Remedy Plan Therapeutics has commenced dosing in a randomised Phase I trial of hyperbolic nicotinamide phosphoribosyltransferase (NAMPT) inhibitor, RPT1G, for cancers.

RPT1G is designed to target cells with elevated NAMPT levels found in certain cancers and other diseases.

The placebo-controlled, double-blind trial is being carried out in adult healthy volunteers in Australia and aims to assess the pharmacokinetic and safety properties of the therapy alongside exploring pharmacodynamic markers.

It is set to play a pivotal role in advancing the company’s oncology programme, particularly for acute myeloid leukaemia (AML) and high-risk myelodysplastic syndromes (MDS).

The findings, expected in the first half of next year, are set to fast-track the development of treatments for these conditions, with further trials planned for the second half.

RPT1G’s mechanism is designed to minimise on-target toxicity, thereby preserving the biological function in healthy cells.

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Preclinical models have shown that the therapy has a favourable tolerability and efficacy profile compared to other complete NAMPT inhibitors.

These studies provide evidence supporting its use in treating haematological malignancies. Furthermore, the therapy has demonstrated potential in overcoming cancer cell resistance to venetoclax, a standard care drug, suggesting a treatment benefit for leukaemia patients.

Remedy Plan Therapeutics CEO and founder Greg Crimmins said: “We are thrilled to initiate our Phase I trial of RPT1G in healthy subjects. RPT1G is not only the first hyperbolic NAMPT inhibitor but also the first NAMPT inhibitor to be tested in a healthy volunteer study, showcasing the importance of our preclinical work that clearly highlights the favourable safety profile of our hyperbolic NAMPT inhibitors.

“The results of this trial will enable us to initiate our subsequent trial in cancer patients at a starting dose that could provide meaningful therapeutic benefit.”

In addition to its implications for cancer treatment, RPT1G and its analogues are also being evaluated for their therapeutic potential in autoimmune and metabolic diseases.