BASEL, Switzerland– Rhizen Pharmaceuticals AG (Rhizen), a Switzerland-based privately held, clinical-stage oncology & inflammation-focussed biopharmaceutical company announced today that it has commenced dosing in a phase II trial to evaluate Tenalisib (RP6530; isoform selective dual PI3K δ/γ inhibitor with additional SIK3 activity) in patients with locally advanced or metastatic breast cancer. This multi-center, randomized phase II study is being conducted in eastern Europe and is designed to assess Tenalisib’s anti-tumor activity and safety across two dose levels. The study also includes translational assessments intended to delineate the effect of Tenalisib’s multivalent mechanism on relevant cytokines/chemokine levels and gene expression changes within the tumor microenvironment.
Rhizen indicated that Tenalisib, in addition to its selective dual PI3K δ/γ inhibitory activity, also has Salt-Inducible Kinase 3 (SIK3) activity via its principal metabolite, that could potentially contribute to its chemo-sensitization effect as observed in its preclinical studies, especially in breast cancer. Rhizen hopes to establish the single agent activity of Tenalisib in this current study after which it plans to expand the assessment across additional solid tumor indications and combinations both with chemotherapeutic agents and with immune-checkpoint inhibitors.
“PI3K inhibition continues to remain a relevant therapeutic intervention across tumor types given the importance of its signalling in tumor development. We have demonstrated our ability to develop safe and differentiated isoform selective PI3K inhibitors that can withstand the rigors of development and be integrated into clinical practice” said Swaroop Vakkalanka, Founder & CEO of Rhizen Pharma. Swaroop also added that “This is a sentinel study that we expect will pave the way for Tenalisib’s potential to be expanded beyond haematological cancers into solid tumors, given its stellar safety profile, multivalent activity and consequent combinability.”
