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Identification of GDC-1971 (RLY-1971), a SHP2 Inhibitor Designed for the Treatment of Solid Tumors

Protein tyrosine phosphatase SHP2 mediates RAS-driven MAPK signaling and has emerged in recent years as a target of interest in oncology, both for treating with a single agent and in combination with a KRAS inhibitor. We were drawn to the pharmacological potential of SHP2 inhibition, especially following the initial observation that drug-like compounds could bind an allosteric site and enforce a closed, inactive state of the enzyme. Here, we describe the identification and characterization of GDC-1971 (formerly RLY-1971), a SHP2 inhibitor currently in clinical trials in combination with KRAS G12C inhibitor divarasib (GDC-6036) for the treatment of solid tumors driven by a KRAS G12C mutation.

 

Comments:

That's a fascinating development! The targeted inhibition of SHP2 in conjunction with a KRAS G12C inhibitor sounds promising for treating solid tumors with that specific mutation. The approach of using GDC-1971 (formerly RLY-1971) as a SHP2 inhibitor in combination with divarasib (GDC-6036) to tackle RAS-driven MAPK signaling represents a significant stride in oncology research.

The allosteric binding of drug-like compounds to enforce an inactive state of SHP2 seems like a strategic approach to modulate its activity. Clinical trials involving these compounds could potentially offer a more effective treatment strategy for solid tumors associated with KRAS G12C mutations, which have historically been challenging to target.

The synergy between the SHP2 inhibitor and the KRAS G12C inhibitor might enhance the therapeutic effect by simultaneously disrupting the signaling pathways necessary for tumor growth and proliferation. It would be intriguing to learn about the outcomes of ongoing clinical trials and their implications for the future of oncology treatments.

Related Products

Cat.No. Product Name Information
E1191 GDC-1971 GDC-1971 (compound 199) is a SHP2 inhibitor.

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phosphatase