Real-World Observational Study on Vildagliptin With Insulin (VIL-INS) or Vildagliptin and Metformin With Insulin (VIL-MET-INS) Therapy in Indian Patients With Type 2 Diabetes Mellitus.

BACKGROUND AND OBJECTIVE:  The therapeutic use of vildagliptin and insulin (VIL-INS) or vildagliptin and metformin in combination with insulin (VIL-MET-INS) in the Indian scenario has yet to be explored by generating real-world evidence. Therefore, the present study aimed to evaluate the demographic, clinical characteristics, and treatment patterns of patients with type 2 diabetes mellitus (T2DM) in Indian settings in the above context. METHODOLOGY:  This observational study conducted at 600 healthcare centers in India retrospectively analyzed data of adult patients with T2DM who had been treated with either vildagliptin with insulin or a combination of vildagliptin and metformin with insulin. Data were collected from medical records and analyzed by appropriate statistical tests. RESULTS:  A total of 12,603 patients with T2DM were included with a mean age of 53.4 years of which 63.8% were males. The majority of patients (n=6511; 51.7%) received a combination of vildagliptin and metformin on top of insulin. A significantly high proportion of patients in the age group of 18-40 years received this treatment compared to patients who were initiated on insulin treatment after vildagliptin and metformin combination (11.6% vs. 9.7%; P<0.001). Of all the patients, 70.0% were able to achieve target glycemic control with either VIS-INS or VIL-MET-INS. After treatment with VIL-INS or VIL-MET-INS, the mean glycated hemoglobin (HbA1c) levels significantly decreased with a mean change of 1.46%. Out of all patients, 13.5% experienced weight changes during treatment, with 67.4% of them showing weight loss. A total of 68 patients reported hypoglycemic events and among them, 49 patients had mild hypoglycemic events. Physician global evaluation of efficacy and tolerability showed a majority of patients rated their experience as good to excellent (86.3% and 86.0%, respectively). CONCLUSION:  Both treatment regimens were effective in terms of reduced HbA1c to achieve glycemic control. Furthermore, it is well tolerated without an increase in the risk of hypoglycemia or weight gain. Hence, this therapy has favorable outcomes for T2DM management in Indian clinical settings.

Sustained-Release Vildagliptin 100 mg in Type 2 Diabetes Mellitus: A Review.

Dipeptidyl peptidase-4 inhibitors (DPP4Is) were introduced into the management of type 2 diabetes mellitus (T2DM) as they are insulinotropic and have no inherent risk of hypoglycemia and no effect on body weight. Currently, 11 drugs in this class are available for the management of diabetes. Although they have a similar mechanism of action, they differ from one other in their binding mechanisms, which influences their therapeutic and pharmacological profiles. Vildagliptin's overall safety and tolerability profile was comparable to placebo throughout clinical studies, and real-world data in a large group of T2DM patients corroborated this finding. Therefore, DPP4Is like vildagliptin is a secure alternative for treating patients with T2DM. Vildagliptin treatment given as a once-daily (QD) 100 mg sustained release (SR) formulation fits the criteria of adherence and compliance. This SR formulation, given once daily has the potential to provide glycemic control like the vildagliptin 50 mg twice-daily (BD) formulation. This comprehensive review discusses the journey of vildagliptin as 50 mg BD therapy as well as 100 mg SR QD therapy.

Highly selective on-off fluorescence recognition of Fe3+ based on a coumarin derivative and its application in live-cell imaging.

A novel coumarin chemosensor, 7-hydroxy-2-oxo-N-(pyridin-2-ylmethyl)chromene-3-carboxamide (Probe 1), demonstrated significant selectivity towards Fe3+ ions. Probe 1 exhibited high fluorescence emission profile at 447nm, excellent selectivity towards Fe3+ over other biologically important metal ions (Al3+, Ba2+, Co2+, Cu2+, Zn2+, Cd2+, Hg2+, Pb2+ and Sn2+). Interestingly, there was ~30-fold decrease in fluorescence intensity upon Fe3+ binding. The limit of detection of Fe3+ was found to be 0.76µM (~40ppb). Probe 1 also exhibited high potential as an intracellular chemosensor for Fe3+.

Fluorescent probes for biomedical applications (2009-2014).

The discovery and subsequent development of fluorescent probes was one of the most exciting innovations in life sciences, which marked the beginning of interpretation of numerous biological phenomena. Today, fluorescent probes are used for a wide range of biomedical applications, such as pharmaceutical research, clinical diagnostics and high-throughput screening, to name a few. Despite the availability of a large number of these probes, efforts to invent newer versions utilizing novel chemistry to address limitations of the current approaches continue. This review article gives a rundown on 'small-molecule fluorescent probes' patents/patent applications from January 2009 to March 2014. The patent literature was classified based on 'preparation' and 'biomedical applications' of these 'fluorescing wonders'.

Reverse docking: a powerful tool for drug repositioning and drug rescue.

Reverse or inverse docking is proving to be a powerful tool for drug repositioning and drug rescue. It involves docking a small-molecule drug/ligand in the potential binding cavities of a set of clinically relevant macromolecular targets. Detailed analyses of the binding characteristics lead to ranking of the targets according to the tightness of binding. This process can potentially identify novel molecular targets for the drug/ligand which may be relevant for its mechanism of action and/or side effect profile. Another potential application of reverse docking is during the lead discovery and optimization stages of the drug-discovery cycle. This review summarizes the state-of-the-art and future prospects of the reverse docking with particular emphasis on computational molecular design.