Lexibulin is a small-molecule tubulin-depolymerizing agent that is being developed by
YM BioSciences
as a
vascular-disrupting agent (VDA) for the potential treatment of cancer. In vitro cell culture and in v
ivo tumor
models established that lexibulin has vascular-disrupting activity. Lexibulin is currently undergoing
clinical
development and can be administered either intravenously or orally. In two phase I clinical trials in
patients
with solid tumors, lexibulin induced changes in tumors that were consistent with vascular disruption
and
associated blood-flow modifications. Pharmacokinetics of lexibulin were favorable and generally dose-
linear
for both the oral and intravenous formulations. The side-effect profile of lexibulin was similar to t
hat of other
VDAs and included cardiovascular, respiratory and hematological toxicities. Lexibulin was also to be
assessed
in a phase Ib/II trial in combination with
carboplatin
in patients with relapsed glioblastoma multiforme and
a phase II trial as monotherapy in patients with multiple myeloma. However, both trials were terminat
ed,
although preliminary efficacy results are available for the combination trial. At the time of publica
tion,
lexibulin remained listed as being in phase II development on
YM BioSciences
' pipeline.
CORE (COnnecting REpositories)
CORE (COnnecting REpositories)