SAN DIEGO, May 1, 2017 /PRNewswire-iReach/ -- SignalRx Pharmaceuticals Inc., a clinical-stage company developing novel small-molecules therapeutics to inhibit key orthogonal and synergistic oncotargets for the treatment of cancer, today announced the presentation last week of its novel approach to immune-oncology treatments. 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.
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.
About SignalRx Pharmaceuticals Inc.
SignalRx is a privately held corporation based in San Diego, CA developing small molecule inhibitors of key signaling pathways in cancer and cancer stem cells. The company has developed its proprietary CRIMP technology platform to develop new small-molecule therapeutics against more than one target molecule selected from the discovery of synthetic lethalities in cancer cells, epigenetic regulatory processes, immune checkpoints and DNA repair actions. SignalRx’s research programs have novel dual inhibitors targeting critical onco-targets such as PI3K, MEK, BRAF, IDO1, IDH1, CDK4/6, Wnt, HDAC, DNMT, PARP and BET bromodomains. SignalRx is leveraging its expertise in novel multi-action inhibitors to develop enhanced anticancer therapeutics with improved efficacy, novel mechanism of action in a single molecule, and the potential to streamline their development (single agent, combination therapies).
For additional information please visit our website (www.signalrx.com) or contact our Chief Business Officer Dr. Guillermo Morales, PhD, MBA at morales@signalrx.com
Acknowledgement of NIH Support. The project described above was supported by award number 1 R41 CA192656-01 from the NCI division of the NIH. The above description is solely the responsibility of SignalRx and does not necessarily represent the official views of the NIH or NCI.
Media Contact: Guillermo Morales, SignalRx Pharmaceuticals Inc., 520-777-9609, morales@signalrx.com
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