DPP-4 Inhibitor Sitagliptin (Januvia) and Clinical Trials of this New Type 2 Diabetes Treatment

Get New Treatments Alerts:

Yesterday i wrote an introductory post about the class of drugs called Dipeptidyl Peptidase -4 inhibitors (DPP-4) which are the latest medications being used to treat Type 2 Diabetes Mellitus. Today we dig deeper into Sitagliptin (sold as the brand name Januvia), the first DPP-IV drug approved by the FDA in October 2006 for the treatment of type 2 diabetes. Sitagliptin is also available in a combination product with metformin. The drug is manufactured by Merck.

Physiological and Pharmacokinetic Properties of Sitagliptin

Sitagliptin increases postmeal GLP-1 levels by approximately 2-fold when compared with placebo. Sitagliptin is rapidly absorbed after oral administration, with a bioavailability of approximately 87%. The pharmacokinetic properties of
Sitagliptin appear unaffected by age, sex, race, ethnicity, and body mass index as evidenced by clinical trial data.

Results from Clinical trials on the Effectiveness of Sitagliptin (Januvia)

1. A four-month long phase III trial demonstrated that sitagliptin when given in dosages of 100 and 200 mg once/day decreased Hemoglobin A1C (a test to measure long term blood sugar control) values by 0.79% and 0.94%, respectively which was significant in both instances when compared with a control group that was given a placebo (see what a placebo means) . The trial also showed that their were improvements in fasting plasma glucose (FPG) and postprandial glucose (PPG) levels seen with sitagliptin treatment compared to a placeb0.

2. Sitagliptin has also been studied in combination with other anti-diabetic therapies. In one study, patients receiving ongoing Metformin therapy were administered sitagliptin 100 mg/day or a placebo. The Sitagliptin plus metformin group experienced decreases in A1C, at 24 weeks, while the patients in the placebo group experienced no significant changes in A1C

The recommended dosage of sitagliptin is 100 mg once/day, either as monotherapy or in combination with other agents for type 2 diabetes such Metformin.