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.