Table 1.

Some therapeutic properties of dipeptidyl peptidase-4 inhibitors in monotherapy of type 2 diabetic patients

Drug	Approval history	Cost	marketing status	Usage mode	Different dosage	Daily dose	Efficacy in HbA1c reduction (%)	Ref.	side effects
Sitagliptin	in 2006, by US FDA, 50–100 mg once a day	25 mg (per each): $17.18 50 mg (per each): $17.18 100 mg (per each): $17.18	prescription (JANUVIA®)	Tablet, oral	25, 50 and 100 mg	100 mg once a day for over 12 weeks	0.54	[29]	gastrointestinal disturbance as abdominal pain, nausea and diarrhea, [29], nasopharyngitis, increase in uric acid, decrease in alkaline phosphatase and increase of white blood cell count [33], (acute pancreatitis and pancreas cancer, controversial data) [34], decrease of renal function [35]
						100 mg once a day for 24 weeks	0.61	[36]
Saxagliptin	in 2009, by US FDA, 2.5–5 mg once daily	2.5 mg (per each): $16.33 5 mg (per each): $16.33	prescription (ONGLYZA ®)	Tablet, oral	2.5 and 5 mg	2.5, 5 and 10 mg once a day for 24 weeks	0.43, 0.46 and 0.54, respectively	[37, 38]	heart failure-controversial data- [27, 34], upper respiratory tract infections, urinary tract infections, headache [37], nasopharyngitis, back [39], abdominal pain [40], (lymphopenia, rash, increase of blood creatinine and creatine phosphokinase- severe side effects) [39].
Linagliptin	in 2011, by US FDA, 5 mg once daily	5 mg (per each): $16.46	prescription (TRADJENTA®)	Tablet, oral	5 mg	5 mg once a day after 24-week	0.69	[41]	hypersensitivity reactions (urticaria, angioedema, localized skin exfoliation, bronchospasm, myalgia and pancreas disorders)3 [34, 40], Headache, hypertension, and back pain [40]
Alogliptin	in 2013, by US FDA, 25 mg once daily	Tablets (Alogliptin Benzoate Oral) 6.25 mg (per each): $7.80 12.5 mg (per each): $7.80 25 mg (per each): $7.80 Tablets (Nesina oral) 6.25 mg per each): $14.97 12.5 mg (per each): $14.97 25 mg (per each): $ 14.97	prescription (NESINA ®)	Tablet, oral	6.25, 12.5 and 25 mg,	12.5 and 25 mg once a day after 26-week	0.56–0.96	[42]	dizziness, constipation [43], nasopharyngitis and upper respiratory tract infections [44], headache, hypoglycemic episodes [43, 44], pruritic rash [42], hepatic adverse effects [34, 42], acute pancreatitis, hypersensitivity reactions (anaphylaxis, angioedema- controversial data-[34] and severe cutaneous reactions including Stevens-Johnson syndrome- severe side effects) [44]
Vildagliptin	2007 by European Union, 50 mg twice a day	–	–	–	–	50 mg once a day, 50 mg twice a day and 100 mg once a day after 24-week	0.5, 0.7 and 0.8 respectively	[34, 45]	pancreas- or hepatic-related adverse effects- controversial data- [34]
Gemigliptin	in 2012, by Republic of Korea with 50 mg once daily	–	–	–	–	50 mg once a day, after 24-week	0.713 from placebo baseline	[46]	nasopharyngitis, urinary tract infection, diarrhea, headache, cough, arthralgia and hypertension [47].
Anagliptin	in 2012, by Japan with 200 mg daily	–	–	–	–	100 mg or 200 mg twice a day for 12-week	0.75–0.82, respectively	[48]	constipation, gastritis and somnolence, hypokalemia and muscle weakness [48]
Evogliptin	in 2015, by South Korea with 5 mg once daily	–	–	–	–	5 mg once daily for 12 weeks	0.7	[30]	Nervous system disorders (dizziness and headache), sleep disorder, fatigue, abdominal discomfort, epigastric discomfort, urticarial, oral mucosa erosion, chest discomfort, urinary frequency, hyperglycemia, pruritus [30, 49], nasopharyngitis and arthralgia [50]
Omarigliptin	in 2015, by Japan with 25 mg once a week	–	–	–	–	25 mg once a week for 12 weeks	0.71	[32, 51]	nasopharyngitis, bronchitis, influenza, pharyngitis, diarrhea, gastritis [30], dyspepsia, constipation, abdominal discomfort, constipation and abdominal discomfort [52]
Trelagliptin	in 2015, by Japan with 100 mg once a week	–	–	–	–	12.5–200 mg once weekly for 12 weeks	0.32 to 0.55	[53, 54]	Nasopharyngitis
Teneligliptin	in 2012, by Japan with 20 mg once a day	–	–	–	–	10, 20 and 40 mg once a day for 12 weeks	0.8, 0.8 and 0.9, respectively	[31, 55, 56]

US FDA: United States Food and Drug Administration