Dersimelagon

Dersimelagon is an agonist of melanocortin receptor 1 (MC1R).¹ It selectively induces cAMP accumulation in HEK293 cells expressing human MC1R (EC50 = 8.16 nM) over HEK293 cells expressing human MC2R (EC₅₀ = >10,000 nM) but also induces cAMP accumulation in HEK293 cells expressing human MC4R (EC₅₀ = 79.6 nM). Dersimelagon increases melanin levels in B16-F1 melanocytes (EC₅₀ = 13 pM). It increases eumelanin levels in the hair roots of, and induces coat darkening in, mice when administered at doses of 0.3 or 3 mg/kg per day. Dersimelagon (3 mg/kg per day) also decreases bleomycin-induced increases in skin thickness, skin levels of collagen, dermal levels of myofibroblasts, lung weight, and serum levels of pulmonary surfactant-associated protein D (PSP-D), adiponectin, matrix metalloproteinase-2 (Mmp-2), Mmp-3, P-selectin, Tnf receptor 1 (Tnfr1), and Tnfr2 in a mouse model of bleomycin-induced systemic sclerosis.²

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1. Suzuki, T., Kawano, Y., Matsumoto, A., et al. Melanogenic effect of dersimelagon (MT-7117), a novel oral melanocortin 1 receptor agonist. Skin Health Dis. 2(1), e78 (2021).

2. Kondo, M., Suzuki, T., Kawano, Y., et al. Dersimelagon, a novel oral melanocortin 1 receptor agonist, demonstrates disease-modifying effects in preclinical models of systemic sclerosis. Arthritis Res. Ther. 24(1), 210 (2022).