What Is a Prodrug?

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  • Written By: Andrew Kirmayer
  • Edited By: Allegra J. Lingo
  • Last Modified Date: 03 November 2019
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A prodrug is a substance which in its initial form is inactive. Once ingested, the compound transforms into an active state when it is metabolized by the human body. The medication then takes effect to treat a specific ailment or condition at a desired time interval. Metabolization changes the molecular structure of a prodrug, and this process divides this pharmacological substance into one in which molecules break into fragments as well as another that becomes soluble upon being metabolized.

Many of these drugs have an altered chemical, physical, or biochemical makeup that allows them to remain dormant. It is also possible to structure the drug so that it will be processed by the body as if coated with nutritional compounds or lipids. A prodrug has a better oral availability than drugs that are typically injected into veins, muscles, or under the skin. Fewer injections are possible because the substance isn’t fully active until it reaches the part of the body it is intended to target, and drugs that previously had to be injected can now be swallowed orally.

There are various prodrug types that allow for water-soluble medications to reach organs, such as the liver or lungs, or pass into the blood or lymphatic system before becoming active. Such substances become active through a process known as hydrolysis. Certain substances can remain intact until reaching the small intestine and then get absorbed at this point.


Many conditions are treatable using prodrug varieties. Attention Deficit Hyperactivity Disorder (ADHD) patients benefit from the delay in bioactivation as well as the targeting of specific parts of the body, such as one that acts as a brain stimulant and another that only affects the prefrontal cortext. One kind even stops a particular strain of Human Immunodeficiency Virus (HIV), which is resistant to many other medications, from getting inside of white blood cells.

Prodrug development has also led to the development of medications that can get the body’s immune system to turn on cancer cells and tumors. It is not only people that are benefiting from variants of new pharmacological compounds, but more studies and clinical trials are required before these drugs are on the market. One type alleviates motion sickness in dogs without common side effects, such as nausea, that are brought on by some traditional remedies. Innovations in molecular science are leading to more and more medications that are taking the place of uncomfortable medical procedures and even surgeries.


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