La Chaux-de-Fonds, Switzerland, Dec. 05, 2017 (GLOBE NEWSWIRE) -- Rhizen Pharmaceuticals S.A., today announced that updated data for RP6530 (tenalisib), the Company’s highly selective and orally active dual PI3K delta/gamma inhibitor, and RP4010, the Company’s novel, first-in-class oral small molecule inhibitor of calcium release-activated calcium (CRAC) channel, have been selected for poster presentations at the upcoming 59th American Society of Hematology (ASH) annual meeting, to be held December 9-12, 2017, at the Georgia World Congress Center in Atlanta, GA, USA. Abstracts are available online and can be accessed on the ASH meeting website at www.hematology.org. Clinical and preclinical abstract highlights as well as the details of posters to be presented at ASH are outlined below:
Clinical Abstract Highlights:
- RP6530 (tenalisib) updated data from ongoing Phase I/IB study: Demonstrated highly promising single-agent clinical activity with acceptable safety in relapsed/refractory T-cell Lymphoma.
- R/R Peripheral T-cell Lymphoma (R/R PTCL) objective response rate (ORR) = 58%
- R/R Cutaneous T-cell Lymphoma (R/R CTCL) objective response rate (ORR) = 56%
Preclinical Abstract Highlights:
- RP6530 (tenalisib): RNA sequencing analysis in Hodgkin Lymphoma (HL) cell lines demonstrate that RP6530 can affect both HL tumor cells and their microenvironment. RP6530 inhibits chemokines and cytokines capable of stimulating and recruiting myeloid cells, blocks JAK/STAT pathway and strikingly reduces the expression of Pyruvate kinase muscle isozyme M2 (PKM2). In addition, RP6530 increased the expression of M1 markers, switching the activation of macrophages from an immunosuppressive M2-like phenotype to an inflammatory M1-like state.
- RP4010: Highly promising data in Diffuse Large B Cell Lymphoma (DLBCL) cell lines and in vivo mouse xenograft model. Gene expression analysis revealed a strong correlation between ORAI1 expression and sensitivity to RP4010-induced cell death. Preclinical data supports the ongoing multi-center Phase I/IB dose-escalation trial evaluating the safety and efficacy of RP4010, a CRAC channel inhibitor in patients with relapsed or refractory Non-Hodgkin Lymphoma (NHL) in USA (ClinicalTrials.gov Identifier: NCT03119467)
Details of the poster presentations:
- Poster Title: Safety and Anti-Tumor Activity of RP6530, Dual PI3K d/g Inhibitor, in Relapsed/Refractory T-cell Lymphoma: Updated Results from the Dose Expansion Cohort of an on-Going Phase I/Ib Study
- Abstract Number: 2791
- Session: 624. Hodgkin Lymphoma and T/NK Cell Lymphoma – Clinical Studies: Poster II
- Date and Time: Sunday, December 10, 2017; 6:00 PM – 8:00 PM US EST
- Location: Bldg A, Lvl 1, Hall A2 (Georgia World Congress Center)
- Presenter: Yasuhiro Oki, MD, University of Texas MD Anderson Cancer Center, Houston, TX
- Poster Title: RNA Sequencing Reveals Mechanisms Underlying Modulation of Hodgkin Lymphoma Cells and Tumor Microenvironment By the PI3K d/g inhibitor, RP6530
- Abstract Number: 2476
- Session: 602. Disordered Gene Expression in Hematologic Malignancy, including Disordered Epigenetic Regulation: Poster II
- Date and Time: Sunday, December 10, 2017; 6:00 PM – 8:00 PM US EST
- Location: Bldg A, Lvl 1, Hall A2 (Georgia World Congress Center)
- Presenter: Silvia Locatelli, Ph.D., Humanitas Clinical and Research Center, Rozzano, Italy
- Poster Title: The Novel Calcium Release-Activated Calcium (CRAC) Channel Inhibitor RP4010 Exerts Potent Antitumor Effects in NOD/SCID/IL2Rg -/- Mice with Diffuse Large B Cell Lymphoma (DLBCL) Cell Line Xenografts
- Abstract Number: 4101
- Session: 625. Lymphoma: Pre-Clinical – Chemotherapy and Biological Agents: Poster III
- Date and Time: Monday, December 11, 2017; 6:00 PM – 8:00 PM US EST
- Location: Bldg A, Lvl 1, Hall A2 (Georgia World Congress Center)
- Presenter: Silvia Locatelli, Ph.D., Humanitas Clinical and Research Center, Rozzano, Italy
About RP6530 (tenalisib):
RP6530 (tenalisib) is a highly selective and orally active dual PI3K delta/gamma inhibitor with efficient translation of activity through enzyme, cell, and whole blood-based studies. Besides inhibiting growth of immortalized cancerous cell lines and primary patient leukemic/lymphoma cells, RP6530 plays a significant role in modulation of tumor microenvironment at clinically achievable concentrations. In preclinical studies, RP6530 reprograms macrophages from an immunosuppressive M2-like phenotype (pro-tumor) to an inflammatory M1-like state (anti-tumor), which can potentially enhance the activity of checkpoint inhibitors or overcome resistance to these drugs.
About RP4010:
RP4010 is a novel first-in-class oral small molecule inhibitor of calcium release activated calcium (CRAC) channel pathway with demonstrated preclinical activity in a broad range of cancers. Aberrant CRAC channel activity has been linked to various autoimmune disorders and certain cancers via the NFAT pathway. In addition, the blockage of store-operated calcium entry (SOCE) by a CRAC channel inhibitor could suppress tumor growth through a number of mechanisms, including the inhibition of calcium-dependent activation of Akt/NF-kB and ERK 1/2 pathways.
About Rhizen Pharmaceuticals S.A.:
Rhizen Pharmaceuticals is an innovative, clinical-stage biopharmaceutical company focused on the discovery and development of novel therapeutics for the treatment of cancer, immune and metabolic disorders. Since its establishment in 2008, Rhizen has created a diverse pipeline of proprietary drug candidates targeting several cancers and immune associated cellular pathways. Rhizen is headquartered in La-Chaux-de-Fonds, Switzerland. For additional information, please visit Rhizen’s website, www.rhizen.com.