Presentations & Publications

INSIGHT: A phase 3, randomized, multicenter, open-label study of ripretinib vs sunitinib in patients with advanced gastrointestinal stromal tumor previously treated with imatinib harboring KIT exon 11 + 17 and/or 18 mutations.

Outcomes in patients with advanced gastrointestinal stromal tumor who did not have baseline ctDNA detected in the INTRIGUE study.

Overall survival and long-term safety in patients with advanced gastrointestinal stromal tumor previously treated with imatinib: Updated analyses from INTRIGUE.

DCC-3084, a RAF dimer inhibitor, broadly inhibits BRAF class I, II, III, BRAF fusions, and RAS-driven solid tumors leading to tumor regression in preclinical models.

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.

DP-9024, an investigational small molecule modulator of the Integrated Stress Response kinase GCN2, synergizes with asparaginase therapy in leukemic tumors.

Pan-exon mutant KIT inhibitor DCC-3009 demonstrates tumor regressions in preclinical gastrointestinal stromal tumor models.

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

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.

Dimerization-induced activation of the Integrated Stress Response kinase PERK by an investigational small molecule modulator, DP-9024.

DP-9024, an investigational small molecule modulator of the Integrated Stress Response kinase PERK, causes B-cell cancer growth inhibition as single agent and in combination with standard-of-care agents.

DP-9149, an investigational small molecule modulator of the Integrated Stress Response kinase GCN2, pre-clinically causes solid tumor growth inhibition as a single agent and regression in combination with standard of care agents.

Mutational heterogeneity of imatinib resistance and efficacy of ripretinib vs sunitinib in patients with gastrointestinal stromal tumor: ctDNA analysis from INTRIGUE.

Efficacy And Safety Of Ripretinib In Chinese Patients With Advanced Gastrointestinal Stromal Tumors: A real-world, multicenter, observational study.

Efficacy and Safety of Ripretinib vs Sunitinib in Patients with Advanced Gastrointestinal Stromal Tumor Previously Treated with Imatinib: A Phase 2 Multicenter, Randomized, Open-Label Study in China.

Efficacy and safety of vimseltinib in tenosynovial giant cell tumor (TGCT): Phase 2 expansion.

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

Safety and efficacy of vimseltinib in tenosynovial giant cell tumor (TGCT): Long-term phase 1 update.

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.

Ripretinib Versus Sunitinib in Patients With Advanced Gastrointestinal Stromal Tumor After Treatment With Imatinib (INTRIGUE): A Randomized, Open-Label, Phase III Trial.

Efficacy and safety of ripretinib in patients with KIT-altered metastatic melanoma.

Effects of CYP3A Inhibition, CYP3A Induction, and Gastric Acid Reduction on the Pharmacokinetics of Ripretinib, a Switch Control KIT Tyrosine Kinase Inhibitor.

DCC -3116 Overview and Preclinical Data.

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.

INTRIGUE: A phase III, randomized, open-label study to evaluate the efficacy and safety of ripretinib vs sunitinib in patients with advanced gastrointestinal stromal tumor previously treated with imatinib.

Clinical Activity of Ripretinib in Patients with Advanced Gastrointestinal Stromal Tumor Harboring Heterogeneous KIT/PDGFRA Mutations in the Phase III INVICTUS Study.

Ripretinib for advanced gastrointestinal stromal tumor: Plain language summary of the INVICTUS study.

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.

A phase 1b/2 study of rebastinib and paclitaxel in advanced/metastatic platinum-resistant ovarian cancer.

Phase 1 study of ripretinib, a broad-spectrum KIT and PDGFRA inhibitor, in patients with KIT-mutated or KIT-amplified melanoma.

Presentation of New Clinical Study Results from Rebastinib and Vimseltinib at the European Society for Medical Oncology (ESMO) Congress 2021.

Ripretinib as ≥4th-line treatment in patients with advanced gastrointestinal stromal tumour (GIST): Long-term update from the phase 3 INVICTUS study.

Safety and preliminary efficacy of vimseltinib in tenosynovial giant cell tumor (TGCT).

Clinical activity of ripretinib in patients with advanced gastrointestinal stromal tumor harboring heterogenous KIT/PDGFRA mutations in the phase 3 INVICTUS study.

Vimseltinib: A precision CSF1R therapy for tenosynovial giant cell tumors and diseases promoted by macrophages.

Ripretinib intrapatient dose escalation after disease progression provides clinically meaningful outcomes in advanced gastrointestinal stromal tumour.

Clinical Benefit of Ripretinib Dose Escalation After Disease Progression in Advanced Gastrointestinal Stromal Tumor: An Analysis of the INVICTUS Study.

Dermatopathological review of cutaneous squamous cell carcinoma events in patients with gastrointestinal stromal tumor treated with ripretinib.

An open-label, multicenter, phase 1b/2 study of rebastinib in combination with paclitaxel in a dose expansion cohort to assess safety and preliminary efficacy in patients with advanced or metastatic endometrial cancer.

Intra-patient dose escalation of ripretinib after disease progression in patients with advanced gastrointestinal stromal tumor: Analyses from the phase 3 INVICTUS study.

Ripretinib and MEK inhibitors synergize to induce apoptosis in preclinical models of GIST and Systemic Mastocytosis.

Effect of gastric acid reduction and strong CYP3A induction/inhibition on the pharmacokinetics of ripretinib, a switch control tyrosine kinase inhibitor.

Population pharmacokinetics of ripretinib in patients with advanced malignancies.

Discovery of vimseltinib (DCC -3014), a highly selective switch -control inhibitor of CSF1R kinase.

Discovery of ULK1/2 inhibitor DCC 3116 for treatment of RAS driven cancers.

Characterization of the extensive heterogeneity of KIT/PDGFRA mutations in patients with fourth-line advanced gastrointestinal stromal tumor: Genomic analysis of the phase 3 INVICTUS study.

Clinical benefit with ripretinib as ≥fourth-line treatment in patients with advanced gastrointestinal stromal tumor: Update from the phase 3 INVICTUS study. 

Phase 1 Dose-Escalation Study of the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of DCC-3014 in Advanced Solid Tumors and Tenosynovial Giant Cell Tumor (TGCT) (NCT3069469). 

Ripretinib demonstrated activity across all KIT/PDGFRA mutations in patients with fourth-line advanced gastrointestinal stromal tumor: Analysis from the phase 3 INVICTUS study. 

Ripretinib Intra-Patient Dose Escalation Following Disease Progression Provides Clinically Meaningful Progression-Free Survival in Gastrointestinal Stromal Tumor in Phase 1 Study. 

Clinical Benefit with Ripretinib as ≥4th Line Treatment in Patients with Advanced Gastrointestinal Stromal Tumors (GIST): Update from the Phase 3 INVICTUS Study. 

Ripretinib Intra-patient Dose Escalation (IPDE) Following Disease Progression Provides Clinically Meaningful Progression Free Survival (PFS) in Gastrointestinal Stromal Tumor (GIST) in Phase 1 Study. 

A phase 1 study of rebastinib and carboplatin in patients with metastatic solid tumors. 

A phase 1b/2 study of rebastinib and paclitaxel in advanced or metastatic platinum-resistant ovarian cancer. 

Switch Control Inhibition of KIT and PDGFRA in Patients With Advanced Gastrointestinal Stromal Tumor: A Phase I Study of Ripretinib.  

Efficacy and safety of ripretinib as ≥4th-line therapy for patients with gastrointestinal stromal tumor (GIST) following crossover from placebo: Analyses from INVICTUS.

Ripretinib in patients with advanced gastrointestinal stromal tumours (INVICTUS): a double-blind, randomised, placebo-controlled, phase 3 trial.

An open-label, multicenter, phase 1b/2 study of rebastinib in combination with paclitaxel in a dose expansion cohort to assess safety and preliminary efficacy in patients with advanced or metastatic endometrial cancer. 

Quality of life (QoL) and self reported function with ripretinib in ≥4th line therapy for patients with gastrointestinal stromal tumors (GIST): Analyses from INVICTUS. 

Safety profile of ripretinib, including impact of alopecia and palmar plantar erythrodysesthesia syndrome (PPES) on patient reported outcomes (PROs), in ≥4th line advanced gastrointestinal stromal tumors (GIST): Analyses from INVICTUS. 

Thresholds for Meaningful Change for the EQ-5D VAS and EORTC QLQ-C30 Physical and Role Functioning Scale in Gastrointestional-Related Cancers

INVICTUS, A Phase 3, interventional, double blind, placebo controlled study to assess the safety and efficacy of ripretinib (DCC 2618) in patients with advanced gastrointestinal stromal tumors (GIST) who have received treatment with prior anticancer therapies.

Phase 1 study of DCC-3014 to assess the safety, tolerability, pharmacokinetics, and pharmacodynamics in patients with malignant solid tumors and diffuse-type tenosynovial giant cell tumor. 

Phase 1 study of DCC-3014, an oral inhibitor of CSF1R, to assess the safety, tolerability, pharmacokinetics, and pharmacodynamics in patients with advanced solid tumors, including diffuse-type tenosynovial giant cell tumor.

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

Updated results of phase 1 study of ripretinib (DCC-2618), a broad spectrum KIT and PDGFRA inhibitor, in patients with gastrointestinal stromal tumor (GIST) by line of therapy (NCT02571036). 

Phase 1b/2 study of rebastinib (DCC-2036) in combination with paclitaxel: Preliminary safety, efficacy, pharmacokinetics, and pharmacodynamics in patients with advanced or metastatic solid tumors.

INVICTUS, A Phase 3, INterVentional , Double Blind, Placebo Controlled Study to Assess the Safety and Efficacy of Ripretinib as ≥4th Line Therapy In Patients with AdvanCed Gastrointestinal Stromal TUmorS (GIST) Who Have Received Treatment with Prior Anticancer Therapies (NCT03353753).

The INVICTUS Trial: Ripretinib As ≥4th-Line Therapy In Patients With Advanced Gastrointestinal Stromal Tumors (GIST)

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

Ripretinib (DCC-2618) Is a Switch Control Kinase Inhibitor of a Broad Spectrum of Oncogenic and Drug-Resistant KIT and PDGFRA Variants.

Ripretinib (DCC-2618) Pharmacokinetics (PK) in a Phase 1 Study in Patients with Gastrointestinal Stromal Tumors (GIST) and other Advanced Malignancies: A Retrospective Evaluation of the PK Effects of Proton Pump Inhibitors (PPIs).

DCC-2618, a broad-spectrum inhibitor of KIT and PDGFRA mutants,synergizes with inhibitors of the MAPK pathway. 

Initial Results of Phase 1 Study of DCC-2618, a Broad-Spectrum KIT and PDGFR⍺ Inhibitor, in Patients (PTS) with Gastrointestinal Stromal Tumor (GIST) by Number of Prior Regimens.

Mutation Profile of Drug Resistant GIST Patients Enrolled in the Phase 1 Study of DCC-2618

Inhibition of oncogenic and drug-resistant PDGFRA and KIT alterations by DCC-2618. 

Pharmacokinetic (PK), Safety, and Tolerability Profile of DCC-2618 in a Phase 1 Clinical Trial Supports 150mg QD Selected for a Pivotal Phase 3 Study in Gastrointestinal Stromal Tumor (GIST). 

The KIT and PDGFRA switch-control inhibitor DCC-2618 blocks growth and survival of multiple neoplastic cell types in advanced mastocytosis.

DCC-2618, a novel pan-KIT and PDGFRα kinase switch control inhibitor, shows encouraging signal in a patient with glioblastoma (GBM).

DCC-2618, a novel pan-KIT and PDGFRα Kinase switch control inhibitor demonstrates encouraging activity in patients (pts) with Gastrointestinal Stromal Tumors (GIST). 

The selective TIE2 inhibitor rebastinib blocks recruitment and function of TIE2Hi macrophages in breast cancer and pancreatic neuroendocrine tumors.

Encouraging activity of novel pan-KIT and PDGFRα inhibitor DCC-2618 in patients (pts) with gastrointestinal stromal tumor. (GIST)

Neoadjuvant chemotherapy induces breast cancer metastasis through a TMEM-mediated mechanism.

Pharmacokinetic-driven phase I study of DCC-2618 a pan-KIT and PDGFR inhibitor in patients (pts) with gastrointestinal stromal tumor (GIST) and other solid tumors. ASCO 2017 Annual Meeting, Chicago, Il. Abstract# 2515

Translational research in a phase I proof-of-concept study supports that DCC-2618 is a pan-KIT inhibitor.

Phase 1 dose-finding study of rebastinib (DCC-2036) in patients with relapsed chronic myeloid leukemia and acute myeloid leukemia.

DCC-2618, a pan-KIT and PDGFRA switch control inhibitor, achieves proof-of-concept in a first-in-human study.

The highly specific CSF1R inhibitor DCC-3014 exhibits Immunomodulatory and anti-invasive activities in cancer models. 

DCC-2618 is a potent inhibitor of wild type and mutant KIT, including refractory Exon 17 D816 KIT mutations.

Rebastinib potently inhibits function of perivascular TIE2 expressing macrophages in vitro and in vivo. 

Imaging the tumor microenvironment of metastasis reveals the mechanism of transient blood vessel permeability and tumor cell intravasation. 

Mechanisms of transendothelial migration by invasive breast carcinoma cells from patients.

Rebastinib, a selective TIE2 kinase inhibitor, decreases TIE2-expressing macrophages, reduces metastasis, and increases survival in murine cancer models.

Inhibiting endothelium directed tumor cell streaming by targeting the HGF/c-MET and EGF/CSF-1 signaling pathways. 

The specific FMS kinase inhibitor, DCC-3014, durably inhibits FMS kinase in vivo and blocks cancer bone invasiveness. 

Rebastinib in combination with paclitaxel ablates TIE2-expressing macrophages, reduces metastasis, and increases survival in the PyMT metastatic breast cancer model.

Rebastinib in combination with eribulin ablates TIE2-expressing macrophages, reduces metastasis, and increases survival in the PyMT metastatic breast cancer model.

Rebastinib, a small molecule TIE2 kinase inhibitor, prevents primary tumor growth and lung metastasis in the PyMT breast cancer model. 

Targeting the KIT activating switch control pocket: a novel mechanism to inhibit neoplastic mast cell proliferation and mast cell activation.

A phase 1 study of DCC-2036, a novel oral inhibitor of BCR-ABL kinase, in adult subjects with Philadelphia chromosome positive (Ph+) leukemias including subjects with T315I mutation.

The ABL Switch Control Inhibitor DCC-2036 Is Active against the Chronic Myeloid Leukemia Mutant BCR-ABLT315I and Exhibits a Narrow Resistance Profile.

Conformational Control Inhibition of the BCR-ABL1 Tyrosine Kinase, Including the Gatekeeper T315I Mutant, by the Switch-Control Inhibitor DCC-2036.