Janagliflozin (DB16209): A Comprehensive Pharmacological and Clinical Monograph

Executive Summary

Janagliflozin (DrugBank ID: DB16209) is a novel, orally administered, selective small-molecule inhibitor of the sodium-glucose cotransporter 2 (SGLT2). Developed by Sihuan Pharmaceutical's subsidiary, Huisheng Biopharmaceutical, it is designated as a national Class 1 innovative drug in China.[1] In January 2024, Janagliflozin, under the trade name Huiyoujing®, received drug registration approval from the National Medical Products Administration (NMPA) of China for the treatment of Type 2 Diabetes Mellitus (T2DM). This approval covers its use as both monotherapy and in combination with metformin.[1] The drug remains investigational in other global regions.[2]

Consistent with its therapeutic class, Janagliflozin exerts its antihyperglycemic effect through an insulin-independent mechanism. It selectively inhibits SGLT2 in the proximal renal tubules, which reduces the reabsorption of glucose from the glomerular filtrate, thereby promoting urinary glucose excretion (glucosuria) and lowering plasma glucose concentrations.[5] This mechanism confers a low intrinsic risk of hypoglycemia.

Pivotal Phase 3 clinical trials conducted in Chinese patients with T2DM have demonstrated robust efficacy. As a monotherapy in drug-naive patients, Janagliflozin at 25 mg and 50 mg daily doses achieved statistically significant, placebo-adjusted glycated hemoglobin (HbA1c​) reductions of -0.80% and -0.88%, respectively.[7] When used as an add-on therapy to metformin in patients with inadequate glycemic control, both the 25 mg and 50 mg doses provided an identical placebo-adjusted

HbA1c​ reduction of -0.58%.[8] This glycemic efficacy is accompanied by clinically significant pleiotropic benefits, including reductions in body weight and systolic blood pressure, which are characteristic of the SGLT2 inhibitor class.[7]