Scientific Publications

FLX475  
Oral CCR4 Antagonist FLX475 Antitumor Activity Against Extranodal NK/T-cell Lymphoma. 2022 T-Cell Lymphoma Forum View presentation (PDF)
Phase 2 study of FLX475 in combination with ipilimumab in advanced melanoma. SITC 2021 View poster (PDF)
Tumors establish resistance to immunotherapy by regulating Treg recruitment via CCR4 View paper
Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as a Single Agent and in Combination with Checkpoint Inhibitors View paper
Discovery of a Potent and Selective CCR4 Antagonist That Inhibits Treg Trafficking into the Tumor Microenvironment View paper
T-regulatory Cells Impair CAR T-cell-mediated Antitumor Activity in a Murine Solid Tumor Model. AACR 2021. View poster (PDF)
Phase 1/2 Dose Escalation and Expansion Study of FLX475 Alone and in Combination with Pembrolizumab in Advanced Cancer. ASCO 2020 View poster (PDF)
Phase I/II Dose Escalation and Expansion Study of FLX475 Alone and in Combination with Pembrolizumab in Advanced Cancer. ASCO-SITC 2019. View poster (PDF)
Pharmacokinetics, Pharmacodynamics, and Safety of FLX475, an Orally-Available, Potent, and Selective Small-Molecule Antagonist of CCR4, in Healthy Volunteers. SITC 2018. View poster (PDF)
CCR4 Antagonists Inhibit Treg Trafficking into the Tumor Microenvironment. ACS Medicinal Chemistry Letters on September 10, 2018. View paper
EBV-Associated Tumors Increase Regulatory T Cell Recruitment via CCR4 Ligand Expression and are a Promising Indication for Treatment with Small Molecule CCR4 Inhibitors. AACR 2018 on April 17, 2018 View poster (PDF)
Potent and Selective CCR4 Antagonists Inhibit Regulatory T Cell Recruitment, Increase Effector T Cell Numbers, and Potentiate Anti-Tumor Responses in Mice. SITC 2017 on November 11, 2017. View poster (PDF)
Patient Selection Strategies and Pharmacodynamic Assays for CCR4 Antagonists. SITC 2017 on November 10, 2017. View poster (PDF)
Potent and Selective C-C Chemokine Receptor (CCR4) Antagonists Potentiate Anti-tumor Immune Responses by Inhibiting Regulatory T cells (Treg). AACR on April 2, 2017 View poster (PDF)
RPT193  
Blood And Skin Biomarkers From A First-in-human Study Of RPT193 – An Oral CCR4 Antagonist For The Treatment Of Atopic Dermatitis. Biomarker and Companion Diagnostics Conference, June 2022. View poster (PDF)
RPT193, A CCR4 Antagonist, Improves the Inflammatory Skin Transcriptomic Profile in Patients with Atopic Dermatitis. SID Annual Meeting 2022 View poster (PDF)
RPT193, a novel CCR4 inhibitor, improves clinical severity of atopic dermatitis and modulates the transcriptomic profile of lesional skin. 2022 AAD Annual Meeting. View presentation (PDF)
RPT193, an oral CCR4 inhibitor: Efficacy results from a randomized, placebo controlled Phase 1b monotherapy trial in patients with moderate to severe atopic dermatitis. ISDS 2021 View presentation (PDF)
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Clinical safety and efficacy of RPT193, an oral CCR4 inhibitor: Results from a randomized, placebo-controlled Phase 1b monotherapy trial in patients with moderate-to-severe atopic dermatitis. 2021 EADV Congress. View presentation (PDF)
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Development and first-in-human characterization of a potent oral CCR4 antagonist for the treatment of atopic dermatitis. Society of Investigative Dermatology on May 15, 2020. View presentation (PDF)
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FLX193: A Potent, Selective CCR4 Antagonist for Allergic Disorders View poster (PDF)
HPK1  
Development of Small-Molecule HPK1 Inhibitors to Unleash Tumor-Specific T Cell Responses. AACR 2021. View poster (PDF)
Discovery Programs  
MYCN drives chemoresistance in small cell lung cancer while USP7 inhibition can restore chemosensitivity View paper
Novel, Selective Inhibitors of USP7 Uncover Multiple Mechanisms of Antitumor Activity In Vitro and In Vivo View paper
Discovery of Potent, Selective, and Orally Bioavailable Inhibitors of USP7 with In Vivo Antitumor Activity View paper
Discovery of Potent And Selective Inhibitors Of USP7 With Anti-Tumor Activity In Vitro And In Vivo. AACR 2019. View poster (PDF)
Discovery and Optimization of Potent and Selective Inhibitors of USP7 to Enhance Anti-Tumor Immunity and Target Tumor Growth. AACR 2018 on April 16, 2018. View poster (PDF)
Targeting the Stress Response Kinase GCN2 to Restore Immunity in the Tumor Microenvironment. AACR 2021. View poster (PDF)
Targeting the Stress Response Kinase GCN2 to Restore Immunity And Decrease Tumor Cell Survival SITC 2019. View poster (PDF)
Targeting the Stress Response Kinase GCN2 to Restore Immunity in the Tumor Microenvironment. AACR 2019. View poster (PDF)
Targeting the Stress Response Kinase GCN2 to Restore Immunity in the Tumor Microenvironment. Keystone Conference 2019. View poster (PDF)
Targeting the Stress Response Kinase GCN2 to Restore Immunity in the Tumor Microenvironment. SITC 2018 on November 9, 2018. View poster (PDF)