Scientific Publications
| Zelnecirnon (RPT193) | |
| Clinical and molecular effects of oral CCR4 antagonist RPT193 in atopic dermatitis: A Phase 1 study. Allergy, November 2023 | View paper (PDF)  |
| Treatment with the Oral CCR4 Antagonist RPT193 Results in Meaningful Changes in Cutaneous Biomarkers Detected by Transcriptomic Profiling of Tape-Strips. ISDS 2023 | View presentation (PDF) View poster (PDF) |
| 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) View poster (PDF) |
| 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) View presentation video |
| 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) View presentation video |
| FLX193: A Potent, Selective CCR4 Antagonist for Allergic Disorders | View poster (PDF) |
| Tivumecirnon (FLX475) | |
| Phase 2 Study of Oral CCR4 Antagonist FLX475 (tivumecirnon) Plus Pembrolizumab in Subjects with Head and Neck Squamous Cell Carcinoma (HNSCC) Previously Treated with Checkpoint Inhibitor. Forum: AACR 2024. | View presentation (PDF) |
| A Combined mregDC and Treg Signature Associates with Antitumor Efficacy of CCR4 Antagonist Tivumecirnon FLX475. Forum: AACR 2024. | View presentation (PDF) |
| Phase 2 safety and efficacy of oral CCR4 antagonist FLX475 (tivumecirnon) plus pembrolizumab in subjects with non-small cell lung cancer not previously treated with checkpoint inhibitor. Forum: SITC 2023. | View presentation (PDF) |
| Biological activity of FLX475, an oral CCR4 antagonist, as monotherapy and in combination with pembrolizumab in advanced cancer. Forum: SITC 2023. | View presentation (PDF) |
| Clinical And Biological Activity Of FLX475, An Oral CCR4 Antagonist, In Combination With Pembrolizumab In Advanced Cancer. Forum: CICON 2023. | View presentation (PDF) |
| Clinical and Biological Activity of FLX475, an Oral CCR4 Antagonist, in Advanced Cancer. ASCO 2023 | View presentation (PDF) |
| Phase 1/2 study of the oral CCR4 antagonist, FLX475, as monotherapy and in combination with pembrolizumab in advanced cancer. 2022 ESMO-IO | View presentation (PDF) |
| 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) |
| HPK1 | |
| HPK1 inhibits CD8+ T cell effector gene expression following T cell activation. AACR 2024. | View poster (PDF) |
| 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) |