Sitagliptin Phosphate: A Blockbuster DPP-4 Inhibitor for Treating Type-2 Diabetes

Sitagliptin Phosphate: A Blockbuster DPP-4 Inhibitor for Treating Type-2 Diabetes

Sitagliptin Phosphate
Anti-Diabetic, Drug Research & Development API

Sitagliptin Phosphate CAS No: 654671-78-0

Sitagliptin Phosphate was approved more than a decade ago primarily as a way to combat type 2 diabetes. This dipeptidyl-peptidase-4 inhibitor lowers the levels of glucose in the patient directly following a meal and can also help regulate general blood sugar levels over time. It’s usually used in combination with other types of treatment if monotherapy fails, but can also be an alternative to standard hypoglycemic medications. This API encourages insulin secretion in the case of hyperglycemia while simultaneously inhibiting glucagon secretion.

What It Does

There are a lot of hypoglycemic agents on the market that people with diabetes can take to help them lower their blood sugar. However, many of these products have proven to be ineffective at regulating the levels to a healthy medium. It’s not uncommon for a patient’s blood sugar to take a plunge in the opposite direction with traditional hypoglycemic medications, such as sulfonylureas. With Sitagliptin Phosphate, patents have a much better chance of suppressing the release of glucagon without the accompanying risk of dangerously low blood pressure. It is not designed to help those with Type-1 diabetes.

Test Results

Research has shown this API to lower HbA1c levels by an average of .7% as compared to placebo. Steady-state plasma concentrations are typically reached after about three days with a low accumulation rate. Its elimination half-time is between 12 to 14 hours, with about 75% of the drug excreted unchanged. The chemical formula of Sitagliptin Phosphate is such that it has an affinity for DPP-4 as opposed to the other DDP enzymes. Researchers found people of all ethnic backgrounds were able to tolerate the API and that the results stayed steady even after long-time exposure to the drug. Patients did not typically experience weight gain when using the API.

How It’s Used

Most people will not take Sitagliptin Phosphate as a stand-alone therapy (Januvia), rather as in combination with Metformin HCl (Janumet). While Sitagliptin Phosphate can inhibit DPP-4 by up to 80% or even more, most patients will generally start with metformin and general lifestyle changes. They may need to quit smoking, improve their diet, or get more exercise in their life. Only when these tactics fail will doctors add Sitagliptin Phosphate into a patient’s routine to monitor their blood sugar levels. This API is generally given via tablet with the standard dose of Sitagliptin being 100 mg daily (Januvia), or 50 mg daily in combination with 1,000 mg of Metformin HCl (Janumet). It can be taken with or without food.

Side Effects

Side effects with Sitagliptin Phosphate tend to mirror those of the placebo with a few notable exceptions. One is cold-like symptoms, such as a runny nose or muscle pain. There have been select reports that potentially connect this API to more serious disorders, such as renal failure or pancreatitis. While there is not enough evidence to state that Sitagliptin is the cause of these conditions, doctors will usually raise or lower dosages based on a patient’s overall health. For example, those with moderate renal insufficiency will typically take about half that of someone with a healthy renal system. Sitagliptin Phosphate performed well also in combination with other drugs.

LGM Pharma

LGM Pharma is an innovation-driven API company, involved in the distribution of quality cGMP pharma ingredients to leading pharmaceutical companies. We specialize in streamlining the API supply chain management throughout all development and commercial stages while providing complete technical capabilities, expert regulatory support as well as other value-added services.




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