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.

Sitagliptin phosphate indications

In a study published July 2014, Weir et al. further evaluated the effect of sitagliptin (Januvia) on cardiovascular endpoints (all-cause hospital admission/death as well as heart-failure-specific hospitalization/death in 7,620 diabetic patients recently diagnosed with heart failure) [146]. [source, 2015]
We found that the DPP4 inhibitor MK-0431 and the FAP inhibitor 3099 had no effect on adipocyte differentiation, while the DPP8/9 inhibitor 1G244 blocked adipogenesis in 3T3-L1 cells as measured by Oil red O staining (Fig. 2A). [source, 2015]
On the other hand, DPP4 inhibitor MK-0431 and FAP inhibitor 3099 had no effect on DMI induced expression of CEBPα, CEBPβ, CEBPδ and PPARγ2 during 3T3-L1 differentiation (Fig. 4C). [source, 2015]
Initially we used Sitagliptin phosphate 30 μM, which has been reported to selectively inhibit DPPIV/CD26, but not DP-8 and -9 [33, 34]; however, in our tests this concentration of inhibitor had no effect (data not shown). [source, 2015]
Whereas Sitagliptin phosphate has affected adhesion also in HeLa cell line, which practically does not express DPPIV/CD26, we believe that this effect may be mediated independent of DPPIV/CD26 enzymatic activity. [source, 2015]
Although this effect appears to be mediated independent of DPPIV/CD26 enzymatic activity, in view of the HeLa cell line adhesion was also affected by Sitagliptin phosphate. [source, 2015]
Although the effects of MK-0431 depend on its dose, we were unable to obtain sufficient plasma from mice to measure DPP-4 enzyme activity or active GLP-1 concentration after treatment with MK-0431. [source, 2014]
Hence, we cannot exclude the possibility that higher dose of MK-0431 may have beneficial effects on islet transplantation. [source, 2014]
13 (Januvia, Merck) reduces glucose and HbA1c levels but has no effect on body weight. [source, 2014]
There is paucity of data in the literature regarding the effect of Sitagliptine on lipid profile. [source, 2013]