This technology describes a set of small molecules cGAS inhibitor that have been chemically modified for improved bioavailability to improve activation of anti-tumor immunity.
The cGAS/STING inflammatory pathway is an attractive target for anti-viral and anti-tumor treatment. Tumors with high chromosomal instability show aberrant signaling of the cGAS-STING pathway, which promotes tumor growth. Current cGAS inhibitors in development lack the necessary pharmacokinetic and pharmacodynamic properties for therapeutic use. As such, there is a need for a bioavailable cGAS inhibitor to restrain pro-tumor signaling and impeding tumor growth for the treatment of cancer.
This technology describes a set of chemically-modified small molecule cGAS inhibitors to target the cGAS-STING pathway for cancer treatment. The parent compound (G150) has been altered with additional chemical groups, such as polar functional groups, to improve solubility, permeability, and bioavailability. One produced prodrug can undergo aminopeptidase hydrolysis to release the parent drug for improved solubility. As such, these compounds overcome the limitations of previous cGAS inhibitors to make targeting the cGAS-STING pathway a viable option for cancer treatment.
Patent Pending
IR CU23316
Licensing Contact: Joan Martinez
