ARDR STORY

Inhibited potential

February 2015 - It's a deal worth up to US$0.5 billion (around $700 million), and this does not even include potential earnings through royalties and sales:

On behalf of the Melbourne-based Cooperative Researcher Centre for Cancer Therapeutics (CTx), a UK based agency has entered a licensing agreement with global pharma giant Merck to further develop and commercialise a new type of drugs for the treatment of cancerous and non-cancerous blood disorders.

PRMT5 modifies regulatory proteins that interact with DNA, including tumour surpressor p53 and the DNA-structure determining histones.
Image is simplified illustration and based on a figure published by Shelley Berger

And CTx will be the main beneficiary of the potential returns.

The licence relates to a new class of drugs that inhibit a protein involved in many cellular processes, including in cancer - the arginine methyltransferase 5 (PRMT5).

The protein is one of the cell's tools to modulate the activity of genes.

PRMT5 does this by chemically modifying key proteins that interact with DNA, including histones and a group of proteins involved in the prevention of cancer formation (tumour surpressor p53).

The important points of the deal:
  • Promising new drugs which have potential clinical applications for both cancer and non-cancer blood disorders affecting millions of people worldwide;
  • Upfront payment in excess of $21 million and potential payments in excess $0.7 billion;
  • Majority of revenues will be returned to CTx and its Australian research partners;
  • Additional funded collaboration between Merck and CTx on blood disorders.

The levels of PRMT5 have been found increased in many cancers, and hence it is an attractive drug target.

This motivated researchers from the CTx and its research partners to screen a diverse library of 350,000 small compounds for their inhibitory activity against PRMT5.

And as they recently described in a paper in Cancer Research, the set of potential inhibitors they obtained was then used to develop classes of highly selective inhibitors of PRMT5.

In addition to their potential as a treatment of cancer, the new inhibitors were found to also increase the activity of important genes involved in the replenishing of blood. Therefore, the new PRMT5 inhibitors could provide new treatment options for both patients with cancer and patients with blood disorders like sickle cell disease and beta thalassemia.

More information: www.cancercrc.com
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