Challenge: Improving efficiency of low molecular weight radioligands for cancer therapy

Debiopharm, the Seeker for this Innocentive Challenge, is looking for novel broadly applicable approaches to reducing the renal reabsorption of low-molecular weight radioligands, in particular small-peptide radioligands or small-peptidomimetic radioligands, as a means of improving the efficiency and safety of these types of compounds in cancer therapy.

A hospital lab.

A hospital lab. Image credit: Pavel Danilyuk via Pexels, free license

In recent years, low-molecular weight radioligands, e.g. small-peptide radioligands or small-peptidomimetic radioligands, have emerged as a promising approach to treat cancers that are characterized by overexpression of specific surface targets. Prostate cancer and neuroendocrine tumors are typical examples of this type of cancer.

However, such compounds face a major physiological hurdle: renal reabsorption. Due to their small size these radioligands are freely filtered through renal glomeruli and can be actively reabsorbed in renal cells, resulting in renal radiotoxicity and renal impairment, or even renal failure.

Current approaches to reducing the renal absorption of low-molecular weight radioligands, e.g. small-peptide radioligands or small-peptidomimetic radioligands, are insufficient; novel broadly applicable approaches are therefore needed. Finding such approaches is the objective of this Challenge.

Submissions to this Challenge must be received by 11:59 PM (US Eastern Time) on February 2nd, 2026.

Source: InnoCentive