Bioavailability breakthrough key to new cancer drug OKed in Japan

Japan has become the first country to approve a new cancer pill that treats disease by interfering with DNA replication in tumour cells.

The new drug – Lonsurf – is a formulation of the nucleoside analog trifluridine and the bioavailability enhancement agent tipiracil hydrochloride that has been cleared for the treatment of patients with otherwise untreatable colorectal cancer.

During cell division, either cancerous or normal, the DNA of the mother cell is duplicated with a copy being transferred to the new cell.

This copying process involves the rungs of the DNA double helix breaking apart with each strand of the molecule then acting as a template against which complementary bases are arranged until two new complete molecules are formed.

The trifluridine (FTD) in the newly approved drug has a very similar structure to the chemical Thymidine, which is one of four bases that usually make up a DNA strand. If FTD is present it is incorporated into the new DNA strand in place of Thymidine, which halts replication.

According to a filing by the drug's developer Taiho Pharmaceutical “FTD induces DNA dysfunction through efficient incorporation into DNA, which leads to the inhibition of tumor growth.

The tipiracil hydrochloride (TPI) part of the formulation prevents degradation of FTD thereby allowing more sustained and effective concentrations of the FTD.

Taiho said in a press release that “Japan is the first country in the world to grant marketing authorization for Lonsurf. The approval is based primarily on the results of a randomized, double blind placebo controlled Phase II clinical trial conducted in Japan.”

Taiho is conducting a global Phase III clinical trial on patients with metastatic colorectal cancer refractory to standard chemotherapies."

Bioavailability Challenge 2014

Drug bioavailability is a hot topic for the drug industry, with both small molecule-focused pharmaceutical firms and biopharmaceutical developers increasingly interested in technologies that can help them make promising therapeutic candidates into sellable products.

On March 27 are holding the second edition of our “Bioavailability Challenge 2014” a free to ‘attend’ online webinar series on March 20 focused on the difficulties developers face in ensuring their drug candidates are bioavailable.

Our editorial programme will feature contributions from Yorkshire Biotec and analysts group Frost & Sullivan will share its overview of the bioavailability services market.

The event will also feature presentations from scientists from Ashland, BASF, Dow and many more…

Click here to sign up for the show. See you on March 27.