Rgenix has treated the first patient in a Phase Ia/b study of RGX-202 for the treatment of gastrointestinal cancers.
The open-label, non-randomised, dose-escalation trial will evaluate RGX-202 alone and in combination with chemotherapy.
Rgenix intends to enrol around 60 patients with advanced gastrointestinal tumours who have had progressive disease on available therapies, or where there are no standard systemic therapies available.
The expansion stage of the trial will see the treatment of additional patients with advanced gastrointestinal malignancies at the recommended Phase II dose to determine the safety, efficacy, pharmacokinetics (PK), and pharmacodynamics of RGX-202 as a single agent and as a combination therapy.
Primary endpoints of the trial are maximum tolerated dose, overall response rate, and treatment-emergent adverse events.
The trial’s secondary endpoints include maximum plasma concentration, and area under the curve.
Rgenix chief medical officer Roger Waltzman said: “The launch of our Phase I trial for RGX-202 is a result of our commitment at Rgenix to develop treatments for patients suffering from prevalent cancers that lack effective therapies.”
RGX-202 is an investigational oral small molecule designed to inhibit a cancer metabolism pathway involved in supplying energy to cancer cells. It targets SLC6a8, a creatine transporter.
Creatine metabolism, driven by SLC6a8 and creatine kinase CKB, has been implicated in the development of gastrointestinal cancers.
RGX-202 has also shown efficacy in KRAS mutant tumour models that are usually resistant to approved therapies.