On February 10, 2020 Gibson Oncology, LLC ("Gibson"), a privately held clinical stage company, obtained world-wide,reported an exclusive commercial rights to a novel series of 56 rationally designed compounds called Azaindenoisoquinolines ("Aza Compounds"), from Purdue University and the National Cancer Institute (Press release, Gibson Oncology, FEB 10, 2020, View Source [SID1234554100]). These Aza Compounds have proven to be dual inhibitors of cMyc and topoisomerase I (TOP1).
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Previous attempts over decades to target cMyc, a major oncogene involved in driving 80% of all tumors, have failed because of the peculiar characteristics of the shallow binding pockets on the cMyc protein, which created the reputation of being an "undruggable" target. Gibson’s novel Aza Compounds were rationally designed to avoid this issue through a novel mechanism of action (MOA) involving the stabilization of the G-quadruplex in the cMyc promoter, resulting in inhibition of transcription of the cMyc gene and thus inhibition of production of the Myc protein. In addition, these Aza Compounds are also potent TOP1 inhibitors, which synergizes with their G-quadruplex stabilizing activity and further enhances their anti-cancer abilities.
Gibson has already signed contracts to produce clinical candidates suitable for an IND.
Dual targeting of cMyc and TOP1 may serve as a novel and highly effective anticancer strategy across a spectrum of cancers. New intellectual property on composition of matter and method of use claims cover such novel compounds to at least 2037.
Randall Riggs, the CEO of Gibson Oncology, LLC, said that "We are excited about the Aza Compounds because scientific literature reports that 80% of all tumors are driven by cMyc. Developing a cMyc inhibitor has been long sought and offers a potential breakthrough therapeutic for many cancers."