Anagliptin

Anagliptin is an inhibitor of dipeptidyl peptidase 4 (DPP-4; IC₅₀ = 3.8 nM).¹ It is selective for DPP-4 over DPP-8 and DPP-9 (IC₅₀s = 68 and 60 nM, respectively). Dietary administration of anagliptin (0.05 and 0.3% w/w) decreases plasma DPP-4 activity, increases plasma GLP-1 levels, suppresses food intake and body weight gain, ameliorates insulin resistance, and improves glucose tolerance in wild-type and glucokinase knockout mouse models of high-fat diet-induced diabetes.² It decreases hepatic lipid and M1 macrophage accumulation and prevents hepatic fibrosis and steatohepatitis in mice fed a high-cholesterol high-fat diet or a choline-deficient L-amino acid-defined, high-fat (CDAHF) diet.³ Anagliptin also reduces atherosclerotic lesion size in an Apoe^-/- mouse model of atherosclerosis.⁴

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1. Kato, N., Oka, M., Murase, T., et al. Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor. Bioorg. Med. Chem. 19(23), 7221-7227 (2011).

2. Nakaya, K., Kubota, N., Takamoto, I., et al. Dipeptidyl peptidase-4 inhibitor anagliptin ameliorates diabetes in mice with haploinsufficiency of glucokinase on a high-fat diet. Metabolism 62(7), 939-951 (2013).

3. Sakai, Y., Chen, G., Ni, Y., et al. DPP-4 inhibition with anagliptin reduces lipotoxicity-induced insulin resistance and steatohepatitis in male mice. Endocrinology 161(10), bqaa139 (2020).

4. Ervinna, N., Mita, T., Yasunari, E., et al. Anagliptin, a DPP-4 inhibitor, suppresses proliferation of vascular smooth muscles and monocyte inflammatory reaction and attenuates atherosclerosis in male apo E-deficient mice. Endocrinology 154(3), 1260-1270 (2013).