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

The Phase 1 study of DCC-3116 is a multicenter, open-label, first-in-human study designed to evaluate the safety, tolerability, clinical activity, pharmacokinetics (PK), and pharmacodynamics (PD) of DCC-3116 as a single agent and in combination with MEK and KRAS G12C inhibitors, in patients with advanced or metastatic tumors with a RAS/MAPK pathway mutation.

To learn more about this study, click here.

To access the most recent Phase 1 data, 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