Benzamide derivative radiotracers targeting melanin for melanoma imaging and therapy: Preclinical/clinical development and combination with other treatments

Jacques Rouanet (1, 2, 3) , Mercedes Quintana (1) , Philippe Auzeloux (1) , Florent Cachin (1, 3) , Françoise Degoul (1)

1 IMoST - Imagerie Moléculaire et Stratégies Théranostiques
2 CHU Estaing [Clermont-Ferrand]
3 UNICANCER/CJP - Centre Jean Perrin [Clermont-Ferrand]

Cutaneous melanoma arises from proliferating melanocytes, cells specialized in the production of melanin. This property means melanin can be considered as a target for monitoring melanoma patients using nuclear imaging or targeted radionuclide therapy (TRT). Since the 1970s, many researchers have shown that specific molecules can interfere with melanin. This paper reviews some such molecules: benzamide structures improved to increase their pharmacokinetics for imaging or TRT. We first describe the characteristics and biosynthesis of melanin, and the main features of melanin tracers. The second part summarizes the preclinical and corresponding clinical studies on imaging. The last section presents TRT results from ongoing protocols and discusses combinations with other therapies as an opportunity for melanoma non-responders or patients resistant to treatments.

Mots clés: Benzamides; Imaging; Melanin; Metastatic melanoma; Radiopharmaceuticals; Targeted radionuclide therapy

Domaines: Sciences du Vivant [q-bio]; Cancer

Jacques Rouanet, Mercedes Quintana, Philippe Auzeloux, Florent Cachin, Françoise Degoul. Benzamide derivative radiotracers targeting melanin for melanoma imaging and therapy: Preclinical/clinical development and combination with other treatments. Alimentary Pharmacology & Therapeutics (Suppl), 2021, pp.107829. ⟨10.1016/j.pharmthera.2021.107829⟩. ⟨hal-03160223⟩