NEW YORK – Rhizen Pharmaceuticals on Wednesday dosed the first patient in a Phase II trial of tenalisib, an isoform selective dual PI3K inhibitor with additional SIK3 activity, in patients with advanced or metastatic breast cancer.
Rhizen, headquartered in Basel, Switzerland, will evaluate tenalisib at two dose levels in the 40-patient trial in Europe. Patients with HER2-positive breast cancer will be excluded from the study. Researchers will assess tenalisib's effect on relevant cytokines and chemokine levels and gene expression changes within patients' tumor microenvironment.
In the trial, researchers are primarily interested in assessing the proportion of patients who are without disease progression after six months of tenalisib therapy. They will also measure patients' overall response rate, clinical benefit rate, progression-free survival, and adverse events on treatment.
In preclinical studies, tenalisib's mechanism of action has demonstrated a chemo-sensitization effect in breast cancer models. The company hopes to establish tenalisib's single-agent activity in breast cancer in this Phase II trial before studying it in other solid tumors and exploring its activity in combination with chemotherapy or checkpoint inhibitors.
Tenalisib has fast-track and orphan drug status from the US Food and Drug Administration as an investigational treatment for relapsed or refractory peripheral T-cell lymphoma and cutaneous T-cell lymphoma, and has demonstrated activity in both these indications in a Phase II trial. The latest Phase II trial "is a sentinel study that we expect will pave the way for tenalisib's potential to be expanded beyond hematological cancers into solid tumors, given its stellar safety profile, multivalent activity, and consequent combinability," Rhizen CEO Swaroop Vakkalanka said in a statement.
In October 2020, Rhizen entered into an exclusive licensing agreement with Curon Biopharmaceutical, allowing Curon to develop and commercialize tenalisib across all oncology indications in greater China.