PMID- 25050065 OWN - NLM STAT- PubMed-not-MEDLINE DCOM- 20140722 LR - 20211021 IS - 1176-6336 (Print) IS - 1178-203X (Electronic) IS - 1176-6336 (Linking) VI - 10 DP - 2014 TI - Profile of saxagliptin in the treatment of type 2 diabetes: focus on Japanese patients. PG - 547-58 LID - 10.2147/TCRM.S46076 [doi] AB - Saxagliptin is a selective and potent dipeptidyl peptidase (DPP)-4 inhibitor, approved as an adjunct to diet and exercise to improve glycemic control in type 2 diabetes mellitus (T2DM) in the USA on July 2009, and had been launched globally in over 86 countries by September 2013. In patients with T2DM, once-daily administration of saxagliptin before breakfast achieves sustained inhibition of plasma DPP-4 activity and reduction of postprandial hyperglycemia, including after dinner, associated with an increase in plasma glucagon-like peptide-1 levels. This paper reviews the safety and efficacy of saxagliptin in Japanese patients with T2DM. The clinical development study in Japan supported its usefulness for the disease. Saxagliptin 1, 2.5, and 5 mg led to significant improvements in glycated hemoglobin (HbA1c), and was generally well tolerated. Treatment with saxagliptin 5 mg induced a sustained reduction in HbA1c over 52 weeks. Long-term combination therapy with saxagliptin and other oral hypoglycemic agents also provided sustained glycemic control and was well tolerated for up to 52 weeks. Saxagliptin as add-on to sulfonylureas or glinides has a tendency to increase hypoglycemia, but not with other oral antidiabetic agents, such as alpha-glucosidase inhibitors, metformin, or thiazolidinediones. The results of clinical trials have confirmed the long-term efficacy and safety of saxagliptin monotherapy as well as its use as add-on combination therapy, and support its usefulness as a therapeutic agent for T2DM. Saxagliptin has less concern for hypoglycemia and weight gain, which often becomes problematic in routine care of T2DM. Meta-analysis of clinical trials in the USA showed no evidence of increased risk of cardiovascular events associated with saxagliptin, suggesting the superior of saxagliptin in terms of safety. Recently, investigators in the SAVOR-TIMI (Saxagliptin Assessment of Vascular Outcomes Recorded in Patients with Diabetes Mellitus-Thrombolysis in Myocardial Infarction) 53 study suggested that DPP-4 inhibition with saxagliptin did not increase or decrease the rate of ischemic events, although the rate of hospitalization for heart failure was increased. Although saxagliptin improves glycemic control, other approaches are necessary to reduce cardiovascular risk in patients with diabetes. Saxagliptin is applicable for various pathological conditions, and is considered to be clinically significant as a new therapeutic option for Japanese patients with T2DM. FAU - Konya, Hiroyuki AU - Konya H AD - Department of Internal Medicine, Ashiya Municipal Hospital, Ashiya, Japan. FAU - Yano, Yuzo AU - Yano Y AD - Department of Internal Medicine, Ashiya Municipal Hospital, Ashiya, Japan. FAU - Matsutani, Satoshi AU - Matsutani S AD - Department of Internal Medicine, Ashiya Municipal Hospital, Ashiya, Japan. FAU - Tsunoda, Taku AU - Tsunoda T AD - Division of Diabetes, Endocrinology and Metabolism, Department of Internal Medicine, Hyogo College of Medicine, Nishinomiya, Japan. FAU - Ikawa, Takashi AU - Ikawa T AD - Division of Diabetes, Endocrinology and Metabolism, Department of Internal Medicine, Hyogo College of Medicine, Nishinomiya, Japan. FAU - Kusunoki, Yoshiki AU - Kusunoki Y AD - Division of Diabetes, Endocrinology and Metabolism, Department of Internal Medicine, Hyogo College of Medicine, Nishinomiya, Japan. FAU - Matsuo, Toshihiro AU - Matsuo T AD - Division of Diabetes, Endocrinology and Metabolism, Department of Internal Medicine, Hyogo College of Medicine, Nishinomiya, Japan. FAU - Miuchi, Masayuki AU - Miuchi M AD - Division of Diabetes, Endocrinology and Metabolism, Department of Internal Medicine, Hyogo College of Medicine, Nishinomiya, Japan. FAU - Katsuno, Tomoyuki AU - Katsuno T AD - Division of Innovative Diabetes Treatment, Hyogo College of Medicine, Nishinomiya, Japan. FAU - Hamaguchi, Tomoya AU - Hamaguchi T AD - Division of Diabetes, Department of Internal Medicine, Itami City Hospital, Itami, Hyogo, Japan. FAU - Miyagawa, Jun-Ichiro AU - Miyagawa J AD - Division of Diabetes, Endocrinology and Metabolism, Department of Internal Medicine, Hyogo College of Medicine, Nishinomiya, Japan. FAU - Namba, Mitsuyoshi AU - Namba M AD - Division of Diabetes, Endocrinology and Metabolism, Department of Internal Medicine, Hyogo College of Medicine, Nishinomiya, Japan. LA - eng PT - Journal Article PT - Review DEP - 20140711 PL - New Zealand TA - Ther Clin Risk Manag JT - Therapeutics and clinical risk management JID - 101253281 PMC - PMC4103926 OTO - NOTNLM OT - Japan OT - dipeptidyl peptidase-4 OT - efficacy OT - incretin hormones OT - patient acceptability OT - safety OT - saxagliptin OT - type 2 diabetes mellitus EDAT- 2014/07/23 06:00 MHDA- 2014/07/23 06:01 PMCR- 2014/07/11 CRDT- 2014/07/23 06:00 PHST- 2014/07/23 06:00 [entrez] PHST- 2014/07/23 06:00 [pubmed] PHST- 2014/07/23 06:01 [medline] PHST- 2014/07/11 00:00 [pmc-release] AID - tcrm-10-547 [pii] AID - 10.2147/TCRM.S46076 [doi] PST - epublish SO - Ther Clin Risk Manag. 2014 Jul 11;10:547-58. doi: 10.2147/TCRM.S46076. eCollection 2014.