RT Journal Article
SR Electronic
T1 Pharmaceutical Development of a Parenteral Lyophilised Formulation of the Investigational Anticancer Agent ES-285.HCl
JF PDA Journal of Pharmaceutical Science and Technology
JO PDA J Pharm Sci Technol
FD Parenteral Drug Association (PDA)
SP 246
OP 257
VO 59
IS 4
A1 Monique W.J. Den Brok
A1 Bastiaan Nuijen
A1 Dieuwke M. Meijer
A1 Elena Millán
A1 Consuelo Manada
A1 Jos H. Beijnen
YR 2005
UL http://journal.pda.org/content/59/4/246.abstract
AB ES-285.HCl [(2S,3R)-2-aminooctadecan-3-ol hydrochloride] is a novel investigational anticancer agent which has shown activity against various tumour cell lines with selectivity for certain solid tumours (i.e., hepatocellular, prostate, and renal). The aim of this study was to design stable parenteral pharmaceutical final products containing 25 mg and 50 mg ES-285.HCl per dosage unit for use in phase I clinical trials. ES-285.HCl drug substance was fully characterised and showed very slight solubility in water. The development of the pharmaceutical product, containing 2-hydroxypropyl-β-cyclodextrin, is discussed in view of formulation optimisation and manufacture. The developed freeze-dried products were found stable for at least 6 months at an accelerated storage condition of 25 ± 2°C/60 ± 5% relative humidity and for at least 12 months at the designated long term storage condition of 5 ± 3°C, in the dark. Phase I trials using ES-285.HCl 25 mg/vial and 50 mg/vial final products are currently ongoing.