On May 1, 2017 SignalRx Pharmaceuticals Inc., a clinical-stage company developing novel small-molecules therapeutics to inhibit key orthogonal and synergistic oncotargets for the treatment of cancer, reported the presentation last week of its novel approach to immune-oncology treatments (Press release, SignalRx, MAY 1, 2017, http://www.ireachcontent.com/news-releases/signalrx-discloses-its-novel-immuno-oncology-program-approach-at-the-12th-annual-drug-discovery-chemistry-2017-meeting-620879733.html [SID1234527322]). The presentation by Donald L. Durden, MD, PhD, senior scientific advisor for SignalRx, occurred at 10:30 am on Thursday April 27th, 2017, at the Drug Discovery Chemistry 2017 meeting in San Diego, CA.
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The presentation was entitled"Dual PI3K/BRD4 inhibitor (SF2523) for immuno-oncology to suppress MYC and the MQ immunosuppressive environment". SignalRx’s program provides a novel approach to immune-oncology and is summarized below:
SF2523 is the only known nM potent dual PI3K/BET bromodomain inhibitor; this provides maximal suppression of the oncogenic transcription factor MYC via enhanced MYC degradation (PI3K inhibition) coupled with decreased production of MYC by inhibiting BRD4 which inhibits transcription of MYC.
MYC has been shown by others to regulate the antitumor immune response through immune-oncology checkpoint receptors CD47 and PD-L1; we have demonstrated that SF2523 reduces the expression of PD-L1 in hepatocellular carcinoma cells, likely through the suppression of MYC.
SF2523 inhibits PI3K isoforms shown by others to regulate the immune suppression found in the tumor microenvironment
SF2523 blocks the transition of M1 macrophages to the immune-suppressing M2 macrophage stage which is expected to augment antitumor immunity
SF2523 is the only dual PI3K/BRD4 inhibitor with demonstrated in vivo antitumor, antimetastatic and immune activating activity.
SignalRx is also seeking partnering opportunities to accelerate the development of its programs and advance novel anticancer therapeutics into first-in-man clinical trials based on the promising profile and mode of action of its inhibitors. Since these are single molecules with a single PK/PD and toxicity profile, there is a great opportunity to streamline their development alone and in combination therapies.