On March 8, 2022 Ryvu Therapeutics (WSE: RVU), a clinical-stage drug discovery and development company focusing on novel small molecule therapies that address emerging targets in oncology, reported that the data from its oncology programs will be presented at the upcoming American Association of Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting 2022, taking place April 8-13 in New Orleans, U.S (Press release, Ryvu Therapeutics, MAR 8, 2022, View Source [SID1234609724]).
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Posters to be presented at the conference will include data from RVU120, a CDK8/CDK19 inhibitor program targeting hematologic and solid tumors, and data from an MTA-cooperative PRMT5 inhibitor program.
"We are excited to share the recent preclinical data in breast cancer from our most advanced oncology program, RVU120. This selective inhibitor of CDK8/CDK19 is currently in Phase 1b clinical development for the treatment of acute myeloid leukemia or high-risk myelodysplastic syndromes, as well as in patients with metastatic or advanced solid tumors, and has already delivered promising data," said Krzysztof Brzózka, Chief Scientific Officer at Ryvu Therapeutics. "We have also made rapid progress in our MTA-cooperative PRMT5 inhibitor program, and we look forward to sharing these updates with the scientific community," adds Dr. Brzózka.
Abstract/Poster Details:
Title: RVU120, a selective CDK8/CDK19 inhibitor, demonstrates efficacy against hormone-independent breast cancer cells in vitro and in vivo
Abstract Number: 2647
RVU120 is a specific, low nM, selective inhibitor of CDK8/CDK19, currently being tested in a first-in-human Phase Ib clinical trial in patients with metastatic or advanced solid tumors progressing from previous lines of therapy (ClinicalTrials.gov: NCT05052255). Studies on a panel of cell lines representing various subtypes of breast cancer revealed that TNBC cells were highly sensitive to RVU120. Molecular profiling of responder cells indicated high enrichment for mesenchymal stem cells-like subtype. Single agent efficacy of RVU120 has been confirmed in subcutaneous TNBC xenograft models in vivo at well tolerated doses. Overall, these studies provide rationale for further development of RVU120 in TNBC patients.
Session Title: Novel Targets and Pathways
Session Date and Time: Tuesday Apr 12, 2022 9:00 AM – 12:30 PM
Location: Poster Section 24
Title: Discovery of novel MTA-cooperative PRMT5 inhibitors as a targeted therapeutic for MTAP deleted cancers
Abstract Number: 1117
Targeting PRMT5 in MTAP-deleted tumors in a synthetic lethal approach represents a promising antitumor strategy across many tumor types. Ryvu has identified a series of MTA-cooperative PRMT5 inhibitors with good drug-like physicochemical properties and block methyltransferase activity with nanomolar IC50 values. Ryvu compounds selectively inhibit the growth of MTAP deleted cancer cells in prolonged 3D culture, which strongly correlates with inhibition of PRMT5-dependent protein symmetric demethylation (SDMA) in those cells. Overall, these studies provide the rationale for the further optimization of chemical series towards a clinical candidate.
Session Title: Drug Targets
Session Date and Time: Monday Apr 11, 2022 1:30 PM – 5:00 PM
Location: Poster Section 23
Title: Trials in Progress – RVU120 SOL-021: An open-label, single agent, Phase I/II trial of RVU120 (SEL120) in patients with relapsed/refractory metastatic or advanced solid tumors
Abstract Number: 8023
SOL-021 is a Phase I/II clinical trial of RVU120 in patients with metastatic or advanced solid tumors, who have exhausted available treatments, currently ongoing in Poland and Spain (NCT05052255). The study is designed in 2 parts: Part 1 follows a 3+3 dose escalation design, and the primary objectives are to characterize the safety and tolerability of RVU120 as a single agent in patients with different tumors types and determine the RP2D. Part 2 will primarily explore the anti-tumor activity of RVU120 as a single agent in different patient populations. As of a data cutoff of 11 Feb 2022, 5 patients have been enrolled in Part 1 of the study and no DLTs have been observed.
This Trials in Progress abstract is published in cooperation with the Early Clinical Trials Centre and Department of Oncology and Radiotherapy, Medical University of Gdansk, Poland; Early Drug Development Unit (UITM) Vall d’Hebron Institute of Oncology (VHIO), Vall d’Hebron University Hospital, Barcelona, Spain; Dep. of Internal Medicine III, Univ. Clinic, Bonn, Germany and Maria Sklodowska-Curie Memorial Cancer Center and Institute of Oncology, Warsaw, Poland.
Session Title: Phase II Trials in Progress
Session Date and Time: Monday Apr 11, 2022 9:00 PM – 12:30 PM
Location: Poster Section 34
About AACR (Free AACR Whitepaper) Annual Meeting
The AACR (Free AACR Whitepaper) Annual Meeting program covers the latest discoveries across the spectrum of cancer research—from population science and prevention, to cancer biology, translational, and clinical studies; to survivorship and advocacy—and highlights the work of the best minds in research and medicine from institutions all over the world. Additional information is available on the AACR (Free AACR Whitepaper) conference website View Source