Rhizen Pharmaceuticals S.A. to present Phase 1 clinical and additional preclinical data of RP6530 (dual PI3K delta/gamma inhibitor) in hematological malignancies

La Chaux-de-Fonds, Switzerland, Dec. 3, 2014 (GLOBE NEWSWIRE) -- Rhizen Pharmaceuticals S.A. announces Phase 1 clinical and additional preclinical data presentations for RP6530, a novel dual PI3K delta/gamma inhibitor in hematological malignancies

--- Two posters to be presented at the 56th American Society of Hematology (ASH) Annual Meeting & Exposition, December 6-9, 2014, Moscone Center, San Francisco, CA

Phase 1 clinical study:

---  In the ongoing Phase 1 study in Europe, RP6530 demonstrated excellent safety across four dose levels;25 mg BID, 50 mg BID, 100 mg BID and 200 mg BID.  No increase in ALT/AST, colitis, pneumonia, or drug related neutropenia reported among treated patients

 --- Clinical efficacy was manifested by a significant reduction in peripheral blood cell pAKT expression levels across all doses.   MTD has not been reached and dose escalation continues at 400 mg BID

--- Despite the heavy pre-treatment (median 5) and disease burden, oral administration of RP6530 controlled tumor progression in 75% patients

Preclinical data in combination with ibrutinib (IMBRUVICA ® ) in DLBCL cell lines:

--- Data demonstrated single-agent activity of RP6530 as well as synergism with ibrutinib in DLBCL representative cell lines

--- Addition of RP6530 overcomes ibrutinib resistance in DLBCL cells in vitro.  Combining RP6530 with ibrutinib therefore appears to be a potential therapeutic approach aimed at circumventing resistance emerging in patients after prolonged ibrutinib therapy

About RP6530:

RP6530 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.  A Phase 1 dose-escalation trial evaluating the safety and efficacy of RP6530 in patients with relapsed/refractory hematological malignancies is currently ongoing (ClinicalTrials.gov Identifier: NCT02017613).

Details of the poster presentations:

-- Poster Title:  A Phase 1 Dose Escalation Study of RP6530, a Novel, Dual PI3K -γδ Inhibitor, for Patients with Relapsed or Refractory Hematologic Malignancies

·      Poster Session:                    623. Lymphoma: Chemotherapy, excluding Pre-Clinical Models: Poster II                                                

·      Presentation Date:               07 December 2014

·      Time:                                   6:00 - 8:00 PM Pacific Standard Time

·      Poster Board Number:        3043

·      Place:                                   West Building, Level 1 (Moscone Center)

-- Poster Title:  Addition of RP6530, a Dual PI3K δ/γ Inhibitor, Overcomes Ibrutinib Resistance in DLBCL Cells in Vitro

·      Poster Session:                    625. Lymphoma: Pre-Clinical - Chemotherapy and Biologic Agents: Poster III

·      Presentation Date:               08 December 2014

·      Time:                                   6:00 - 8:00 PM Pacific Standard Time

·      Poster Board Number:         4497

·      Place:                                   West Building, Level 1 (Moscone Center)

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.


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