TRADJENTA
Manufacturer:
Boehringer Ingelheim and Lilly
Pharmacological Class:
Dipeptidyl peptidase-4 inhibitor (DPP-4).
Active Ingredient(s):
Linagliptin 5mg; tabs.
Indication(s):
Adjunct to diet and exercise in type 2 diabetes mellitus, as monotherapy or combination therapy.
Pharmacology:
Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Thus, linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon in the circulation.
Clinical Trials:
Linagliptin was studied in approximately 3800 patients with type 2 diabetes in 8 double-blind, placebo-controlled safety and efficacy trials.
A total of 730 patients participated in two studies, one of 18-week and another of 24-week duration, to evaluate the efficacy and safety of linagliptin monotherapy. Treatment with linagliptin 5mg daily provided statistically significant improvements in A1C, FPG, and 2-hour PPG compared with placebo.
A total of 701 patients participated in a 24-week study designed to assess the efficacy of linagliptin in combination with metformin. In combination with metformin, linagliptin provided statistically significant improvements in A1C, FPG, and 2-hour PPG compared with placebo.
The efficacy of linagliptin is being evaluated in a 104-week double-blind, glimepiride-controlled non-inferiority study in type 2 diabetic patients with insufficient glycemic control despite metformin therapy. After 52 weeks, linagliptin and glimepiride both had reductions from baseline in A1C (-0.4% for linagliptin, -0.6% for glimepiride) from a baseline mean of 7.7%.
A total of 389 patients participated in a 24-week study designed to assess the efficacy of linagliptin in combination with pioglitazone. In initial combination with pioglitazone 30mg, linagliptin 5mg provided statistically significant improvements in A1C and FPG compared to placebo with pioglitazone.
A total of 245 patients participated in an 18-week study designed to assess the efficacy of linagliptin in combination with a sulfonylurea. In combination with a sulfonylurea, linagliptin provided statistically significant improvements in A1C compared with placebo following 18 weeks treatment; the improvements in FPG observed with linagliptin were not statistically significant compared with placebo.
A total of 1058 patients participated in a 24-week study designed to assess the efficacy of linagliptin in combination with a sulfonylurea and metformin. In combination with a sulfonylurea and metformin, linagliptin provided statistically significant improvements in A1C and FPG compared with placebo.
Legal Classification:
Rx
Adults:
5mg once daily.
Children:
Not recommended.
Warnings/Precautions:
Not for the treatment of type 1 diabetes or diabetic ketoacidosis. Pregnancy (Cat. B). Nursing mothers.
Interaction(s):
Antagonized by strong P-gp or CYP3A4 inducers (eg, rifampin); consider alternatives to linagliptin if used in combination. Concomitant sulfonylurea: may need lower dose of sulfonylurea to reduce risk of hypoglycemia. Concomitant insulin: not studied.
Adverse Reaction(s):
Nasopharyngitis, hypoglycemia, arthralgia, back pain, headache; hypersensitivity reactions (eg, urticaria, angioedema, localized skin exfoliation, bronchial hyperreactivity), myalgia, pancreatitis.
How Supplied:
Tabs—30, 90, 1000
Last Updated:
6/16/2011
美国FDA批准一种2型糖尿病新药Tradjenta
美国FDA于2011年5月2日批准Tradjenta 片剂（有效成份为linagliptin）治疗成人2型糖尿病，主要用于结合饮食和运动改善病人对血糖水平的控制。
胰岛素是一种调节血糖水平的激素，而2型糖尿病患者主要是因为自身不能产生胰岛素或者对胰岛素无正常反应。如果血糖水平长时间过高，会引起严重的并发症，包括心脏病、失明、神经及肾脏的损伤等。
2型糖尿病是糖尿病中最常见的一种，在美国2400万糖尿病患者中，90-95%患的是2型糖尿病。饭后服用Tradjenta可通过抑制二肽基肽酶4(dipeptidyl peptidase-4,简称DPP-4)，提升体内相关激素水平，刺激胰岛素释放，从而更好地控制血糖。
临床研究证明Tradjenta安全有效。获批前进行了8项共有3800名2型糖尿病患者参加的双盲对照临床试验，试验表明服用Tradjenta的病人其血糖控制情况与对照组相比有改善。
此外，对Tradjenta单独使用治疗和与其他2型糖尿病药（包括二甲双胍、格列美脲、吡格列酮）联用也进行过研究，但对Tradjenta与胰岛素联用未进行研究。Tradjenta不能用于治疗1型糖尿病，血液或者尿中酮类水平过高（糖尿病酮症酸中毒）的患者也不能服用Tradjenta。
Tradjenta最常见的副作用有上呼吸道感染、鼻塞、流鼻涕、喉咙痛、肌肉痛、头痛等。
Tradjenta由勃林格殷格翰公司(Boehringer Ingelheim Pharmaceuticals Inc.)和礼莱公司(Eli Lilly Co.)联合上市销售。