Chemotherapy tablets: the choice of the future

The argument for oral chemotherapy to be presented at Utrecht University, the Netherlands, 29 March 2017, 2:30pm

On Wednesday 29 March 2017, Dutch researcher Emilia Sawicki will be arguing in favour of orally administered chemotherapy against intravenous ones, using her own research, at Utrecht University, the Netherlands.

Sawicki will describe one of the anticancer medicines for which she developed a tablet formulation, the widely-used drug docetaxel.

The formulation is a tablet which is made as a “solid dispersion” and was co-developed by Sawicki at the Slotervaart Medical Centre and the Netherlands Cancer Institute, Antoni van Leeuwenhoek Hospital, Amsterdam.

The discovery has already progressed to an advanced stage in the clinical development. Shortly, a clinical trial will be opened at several Dutch hospitals where patients with prostate cancer will be treated with the solid dispersion tablet of docetaxel.

Anticancer medicines are increasingly used as capsules or tablets. Oral medicines are more patient-friendly than the traditional way of administration the chemotherapy as an intravenous infusion.

As a solid form, docetaxel and paclitaxel are not well absorbed in the blood. They are broken down by enzymes.

Patients can take the medicine at home as a tablet and no longer have to travel to a hospital to receive chemotherapy. One of the requirements is that the anticancer medicine dissolves in water, then effectively taken up in the blood.

Dissolution is better if a “solid dispersion” is used, i.e., a mixture of tiny particles of powdered medication. These dissolve faster and better in water than larger particles, such as crystalline powders.

In her doctoral thesis “Solid dispersions in oncology: a solution to solubility-limited oral drug absorption”, Sawicki describes a new production method for solid dispersions of docetaxel and paclitaxel, two anticancer medicines that are often prescribed to patients with prostate cancer, breast cancer and lung cancer.

As a solid form, docetaxel and paclitaxel are not well absorbed in the blood. This is because they are very poorly soluble in water and are broken down by enzymes in the gastrointestinal tract and liver.

Solid dispersions dissolve faster in water than larger particles … they are then effectively absorbed in the blood.

The solid dispersion method increases the dissolution of docetaxel and paclitaxel 40–100 times and when co-administered with enzyme inhibitor ritonavir, these anticancer medicines are then effectively absorbed in the blood.

Moreover, the production method for the solid dispersion tablet of docetaxel is suitable to supply the medicine on a large scale, making it possible to conduct large clinical trials.

Sawicki also used the solid dispersion technique to develop a tablet formulation of elacridar, a medicine predominantly used in studies focusing on brain tumours, as elacridar promotes the absorption of other anticancer medicines in the brain.

Amsterdam-based biopharmaceutical company Modra Pharmaceuticals will shortly launch several clinical trials with the solid dispersion tablet of docetaxel.

Emilia Sawicki will be speaking at Utrecht University, the Netherlands, Wednesday 29 March 2017 at 2:30pm.