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