On April 20, 2016 Deciphera Pharmaceuticals, a clinical-stage biotechnology company focused on developing advanced kinase inhibitor treatments targeting the tumor cell and the tumor microenvironment, reported that its highly-selective small molecule CSF1R inhibitor, DCC-3014, has demonstrated highly-specific inhibition of the colony stimulating factor 1 receptor (CSFIR), a key target across many cancer indications (Press release, Deciphera Pharmaceuticals, APR 20, 2016, View Source [SID:1234511141]). In addition, DCC-3014, which was designed as a highly-specific macrophage immunomodulatory agent based on the company’s Switch Control Inhibitor platform, demonstrated significantly enhanced anti-tumor activity when used in combination with an anti-PD-1 checkpoint inhibitor in preclinical cancer models. Based on these data, which were presented at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting 2016, on April 20, 2016 in New Orleans, Deciphera plans to initiate a Phase 1 clinical trial with DCC-3014 in the second half of 2016.

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"DCC-3014’s robust inhibition of the CSF1R kinase, as demonstrated by these data presented at the AACR (Free AACR Whitepaper) Annual Meeting, provide encouraging evidence of its potential as a immunomodulatory agent through its action on tumor-associated macrophages (TAMs), both as a single agent and in combination with other immune checkpoint inhibitors, across a number of cancer models," said Michael D. Taylor, Ph.D., Deciphera’s President and Chief Executive Officer. "We look forward to initiating the first-in-human Phase 1 trial with DCC-3014 later this year."

In a poster titled, "The highly specific CSF1R inhibitor DCC-3014 exhibits immunomodulatory and anti-invasive activities in cancer models," Deciphera researchers presented preclinical data demonstrating DCC-3014’s robust inhibition of CSF1R kinase, and potential utility as a macrophage immunomodulatory agent in combination with other immune checkpoint inhibitors or chemotherapeutic agents. Highlights of the data include:

DCC-3014 exhibited nanomolar potency for inhibition of CSF1R, sparing highly related kinases such as KIT, PDGFR and FLT3 by greater than 100-fold, and sparing other kinases by more than 1,000-fold.
DCC-3014 showed sustained in vivo inhibition of CSF1R, offering greater than 90% inhibition more than 24 hours after dosing, in a murine PK/PD model.
DCC-3014 demonstrated significant single agent activity and additive effects in combination with a murine anti-PD1 antibody in a murine model of colorectal cancer.
DCC-3014 blocked tumor growth, invasion and bone degradation in a prostate cancer model and exhibited optimized biopharmaceutical properties.
About DCC-3014

DCC-3014, a highly-selective small molecule colony stimulating factor 1 receptor (CSFIR), was designed as a highly-specific macrophage immunomodulatory agent based on the company’s Switch Control Inhibitor platform. In preclinical studies, DCC-3014 has demonstrated highly-specific inhibition of CSF1R, a key target across many cancer indications, as well as significantly enhanced anti-tumor activity when used in combination with an anti-PD-1 checkpoint inhibitors. Based on these data, Deciphera plans to initiate a Phase 1 clinical trial with DCC-3014 in the second half of 2016.