Volasertib* and Polo-like kinase (Plk) Inhibitor Infographic

01.05.2011

Volasertib*, a Boehringer Ingelheim investigational compound, is a potential first-in-class selective cell cycle kinase inhibitor targeting Plk1.

How is Plk 1 involved in the cell cycle process?
Cell division is essential for many of the body's functions, including reproduction, growth and tissue repair.¹ Plk1 plays a role in several important steps during cell division, including the passage of cells through mitosis.^2,3

Mode of action of volasertib*
In cancer, over-expression of Plk1 is associated with aggressive tumour growth and a poor prognosis in many cancers.^4,5 Volasertib* is highly selective and works by inhibiting the activity of Plk1.⁶ Inhibition of Plk1 induces mitotic arrest (referred to as Polo Arrest) and apoptosis (cell death) in in-vivo tumour models, resulting in growth inhibition and tumour regression.^7,8

*Volasertib (compound code BI 6727) is an investigational compound. Its safety and efficacy has not yet been fully established.

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2. Schmit TL, Zhong W, Setaluri V, Spiegelman VS, Ahmad N. J Invest Dermatol. 2009;129(12):2843-2853.
3. Strebhardt K, Ullrich A. Tareting polo-like kinase 1 for cancer therapy. Nat Rev Cancer.2006;6(4):321-330.
4. Schöffski P. Polo-Like Kinase (PLK) Inhibitors in Preclinical and Early Clinical Development in Oncology. Oncologist. 2009;14(6):559-570.
5. Takai N, Hamanaka R, Yoshimatsu J, Miyakawa I. Oncogene. 2005;24(2):287-291.
6. Rudolph D, Steegmaier M, Hoffmann M, et al. Clin Cancer Res. 2009;15(9):3094-3102.
7. Liu X, Erikson RL.Polo-like kinase (Plk)1 depletion induces apoptosis in cancer cells. Proc Natl Acad Sci USA 2003;100: 5789-5794.
8. Lenart P, Petronczki M, Steegmaier M, et al. Curr Biol. 2007;17(4):304-315.