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

For diabetes, we found that the reviews for seven drugs (Apidra, Symlin, Exubera, Januvia, Janumet, Victoza and Bydureon) discussed the rationale for use of surrogates and three of them (Symlin, Victoza and Bydureon) justified choosing glycaemic control as an outcome by clearly stating the evidence that corresponds to the highest level of evidence for surrogacy using the ICH-9 criteria. [source, 2015]
We found that a review for one drug in COPD (Arcapta Neohaler) mentioned a MID and reviews for 12 drugs in diabetes (Avandaryl, Symlin, Duetact, Exubera, Januvia, BYETTA, Cycloset, Onglyza, Kombiglyze XR, Victoza, Tradjenta and Bydureon) mentioned a threshold (number of patients achieving the target haemoglobin A1C level) that is linked to patient-centred outcomes. [source, 2015]
Medication history included Amlodipine, Aspirin, Calcium carbonate, Synthroid, Pioglitazone, Humalog, Glucovance, Crestor, Januvia, and Lisinopril. [source, 2015]
Sitagliptin, from Merck Sharp & Dohme, was the first selective DPP-4 inhibitor in the market, approved in 2006 by FDA and commercialized as Januvia. [source, 2015]
Sitagliptin phosphate and Vildagliptin were purchased from Jiacheng-Chem (Hangzhou, China). [source, 2015]
Mice received the control (0.01 M Tris-HCl buffer), trypsin-treated ß-lactoglobulin (300 mg/kg), or Sitagliptin phosphate hydrate (3 mg/kg; positive control) by oral administration 1 h prior to an oral glucose tolerance test. [source, 2015]
However, the IC50 value against DPP-IV of Sitagliptin phosphate hydrate was 19.6 nM and extremely stronger than the hexapeptide. [source, 2015]
DPP-4 inhibitor Sitagliptin phosphate was obtained from Darui, Shanghai, China. [source, 2015]
Sitagliptin (SG), a specific DPP4 inhibitor (DPP4-I), was extracted from Januvia tablets (Merck). [source, 2015]
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]