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Fulltext Efficacy and Safety of Sitagliptin in the Treatment of COVID-19

Mikhael EM, Ong SC, Sheikh Ghadzi SM

J Pharm Pract, 2023 Aug;36(4):980-987.
PMID: 35581701 DOI: 10.1177/08971900221102119

Background: Coronavirus disease 2019 (COVID-19) is associated with a high risk of mortality especially among diabetes mellitus (DM) patients. Effective treatments against COVID-19 can complement the vaccination effort worldwide. Many review articles studied the effects of the dipeptidyl peptidase 4 (DPP-4) inhibitors among COVID-19 patients and found conflicting results. This heterogeneity may be due to different systemic pleiotropic effects of different DPP-4 inhibitors. Sitagliptin appears to be one of the good DPP-4 inhibitors that have antiinflammatory and antithrombotic effect. Therefore, this review assessed the benefits and safety of sitagliptin in the treatment of COVID-19. Methods: A detailed literature review using the electronic databases of Pubmed and Google Scholar was conducted during July and August 2021 to find out studies that published in English language and discussed the role of sitagliptin for COVID-19 patients. Results: 14 articles were eligible and thus included in this narrative review. Nine of these articles agreed to the benefit of sitagliptin in the treatment of COVID-19, while 3 studies considered sitagliptin as non useful or even risky, and one study was neutral in its conclusion towards the usage of sitagliptin in COVID-19. Only one study focused on the safety of sitagliptin and found that it is safe. Conclusion: Sitagliptin has anti-inflammatory, antifibrotic and antiapoptotic properties; such effects may be beneficial in reducing risks of COVID-19. Sitagliptin has good safety and fair benefits to reduce mortality among DM patients with COVID-19. Further randomized clinical trials are needed to confirm these benefits especially among patients without DM.

Matched MeSH terms: Sitagliptin Phosphate/adverse effects
Simple and rapid LC-MS/MS method for determination of sitagliptin in human plasma and application to bioequivalence study

Loh GOK, Wong EYL, Tan YTF, Lee YL, Pang LH, Chin MC, et al.

J Chromatogr B Analyt Technol Biomed Life Sci, 2020 Nov 30;1159:122337.
PMID: 32905988 DOI: 10.1016/j.jchromb.2020.122337

A simple, rapid, sensitive, and reproducible liquid chromatography-tandem mass spectrometry method was developed to determine sitagliptin in human plasma. Diphenhydramine HCl was used as internal standard (IS). The chromatographic separation was achieved using Agilent Poroshell 120 EC-C18 - Fast LC column (100 × 2.1mmID, 2.7) fitted with UHPLC Guard Poroshell 120 EC-C18 (5 × 2.1mmID, 2.7 µm). The mobile phase consisted of 0.1% v/v formic acid and methanol (45:55, v/v) run at a flow rate of 0.45 mL/min at 30 °C. Methanol produced relatively cleaner plasma sample as deproteinization agent. Polytetrafluoroethylene membrane was preferred over nylon membrane as the former produced clear plasma samples. The standard calibration curve was linear over the concentration range of 5-500.03 ng/mL. The within-run precision was 0.53-7.12% and accuracy 87.09-105.05%. The between-run precision was 4.74-11.68% and accuracy 95.02-97.36%. The extended run precision was 3.60-6.88% and accuracy 93.18-95.82%. The recovery of analyte and IS was consistent. Sitagliptin in plasma was stable at benchtop (short term) for 24 h, in autosampler tray for 48 h, in instrumentation room for 48 h (post-preparative), after 7 freeze-thaw cycles (-20 ± 10 °C), and 62 days in the freezer (-20 ± 10 °C). Both sitagliptin (analyte) and IS stock solutions were stable for 62 days when kept at room temperature (25 ± 4 °C) and in chiller (2-8 °C). The validated method was successfully applied to a bioequivalence study of two sitagliptin formulations involving 26 healthy Malaysian volunteers.

Matched MeSH terms: Sitagliptin Phosphate/blood*; Sitagliptin Phosphate/pharmacokinetics*; Sitagliptin Phosphate/chemistry
Synthesis, characterization and in-vitro cytotoxic potential of sitagliptin phosphate nanoparticles against advanced breast cancer cell line - MCF-7

Abdullah M, Rafiq A, Shahid N, Nasir Kalam M, Munir Y, Daoud Butt M, et al.

Pak J Pharm Sci, 2023 Nov;36(6(Special)):1849-1858.
PMID: 38264890

Pharmaceutical substance sitagliptin has long been used to treat diabetes. However, subsequent researches have shown that sitagliptin has additional therapeutic effects. Anti-inflammatory effects are observed. Combining sitagliptin with biodegradable polymers like nanoparticles for chemotherapy may be effective. This method enhances therapeutic agent pharmacokinetics. This study tests sitagliptin (SIT) chitosan base nanoparticles against MCF-7 cancer cell lines for anti-cancer effects. Sitagliptin chitosan-based nanoparticles are tested for their ability to suppress MCF-7 cancer cell proliferation. Ionic gelation, a typical nanoparticle manufacturing method, was used. A detailed examination of the nanoparticles followed, using particle-size measurement, FTIR and SEM. Entrapment efficiency, drug-loading, and in-vitro drug release were assessed. Loaded with chitosan and sitagliptin, the nanoparticles averaged 500nm and 534nm in diameter. Sitagliptin has little effect on particle size. Chitosan-based Sitagliptin nanoparticles grew slightly, suggesting Sitagliptin is present. SIT-SC-NPs had 32% encapsulation efficiency and 30% drug content due to their high polymer-to-drug ratio. SEM analysis showed that both drug-free and sitagliptin-loaded nanoparticles are spherical, as shown by the different bands in the photos. The SIT-CS-NPs had a 120-hour release efficiency of up to 80%. This suggests that these nanoparticles could cure hepatocellular carcinoma, specifically MCF-7 cell lines.

Matched MeSH terms: Sitagliptin Phosphate
Activation of Nrf2 signaling by sitagliptin and quercetin combination against β-amyloid induced Alzheimer's disease in rats

Li Y, Tian Q, Li Z, Dang M, Lin Y, Hou X

Drug Dev Res, 2019 09;80(6):837-845.
PMID: 31301179 DOI: 10.1002/ddr.21567

The objective of this study was to evaluate the neuroprotective effect of sitagliptin (Sita), quercetin (QCR) and its combination in β-amyloid (Aβ) induced Alzheimer's disease (AD). Male Sprague-Dawley rats, weighing between 220 and 280 g were used for experiment. Rats were divided into 5 groups (n = 10) and the groups were as follows: (a) Sham control; (b) Aβ injected; (c) Aβ injected + Sita 100; (d) Aβ injected + QCR 100; and (e) Aβ injected + Sita 100 + QCR 100. Cognitive performance was observed by the Morris water maze (MWM), biochemical markers, for example, MDA, SOD, CAT, GSH, Aβ1-42 level, Nrf2/HO-1 expression and histopathological study of rat brain were estimated. Pretreatment with Sita, QCR and their combination showed a significant increase in escape latency in particular MWM cognitive model. Further co-administration of sita and QCR significantly reduced Aβ1-42 level when compared with individual treatment. Biochemical markers, for example, increased SOD, CAT and GSH, decreased MDA were seen, and histopathological studies revealed the reversal of neuronal damage in the treatment group. Additionally, Nrf2/HO-1 pathway in rat's brain was significantly increased by Sita, QCR and their combination. Pretreatment with QCR potentiates the action of Sita in Aβ induced AD in rats. The improved cognitive memory could be because of the synergistic effect of the drugs by decreasing Aβ1-42 level, antioxidant activity and increased expression of Nrf2/HO-1 in rat brain.

Matched MeSH terms: Sitagliptin Phosphate/pharmacology; Sitagliptin Phosphate/therapeutic use*
Fulltext Dipeptidyl Peptidase-4 inhibitors use in type II diabetic patients in a tertiary hospital

Mak WY, Nagarajah JR, Abdul Halim H, Ramadas A, Mohd Pauzi Z, Pee LT, et al.

J Pharm Policy Pract, 2020;13:34.
PMID: 32566235 DOI: 10.1186/s40545-020-00238-y

Background: In Malaysia, for more than a decade, dipeptidyl peptidase-4 inhibitors (DPP-4i) are among the oral antidiabetic medications used as monotherapy or in combination to manage type II diabetes mellitus (T2DM). These medications are known for the efficacy in glycated haemoglobin (HbA1c) reduction and weight neutral effect with minimal hypoglycaemia occurrence. This study aimed to identify the outcomes of DPP-4i use in one of the largest tertiary public hospital in Southeast Asia.
Methods: This is a retrospective cross sectional study conducted in 2016, where stratified sampling method was used. Patients with T2DM treated with available DPP-4i; namely Linagliptin, Saxagliptin, Sitagliptin and Vildagliptin, for at least 3 months were identified from the pharmacy record. Medical records from Physician Clinic in Hospital Kuala Lumpur (HKL) were reviewed. Data on demographic, anthropometric, antidiabetic treatment modalities, laboratory and documented outcomes were collected. Outcomes endpoints which include changes in HbA1c, fasting blood glucose (FBG), and body weight were recorded and analysed. Adverse drug reactions (ADR) documented were also reported.
Results and discussion: A total of one hundred and five patients were recruited. The patients were 49.5% men (n = 52), with a mean age of 57 years, mean HbA1c of 8.5% (69 mmol/mol) and mean BMI of 29.5 kg/m2. At least 50% of the patients had T2DM for more than 10 years and more than two third of these patients had both T2DM and hypertension. Thirty nine patients were on Vildagliptin, 32 on Sitagliptin, 26 on Saxagliptin and the remaining on Linagliptin. The most commonly prescribed DPP-4i were Vildagliptin and Sitagliptin. Majority of the patients (90.4%) were prescribed with Metformin, with 62.8% of patients on fixed-dose combination, and the remaining on add-on Metformin therapy. Use of DPP-4i as an adjunct was associated with a mean reduction of 0.9% (9 mmol/mol) in HbA1c (p Sitagliptin had the highest reduction in HbA1c (1.66%,19 mmol/mol; p-value

Matched MeSH terms: Sitagliptin Phosphate
Hypoglycemia in patients with type 2 diabetes from India and Malaysia treated with sitagliptin or a sulfonylurea during Ramadan: a randomized, pragmatic study

Aravind SR, Ismail SB, Balamurugan R, Gupta JB, Wadhwa T, Loh SM, et al.

Curr Med Res Opin, 2012 Aug;28(8):1289-96.
PMID: 22738801 DOI: 10.1185/03007995.2012.707119

To compare the incidence of symptomatic hypoglycemia between sitagliptin and sulfonylurea in Muslim patients with type 2 diabetes who fasted during Ramadan.

Matched MeSH terms: Sitagliptin Phosphate