Pharmaceutical Development of a Parenteral Lyophilised Formulation of the Investigational Anticancer Agent ES-285.HCl

Monique W.J. Den Brok; Bastiaan Nuijen; Dieuwke M. Meijer; Elena Millán; Consuelo Manada; Jos H. Beijnen

Abstract

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.

Footnotes

PDA members receive access to all articles published in the current year and previous volume year. Institutional subscribers received access to all content. Log in below to receive access to this article if you are either of these.

If you are neither or you are a PDA member trying to access an article outside of your membership license, then you must purchase access to this article (below). If you do not have a username or password for JPST, you will be required to create an account prior to purchasing.

Full issue PDFs are for PDA members only.

Note to pda.org users

The PDA and PDA bookstore websites (www.pda.org and www.pda.org/bookstore) are separate websites from the PDA JPST website. When you first join PDA, your initial UserID and Password are sent to HighWirePress to create your PDA JPST account. Subsequent UserrID and Password changes required at the PDA websites will not pass on to PDA JPST and vice versa. If you forget your PDA JPST UserID and/or Password, you can request help to retrieve UserID and reset Password below.