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 interactions

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 phosphate and Vildagliptin were purchased from Jiacheng-Chem (Hangzhou, China). [source, 2015]
It was approved in October 2011 and is manufactured by MSD International GmbH for Merck and Co.15 Sitagliptin phosphate monohydrate is described chemically as 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a] pyrazine phosphate (1:1) monohydrate, with the structural formula shown in Figure 1.16 Simvastatin is butanoic acid, 2,2-dimethyl-,1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)-ethyl]-1-naphthalenyl ester, [1S-[1α,3α,7β,8β (2S*,4S*),-8aβ]], with the structural formula shown in Figure 2.16 The combination pill is indicated for patients requiring both medications, and is considered have significant HbA1c-lowering ability and cardiovascular benefits as well. [source, 2015]
In the second cohort, mice were placed on either the 10% fat control diet (D12450K; n = 8) for the duration of the study or 60% fat diet (D12492; n = 64) for 6 weeks, followed by one of the following treatment regimens for the remainder of the study (n = 16 per group): (1) 60% fat diet with no drug (D12492), (2) 60% fat diet containing Rosiglitazone (18 mg/kg diet or ∼3 mg/kg BW per day; Cayman Chemical; Research Diets custom diet formulation D08121002), (3) 60% fat diet containing sitagliptin (4 g/kg diet or ∼750 mg/kg BW per day; Sitagliptin phosphate monohydrate, BioVision; Research Diets custom diet formulation D08062502R), or (4) 60% fat diet (D12492) and metformin (1,1-dimethylbiguanide hydrochloride) in drinking water (1.25 mg/ml or ∼250 mg/kg BW per day). [source, 2015]
Dulbecco’s modified Eagle’s medium (DMEM), penicillin/streptomycin, trypsin/EDTA solution, Fungizone, Gly-Pro-p-nitroanilide, p-nitroaniline, Sitagliptin phosphate, N-Ethylmaleimide (NEM), bovine serum albumin (BSA) and extracellular matrix (ECM) proteins were supplied by Sigma (Sigma Chemical Co., St. Louis, MO). [source, 2015]
The medications used by the subjects for their diabetes are Diamicron, Gibenclamide, Gliclazide, Glipizide, Januvia, Lantus, Levemir, Metformin, Mixtard, NovoRapid flexpen, Sitagliptin. [source, 2014]
One report used positron emission tomography (PET) imaging and demonstrated DPP-4 inhibitor, MK-0431, protected against the loss of islet grafts in Streptozotocin (STZ)-diabetic mice [20]. [source, 2014]
Sitagliptin (Januvia [Merck, Whitehouse Station, NJ, USA]) is a highly selective dipeptidyl peptidase-4 (DPP-4) inhibitor available for the treatment of hyperglycemia in patients with type 2 diabetes,40,41 and Simvastatin (Zocor™ [Merck]) is an HMG-CoA reductase inhibitor available as an adjunctive treatment to diet for reducing elevated LDL-C and other lipids in patient with primary hypercholesterolemia and is indicated for reducing the risk of cardiovascular mortality. [source, 2013]