PT  - JOURNAL ARTICLE
AU  - Den Brok, Monique W.J.
AU  - Nuijen, Bastiaan
AU  - Meijer, Dieuwke M.
AU  - Millán, Elena
AU  - Manada, Consuelo
AU  - Beijnen, Jos H.
TI  - Pharmaceutical Development of a Parenteral Lyophilised Formulation of the Investigational Anticancer Agent ES-285.HCl
DP  - 2005 Jul 01
TA  - PDA Journal of Pharmaceutical Science and Technology
PG  - 246--257
VI  - 59
IP  - 4
4099  - http://journal.pda.org/content/59/4/246.short
4100  - http://journal.pda.org/content/59/4/246.full
SO  - PDA J Pharm Sci Technol2005 Jul 01; 59
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.