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Glutaminase Inhibitors

The Opportunity: 

CRUK has developed a potent, selective and orally bioavailable series of small molecules inhibiting glutaminase (GLS), with superior developability. We are seeking a co-development partner to support key in vivo data and drive rapid progression into clinical trials.

The Technology: 

CRUK has developed a potent, selective and orally bioavailable series of small molecules inhibiting glutaminase (GLS), with superior developability. We are seeking a co-development partner to support key in vivo data and drive rapid progression into clinical trials.

GLS converts glutamine to glutamate, which feeds into the TCA cycle to provide building blocks for cellular survival. Many tumours show increased GLS1 levels and a dependence on glutamine, and extensive target validation work (both knockdown and inhibitor studies) have implicated GLS in multiple tumour types and suggest a role for GLS inhibitors in both combination and immune oncology settings.

Initial compounds showed good in vitro activity but were not sufficiently potent in vivo. However, the follow on lead series has been shown in vitro to have better PK properties, lower toxicity and a clean selectivity profile, predicting better results in vivo. Patent applications covering both the original compound series and new lead series have been published and have extensive territory coverage.

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