C1311 is the lead compound from the imidazoacridinones, a novel group of rationally designed anti-
cancer agents. The compound is pharmaceutically formulated as a lyophilized product containing 100 mg
C1311 (anhydrous free base) per dosage unit and requires reconstitution before
intravenous administration. The aim of this study was to determine the stability of
C1311 in the reconstituted
solution and infusion
solution and its compatibility with infusion devices. Moreover, the
buffer capacity and haemolytic potential of
C1311 infusion solutions, which exhibit a relatively low pH of 2-3, were evaluated in vitro.
C1311 was shown to be stable in the reconstituted
solution for at least 48 h and for at least 96 h after subsequent dilution in 0.9%
sodium chloride and 5%
dextrose. In vitro infusion simulation studies showed
C1311 infusion solutions to be compatible with a
low-density polyethylene administration set. Furthermore, the
buffer capacity and
haemolysis studies showed no indications for
haemolysis or potential for vascular irritation upon continuous infusion of
C1311. In conclusion,
C1311 lyophilized product is adequately stable and compatible after reconstitution and in infusion fluids to be used in the clinic and is not expected to cause formulation-associated side effects in the intended administration schedule in the forthcoming Phase I clinical study.