.
Main Methods:
- Review of preclinical studies evaluating volasertib's activity in cancer cell lines and xenograft models.
- Analysis of clinical trial data for volasertib in different cancer types.
- Examination of volasertib's safety and efficacy profiles.
Main Results:
- Volasertib (BI6727) exhibits high activity against various carcinoma cell lines.
- The inhibitor has shown tumor regression in preclinical xenograft models.
- Clinical studies indicate volasertib's efficacy across multiple tumor types, including AML, leading to FDA Breakthrough Therapy status.
Conclusions:
- Volasertib is a potent Plk1 inhibitor with demonstrated preclinical and clinical anti-cancer activity.
- Its efficacy in combination with other therapies warrants further investigation.
- Volasertib represents a promising novel therapeutic strategy for various malignancies.
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