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Anti-Diabetic Drugs
Published in Awanish Kumar, Ashwini Kumar, Diabetes, 2020
Another ‘incretin’-based therapy includes the DPP-4 inhibitors or the ‘gliptin’ class of drugs, which are oral anti-diabetic medications. DPP-4 is an enzyme present as a transmembrane protein that acts upon the endogenous incretins such as GLP-1 and degrades them. It is due to this enzyme that the half-life of endogenous GLP-1 is almost 5 minutes, which is pharmacologically much less. Thus, inhibition of DPP-4 results in the natural action of endogenous GLP-1 which enhances the insulin secretion. Sitagliptin (Januvia; Merck) was the first drug in this class to be approved by the US FDA in 2006, followed by vildagliptin (Galvus; Novartis) in 2007 [1,15]. Other DPP-4 inhibitors are saxagliptin (Onglyza; AstraZeneca), alogliptin (Nesina; Takeda Pharmaceuticals), linagliptin (Tradjenta; Eli Lilly), trelagliptin (Zafatek; Takeda Pharmaceuticals) and teneligliptin (Tenelia; Daiichi Sankyo). The dosage regimens of these DPP-4 inhibitors are as follows: Sitagliptin (25/50/100 mg once daily), saxagliptin (2.5/5 mg once daily), vildagliptin (50/100 mg per day, not exceeding 100 mg daily), alogliptin (25 mg once daily), linagliptin (5 mg once daily), trelagliptin (100 mg once weekly) and teneligliptin (20 mg once daily). These DPP-4 inhibitors have been used as monotherapy or in combination with metformin, sulphonylureas, TZDs and insulin [16–23]. According to various studies and reports, the major adverse effects associated with DPP-4 inhibitors are pancreatitis, renal problems and even heart failure, which have also been put on the FDA warning list [24]. Therefore, these drugs should be used very cautiously in patients.
Biocatalyzed Synthesis of Antidiabetic Drugs
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Teneligliptin 47 is a DPP4-inhibitor initially developed by Mitsubishi Tanabe Pharma under the name of Tenelia™ (recently available also in Argentina (Teneglucon™), and India (Tenepure™; Teneza™) at relatively affordable price, with an unique structure characterized by five consecutive rings, explaining its powerful activity and its extremely long half-life (24.2 h), with resulting DPP-4 inhibition throughout the day (Scott, 2015; Pujadas et al., 2016; Sharma et al., 2016). Gosogliptin 52 was developed by Pfizer, but it was discontinued in 2012 in Phase II trials; in June 2012, exclusive rights were granted to SatRx LLC, a Russian company, for further development, and it was launched in Russian market in 2016 under the trade name SatRx™.
Advances in pharmacotherapy for acute kidney injury
Published in Expert Opinion on Pharmacotherapy, 2022
Yali Xu, Ping Zou, Xiaojing Cao
Dipeptidyl peptidase (DPP-4) inhibitors are regulatory serine proteases that cut the N-terminal dipeptides of various hormones, cytokines, chemokines, neuropeptides, and growth factors, thus regulating the biological half-life and activity of these polypeptides. The DPP-4 inhibitor teneligliptin was clinically used for type 2 diabetes, and it was recently founded that it is protective against the kidney [23]. DPP-4 is expressed primarily in pro-inflammatory M1 macrophages, while DPP-4 inhibitors induce M2 macrophages polarization [24], and promote the repair of damaged renal tubular segments. Linagliptin protected against endotoxin-induced AKI by reducing ROS via AMPK pathway activation and suppressing the release of TNF-α and IL-1β [25]. Preclinical experiment showed that DPP-4 inhibitor pretreatment reduced the risk of renal ischemia/reperfusion injury in diabetic rats [26]. In addition, clinical statistical analysis showed that the risk of AKI was decreased to varying degrees in patients with diabetes treated with DPP-4 inhibitors [27]. Given the hypoglycemic action of DPP-4 inhibitors, they may not be suitable for patients with normal glucose.
Safety and efficacy of long-term treatment with teneligliptin: Interim analysis of a post-marketing surveillance of more than 10,000 Japanese patients with type 2 diabetes mellitus
Published in Expert Opinion on Pharmacotherapy, 2018
Takashi Kadowaki, Masakazu Haneda, Hiroshi Ito, Makoto Ueno, Miyuki Matsukawa, Tomoko Yamakura, Kazuyo Sasaki, Mayumi Kimura, Hiroaki Iijima
Adult subjects with T2DM, who were treatment-naïve for teneligliptin and who were subsequently prescribed teneligliptin by their physician for the treatment of T2DM, were eligible for registration to this PMS. Teneligliptin was prescribed in accordance with the approved label, which states that the usual adult dosage is 20 mg administered orally, once daily. If the efficacy of teneligliptin 20 mg/day was considered by the physician to be insufficient, the label permitted an increase in dosage up to 40 mg once daily, with close monitoring of the clinical course. All treatment decisions were made at the discretion of physicians. This survey involved the collection of anonymous data from clinical settings; thus, in compliance with Japanese regulations for PMS, it was not necessary to obtain informed consent from patients.
Potential approaches using teneligliptin for the treatment of type 2 diabetes mellitus: current status and future prospects
Published in Expert Review of Clinical Pharmacology, 2023
Harmanjit Singh, Jasbir Singh, Ravneet Kaur Bhangu, Mandeep Singla, Jagjit Singh, Farideh Javid
Teneligliptin offers many beneficial effects, in addition to its anti-diabetic effect. Although these effects are not the indications for teneligliptin therapy, these are additional effects that can be promising in the treatment of patients suffering from multiple health conditions in addition to T2DM.