The oncogene MYC is one of the most sought after and difficult to drug targets in cancer. MYC plays a pivotal role in numerous cancers and has been estimated to be involved in up to 70% human cancers (Gurel et al., 2008; Palaskas et al., 2011). Traditionally MYC has been considered undruggable. However, RDP Pharma is rising to the challenge by utilizing our PromptDegrader™ platform, where we target proteins with intrinsically disordered regions.
Current Achievements in Drug Candidate Discovery:
- Proof of activity has been established in:
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- In vitro – target degradation and tumour cytotoxicity
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- In vivo – effectiveness in lung and triple negative breast cancer xenograft models
- Identified a New Chemical Entity degrader (patented)
- Established “Green Chemistry”
- Ease of synthesis and favourable upscaling properties
- Orally available
- Mechanism of action studies are ongoing
- Optimization of NCEs via in-house own chemistry and computational chemistry departments (structure activity relationship)
- Identified compounds with drug-like properties
- Compliance with the “Lipinski rule of 5” (drug-ability)