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What Pharmacological Advantages Can Deuterated APIs Deliver?

Neulande's Deuterated API Development and Manufacturing ServicesThere have been significant changes in the pharmaceutical industry over the past few years, and some of them have led to significant breakthroughs. One example is the growth of deuterated chemistry in the biopharma space.

With demand soaring for new drugs and medications, deuterated drugs can address a wide variety of problems at an affordable price. Deuteration chemistry has become a popular emerging frontier with tremendous potential to provide medications with improved pharmaco-kinetic and toxicological profiles.

What do pharmaceutical companies and product managers need to know about deuterated drugs, and how could they help you improve your processes?

What Is Deuteration Chemistry?

First, it’s important to discuss the meaning of ‘deuteration chemistry.’ It refers to using deuterium instead of hydrogen in the molecular structure. Hydrogen, the first element on the periodic table, has one electron, one proton, and no neutrons. Deuterium is similar to hydrogen in that it has one proton and one electron, but it also has a neutron. This makes deuterium an isotope of hydrogen, but the extra neutron adds some additional weight to the atom. Deuterated drugs exhibit superior pharmaco-kinetic or toxicological properties due to stronger deuterium–carbon bonds.

The incorporation of deuterium further leads to increased chemical stability, which is reflected by its slower rate of metabolism in the human body when ingested.

What Are the Advantages of Deuterated Drugs?

Pharmacological Advatages Of Deuterated DrugsThere are some significant advantages of deuterated drugs. One of the immediate benefits is that deuterated drugs typically possess a much longer half-life (e.g., the amount of time it takes the body to metabolize the medication).

The C-D bond is approximately 10 times stronger than the C-H bond, so it takes much longer for the body to break down the medication. A deuterated drug is much more resistant to enzymatic cleavage, which means that deuterated drugs will stay in the body for a longer amount of time.

Some of the main advantages of a longer drug half-life include:

  • An overall lower amount of medication is needed to achieve the same desired effect.
  • The medication does not have to be dosed as frequently, which can free up valuable manpower in hospitals and increase patient compliance in outpatient settings.
  • It is easier to maintain the desired level of the medication in the bloodstream, which can reduce the chances of unwanted side effects.
  • A steady level in the bloodstream can also reduce the formation of potentially toxic metabolites.

Deuterated drugs can reduce expenses during the research process and help bring new medications to the market more quickly.

Traditional drugs with a C-H bond can fail testing for a variety of reasons, including:

  • The drugs might be too toxic.
  • The pharmacokinetics might not be advantageous.
  • The drugs might not be efficacious for the issue they are designed to address.

Deuterated drugs can sidestep these issues because they are more efficient and less prone to side effects. They also have access to streamlined approval processes with the FDA. Because many of these issues can be avoided with stable deuterated drugs, clinical trials tend to focus almost exclusively on pharmacokinetics and toxicity, streamlining the approval process and helping companies get new medications to the market more quickly.

Where Does Deuterium Come From?

Clearly, there are a lot of advantages that deuterium can provide in the world of pharmaceuticals, but where exactly does it come from? It is true that hydrogen is significantly more common in the environment than deuterium, so deuterium enrichment is a vital part of the manufacturing process. Heavy water (D2O) produced through the deuterium enrichment is the most convenient source of deuterium.

We manufacture advance deuterated reagents, starting from heavy water (D2O) and deuterated methanol. This process has multiple stages, and we combine the result with the appropriate API to provide our clients with the target compound.

Neuland and Deuteration

Because of the stronger carbon deuterium bonds, deuterated drugs often demonstrate superior pharmacokinetic and toxicological properties. A handful of deuterated drugs have been approved, and many clinical trials continue to move forward.

Neuland Labs is proud to be an industry leader in this developing niche, and is a commercial supplier of deuterated APIs. If you would like to learn more about how we can help you take advantage of deuteration chemistry to improve a therapeutic API, contact us today.

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