DCC-3116

ULK kinase inhibition for cancers caused by RAS/RAF mutations

DCC-3116 in an investigational, orally administered, potent, and highly selective switch-control inhibitor of the ULK kinase that was discovered using our proprietary drug discovery platform. DCC-3116 is designed to inhibit autophagy, a key tumor survival mechanism in cancer cells, by inhibiting the ULK 1/2 kinases, which have been shown to be the initiating factors that activate autophagy. DCC-3116 in combination with RAS/MAP kinase signaling pathway inhibition has the potential to change the treatment of RAS/RAF cancers.

Cancers caused by RAS/RAF mutations are the most common activating mutations of all cancers and represent a significant unmet medical need. The RAS mutation activates signaling through the MAPK (RAF-MEK-ERK) pathway and the autophagy pathway. MAPK inhibitors have not been successful thus far as single agents for the treatment of cancers caused by RAS mutations.

DCC-3116 Phase 1 Study

DCC-3116 is being investigated in a Phase 1/2 study designed to evaluate the safety, tolerability, clinical activity, pharmacokinetics, and pharmacodynamics of DCC-3116 as a single agent and in combination with sotorasib and with QINLOCK in patients with advanced or metastatic solid tumors.
To learn more about this study, click here.
Related Presentations and Publications

04-18-2023 - AACR - DCC-3116, a first-in-class selective inhibitor of ULK1/2 kinases and autophagy, in combination with the KIT inhibitor ripretinib induces complete regressions in GIST preclinical models.

04-18-2023 - AACR - Presentation of New Preclinical Data Highlighting Discovery Research Programs at the American Association for Cancer Research (AACR) Annual Meeting 2023.

04-17-2023 - AACR - DCC-3116, a first-in-class selective inhibitor of ULK1/2 kinases and autophagy, synergizes with encorafenib and cetuximab in BRAF V600E mutant colorectal cancer models.

09-11-2022 - ESMO - Presentation of New Clinical Study Results from DCC-3116 and Vimseltinib at the European Society for Medical Oncology (ESMO) Congress 2022.

09-10-2022 - ESMO - Initial monotherapy results of a phase 1 first‑in‑human study of ULK1/2 inhibitor DCC‑3116 alone and in combination with MAPK pathway inhibition.

04-15-2022 - Corporate Presentation - DCC -3116 Overview and Preclinical Data.

04-12-2022 - AACR - DCC-3116, a First-in-Class Selective Inhibitor Of ULK1/2 Kinases and Autophagy, Combines with the KRASG12C Inhibitor Sotorasib Resulting in Tumor Regression in NSCLC Xenograft Models.

10-07-2021 - AACR-NCI-EORTC - DCC-3116, a first-in-class selective inhibitor of ULK1/2 kinases and autophagy, synergizes with EGFR inhibitors osimertinib and afatinib in NSCLC preclinical models.

11-19-2020 - Autophagy Summit - Discovery of ULK1/2 inhibitor DCC 3116 for treatment of RAS driven cancers.

10-29-2019 - AACR-NCI-EORTC - Preclinical studies with DCC-3116, an ULK kinase inhibitor designed to inhibit autophagy as a potential strategy to address mutant RAS cancers. 

06-18-2019 Corporate Presentation DCC-3116: A Selective ULK Kinase Inhibitor; Potential First-in-Class Autophagy Inhibitor to Treat Mutant RAS Cancers

DCC-3116 Phase 1 Study

Related Presentations and Publications