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New Drugs for Diabetes Treatment Category: Diabetes by - January 21, 2014 | Views: 92666 | Likes: 4 | Comment: 0  

Newest Medications for Treatment of Type 2 Diabetes

Dipeptidyl Peptidase 4 (DPP-4) Inhibitors

Although DPP-4 inhibitors have been available for almost 8 years they are newer than sulfonylureas and metformin. The first DPP-4 inhibitor, sitagliptin (Januvia), was FDA approved in 2006 for use with diet and exercise and was later approved in 2007 for its use in combination with metformin or thiazolidinediones. The second DPP-4 inhibitor, saxagliptin (Onglyza), was approved in 2009 for monotherapy and in combination with metformin, sulfonylurea, or thiazolidinediones. The next DPP-4 inhibitor, linagliptin (Tradjenta), was approved in 2011 for both monotherapy and combination therapy with metformin, sulfonylureas, or pioglitazone. The latest DPP-4 inhibitor, alogliptin (Nesina), was FDA approved in 2013 as monotherapy or in combination with metformin, sulfonylureas, thiazolidinediones, and insulin.

DPP-4 inhibitors increase the amount of two proteins (incretin hormones) found in the body, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). Incretin hormones tell the body to release insulin and lower blood glucose. GLP-1 also decreases the production of glucose and slows down the absorption of glucose.

Incretin hormones are removed from the body by an enzyme called dipeptidyl peptidase-4 (DPP-4). DPP-4 inhibitors block this enzyme resulting in GLP-1 and GIP to stay in the body longer and, therefore, decrease blood glucose levels.

Efficacy of DPP-4 Inhibitors

  • The effectiveness of DPP-4 inhibitors used as monotherapy or in combination with other oral antidiabetic drugs is shown in multiple clinical trials lasting from 12-52 weeks.
    • Average decrease in HbA1c from baseline ranges between 0.5 to 1.9%
    • Average decrease in fasting plasma glucose (FPG) from baseline is 9 to 46 mg/dL
  • A head-to-head trial of saxagliptin 5 mg or sitagliptin 100 mg with metformin therapy demonstrated non-inferiority (one drug was not inferior to the other).

Side Effects of DPP-4 inhibitors

  • Upper respiratory tract infection and common cold symptoms (a runny nose, sore throat, or nasal congestion)
  • Headache
  • Pancreatitis (inflammation of the pancreas)
  • Abdominal pain, nausea, diarrhea (sitagliptin)
  • Urinary tract infection (saxagliptin)
  • Hypoglycemia (low levels of blood glucose; more common with alogliptin)

Additional Facts

  • DPP-4 inhibitors are taken orally with or without food and have once a day dosing.
  • They are safer than sulfonylureas when comparing the rate of hypoglycemic episodes.
  • They do not affect weight.
  • In patients with impaired renal function, linagliptin is the only DPP-4 inhibitor that does not require a dose adjustment.

List of DPP-4 Inhibitors and their Average Wholesale Price (AWP) per Pill 

Next: GLP-1 Agonist



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