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BAL101553

 
 
 
BAL101553 is a highly water soluble prodrug of the synthetic novel small molecule BAL27862, which arrests tumor cell proliferation and induces cell death in cancer cells through disruption of the microtubule network. Microtubules are a well-established target in oncology as they function as a cellular scaffold, essential for tumor cell division. BAL101553 can be administered orally and intravenously in the absence of solubilizing excipients associated with adverse effects. Recent data has shown that BAL101553 (BAL27862) treatment induces a unique microtubule phenotype and causes microtubule destabilization that is distinct from other anti-cancer agents that are also directed against the microtubule network. Activity has been shown against a broad range of tumor types, as well as in many tumor models known to be unresponsive to standard therapeutics, including marketed microtubule-targeting agents such as taxanes or Vinca alkaloids.
 

Ongoing clinical program

BAL101553 is currently in phase I clinical testing. The study is a phase I open-label dose-escalation study that investigates safety, tolerability and pharmacokinetics of intravenous BAL101553 to establish dose and administration schedule for phase II studies. It includes adult patients with advanced solid tumors who have failed standard therapy or for whom no effective standard therapy is available.

The need for novel drugs for the treatment of drug-resistant cancer

Despiteprogress in the development of agents with antitumor activity, cancer remains a significant challenge in healthcare. There is an increasing medical need for novel agents with new mechanisms of action that overcome drug resistance to cancer therapy. Moreover, due to limited water-solubility, most marketed microtubule-targeting agents are administered in the presence of solubilizing excipients which may cause unwanted side-effects (e.g. anaphylactoid reactions). The characteristics of BAL101553 address both of these issues in one unique molecule, with the aim to eradicate refractory tumors while maintaining patient’s quality of life.

 

 
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