SignalRX Pharmaceuticals Awarded $2M Phase II STTR Grant From NCI For The Development Of Epigenetic-Kinase Inhibitors As Anticancer Agents

Published: Aug 08, 2017

SAN DIEGO, Aug. 7, 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 that it has received $2-million non-dilutive funding to advance the preclinical development of their proprietary and first-in-class small-molecule epigenetic-kinase inhibitors as anticancer therapeutics. 

SignalRx was awarded a Phase II Small Business Technology Transfer Research (STTR) grant from the National Cancer Institute (NCI), a division of the National Institutes of Health (NIH), to support further preclinical development of SignalRx's novel epigenetic-kinase inhibitors targeting PI3 kinase (PI3K) and the bromodomain protein BRD4.  The principal investigator on the STTR grant is SignalRx's scientific advisor Dr. Donald Durden, MD, PhD who also serves as the academic collaborator for the grant while in his capacity as the Associate Director for Pediatric Oncology at the Moores UCSD Cancer Center at the University of California, San Diego.

Highlights of the dual BRD4-PI3K inhibition approach include:

  1. Demonstrated efficacy in several mouse tumor models.
  2. Demonstrated to be much safer in vivo over combinations of individual BRD4 & PI3K inhibitors.
  3. Overcomes barrier of additive toxicity to combining drugs.
  4. Overcomes cancer resistance mechanisms.
  5. Increases potential patient population.
  6. Provides maximal pharmacodynamic inhibition in individual cancer cells (8X greater).
  7. Molecular chemotypes distinct from existing competitor single agents.
  8. Opportunity to develop more complex anticancer drug combinations.

"This large STTR grant award by the NCI follows on the heels of our proof-of-concept publication recently in PNAS and supports a change in cancer-development dogma from one-molecule one-target approaches to develop a single molecule that inhibits carefully-selected multi-targets resulting in augmented anti-cancer efficacy with less toxicity" said Donald L. Durden, MD, PhD. "This new approach paves the way for more sophisticated and cost-effective combinations in cancer patients resulting in longer duration of benefits in more patients."

"There is an unmet need in oncology for more effective and especially more durable treatments. Despite new drugs aimed at new exciting cancer targets, these drugs only benefit the patient for a short time" said Dr. Joe Garlich, Chief Scientific Officer at SignalRx. "More durable treatments are now recognized to require combinations of drugs, but optimal combinations of drugs are not achievable due to additive toxicities of the individual drugs in the combination.  Our technology, creating single drugs with multiple mechanisms of action mimicking drug combinations, allows for effective combinations of drug mechanisms to be used with less toxicity and potentially more durability (long lasting)."

SignalRx is interested in partnering discussions to take these novel small molecules through clinical trials together with companion diagnostics for streamlined development and approval.

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 ( or contact Dr. Guillermo Morales, PhD, MBA at

Acknowledgement of NIH Support.

The project described above is supported by award number 2R42CA192656-02A1 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,

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