Basilea initiates trial of derazantinib to treat urothelial cancer

Derazantinib is an oral, investigational small molecule designed to block pan-fibroblast growth factor receptor (FGFR) kinase. The compound is said to possess strong activity against FGFR1, 2, and 3.

The therapeutic also inhibits the colony-stimulating factor 1 receptor kinase (CSF1R). Basilea licensed the product from ArQule last April.

Atezolizumab is a PD-L1-blocking immune checkpoint inhibitor that will be supplied by Roche.

According to Basilea, in-vitro data showed that derazantinib could boost the response to atezolizumab’s PD-L1 checkpoint inhibition.

Named FIDES-02, the multi-cohort, open-label Phase I/II study will be sponsored by Basilea. The trial will assess the efficacy of derazantinib alone and as a combination to treat advanced urothelial cancer patients.

Up to 300 participants testing positive for FGFR1, FGFR2, or FGFR3 gene mutations or fusions will be enrolled across Europe, North America, and Asia.

The primary outcomes of the study are overall response rate (ORR) and the recommended Phase II dose (RP2D) of derazantinib in combination with atezolizumab.

The trial will also measure disease control rate, duration of response, progression-free survival (PFS), and overall survival (OS) at six months, along with the drug’s safety and tolerability.

Basilea Pharmaceutica chief medical officer Dr Marc Engelhardt said: “Patients with advanced urothelial cancer currently have limited treatment options and there is a high unmet medical need, especially for targeted therapies in this common type of cancer.

“This is the first clinical study in which we are exploring derazantinib in combination with atezolizumab. This combination may become a promising new targeted treatment approach for patients with urothelial cancer.”

The trial is expected to be completed in May 2022.