Latest research on Sitagliptin phosphate

Sitagliptin is a new oral hypoglycemic (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. This enzyme-inhibiting drug is to be used either alone or in combination with metformin or a thiazolidinedione for control of type 2 diabetes mellitus. The drug works to competitively inhibit a protein/enzyme, dipeptidyl peptidase 4 (DPP-4), that results in an increased amount of active incretins (GLP-1 and GIP), reduced amount of release of glucagon (diminishes its release) and increased release of insulin.

Latest findings

Sitagliptin (MK-0431), chemically (2R)-4-OXO-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine (see Figure 1) has a very high selectivity towards DPP-4, with an IC(50) of 18 nM. [source, 2007]
Nonetheless, it may be of some relevance that the current prescribing information of sitagliptin (approved as an oral anti-diabetes drug therapy in 2006), reports that in T2DM patients with a mean baseline HbA1c of 8.0%, sitagliptin 100 mg reduced HbA1c by 0.5%–0.7% compared with placebo (Januvia 2007). [source, 2007]