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ICR and Cancer Research UK spinout company Monte Rosa Therapeutics launches with library of anti-cancer compounds

Professor Ian Collins talks about our drug discovery work - including in forming spinout companies funded by venture capital

A company formed as a spinout from Cancer Research UK-funded science at The Institute of Cancer Research, London, has been publicly launched – revealing $32.5m in funding and a library of innovative anti-cancer compounds.

Monte Rosa Therapeutics – formed by Versant Ventures, The Institute of Cancer Research (ICR) and Cancer Research UK – aims to target cancer using new drugs that take advantage of a cutting-edge concept in drug discovery called protein degradation.

This involves co-opting ubiquitin ligases – large cellular proteins involved in the natural degradation of cell products – to destroy cancer-causing proteins that cannot be targeted by current drug types.

Monte Rosa has secured an initial $32.5m of funding from its founding investor Versant Ventures, a healthcare venture capital firm, and New Enterprise Associates.

It will soon launch another round of financing to raise funds to run clinical studies of some of its leading drug candidates.

Monte Rosa Therapeutics

Now based in Boston in the US, the company was formed in 2018 with the involvement of Cancer Research UK-funded ICR scientists Professor Ian Collins, the ICR’s Head of Chemistry, and Professor Raj Chopra, formerly the ICR’s Head of Cancer Therapeutics.

Monte Rosa Therapeutics has built an integrated drug discovery platform that combines one of the most diverse chemical libraries of small-molecule protein degraders with in-house proteomics and structural biology capabilities.

The small molecules act as ‘molecular glue’ – sticking together ubiquitin ligases with other protein targets.

By the end of 2020, Monte Rosa Therapeutics expects the chemical library to grow to more than 10,000 structures designed for ubiquitin ligase reprogramming.

Drug discovery

One of the company’s leading small-molecule compounds, known as MRT-048, was discovered by chemists in the Cancer Research UK Cancer Therapeutics Unit at the ICR, who also developed the initial library of protein degraders.

Further research at the ICR as part of an ongoing collaboration between Monte Rosa, the ICR and Cancer Research UK has shown the potential of MRT-048 as a new breast cancer treatment.

Cancer Research UK and the ICR are eligible to receive milestones and royalties on future products discovered or developed under the collaboration between Monte Rosa, the ICR and Cancer Research UK. Any payments made to Cancer Research UK and the ICR will be invested into future life-saving research.

Targeted protein degradation is one of the most exciting new fields to emerge in drug discovery in recent years.

It was inspired by studies of immunomodulatory drugs from the thalidomide family, which were found to work via a ubiquitin ligase called cereblon, and are still in use today as a treatment for some types of blood cancers.

Discovering ‘innovative new compounds’

Studies of thalidomide revealed the potential of ubiquitin ligases, also known as E3 ubiquitin ligases, to be reprogrammed to act against previously undruggable proteins that drive disease.

Professor Ian Collins, Professor of Medicinal Chemistry at The Institute of Cancer Research, London, a scientific founder of Monte Rosa Therapeutics, said:

“We’re delighted to see the public announcement of Monte Rosa Therapeutics, originally a spinout company based on research led by scientists here at the ICR.

“We’re proud of our world-leading work in partnership with industry, which is leading to the discovery of innovative new compounds like MRT-048 that work in new ways, and emerge from really exciting, collaborative science.”

‘Using cutting-edge research’

Tony Hickson, Chief Business Officer for Cancer Research UK, said:

“We’re delighted to have worked with Versant and world-class Cancer Research UK-funded scientists to help establish Monte Rosa, and it’s fantastic to see that Monte Rosa has attracted the support of leading venture capital firms to take it to the next stage. We’re pleased to be collaborating with Monte Rosa, where we will be using cutting-edge research to accelerate the development of potential new treatments for cancer patients.”

Markus Warmuth, MD, CEO of Monte Rosa Therapeutics and a venture partner at Versant Ventures, said:

“With our improved understanding of the broad potential of cereblon and other ubiquitin ligases, there is now an opportunity to eliminate major – and currently undruggable – drivers of solid tumors such as transcription factors and adaptor proteins.”


Enterprise Unit drug discovery cereblon monte rosa therapeutics centre for protein degradation
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