The ability to deliver the potent anti-
cancer agent
docetaxel via the oral route may enable the development of promising new treatment regimens with reduced toxicity, increased efficacy, and increased patient convenience. Recently, we were able to overcome the low oral bioavailability of
docetaxel by concomitant administration of the pharmacokinetic booster
ritonavir and the design of an oral solid dispersion formulation of
docetaxel (ModraDoc001 10-mg
capsule). Further research lead to the development of a
docetaxel tablet (ModraDoc003 10-mg
tablet) and a fixed-dose combination (FDC)
tablet of
docetaxel and
ritonavir (ModraDoc004 10/50-mg
tablet). In this clinical proof-of-concept study the exposure to
docetaxel and
ritonavir was compared between the single agent formulations and the FDC
tablet. Six evaluable patients received 40 mg
docetaxel and 200 mg of
ritonavir once a week according to a cross-over design. No significant differences were found in the exposure to
docetaxel and
ritonavir between the single agent formulations and the FDC
tablet. There was, however, a tendency towards a higher exposure to
docetaxel after the administration of the FDC
tablet, which could be an effect of the simultaneous release of
docetaxel and
ritonavir in the gastrointestinal tract. The FDC
tablet of
docetaxel and
ritonavir is a pharmaceutically and clinically feasibly option in the development of patient convenient oral anti-
cancer therapy with
docetaxel.