Ibuprofen has become very popular recently. Do you know its origin?

In the fight against the COVID-19 pandemic, ibuprofen can be said to have made outstanding contributions.

Ibuprofen, the world's best-selling antipyretic, analgesic and anti-inflammatory drug, has been in short supply recently. Today, let's talk about the story of ibuprofen.

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No matter which way you take ibuprofen, its invention is related to a British chemist named Stuart Adams.

Stuart Adams, Inventor of Ibuprofen

In 1923, Stuart Adams was born into an ordinary railway worker's family in Britain.

At the age of 15, Adams dropped out of school and worked as an apprentice in Boots' pharmacy, an experience that sparked his interest in pharmacy.

However, if Adams wanted to become a drug development expert, he needed to continue his studies. So after completing his three-year apprenticeship, he entered the University of Nottingham to study for a bachelor's degree in pharmacy, and later obtained a doctorate in pharmacology from the University of Leeds. After graduating with a doctorate, he returned to the research department of Boots to work on the development of drugs for the treatment of rheumatoid arthritis.

British chemist Stuart Adams (Image credit: Marie Lordkipanidzé)

At that time, the treatment for rheumatoid arthritis was to take large doses of corticosteroids and aspirin, but taking these drugs in large doses would cause a series of side effects , such as allergies, bleeding, and indigestion. Therefore, it was imperative to find an alternative drug with fewer side effects at that time.

Dr Adams - left, Dr John Nicholson and Mr R Cobb studying levels of inflammation (Image: The Boots Archive)

01

Thousands of attempts

Finally found "ibuprofen"

Adams' team first tested more than 200 salicylic acid-derived compounds, but the results were not good. Later, they turned their attention to compounds with carboxyl groups and tested more than 600 compounds. Four of them (BTS8402, BTS10335, BTS10499 and ibufenac) reached the clinical trial stage , but unfortunately, all four drugs failed due to side effects during treatment.

Adams' team did not give up. They continued to try and focused their research on "phenylpropionic acid". According to Boots records, Adams' team tested nearly 20,000 candidate compounds before finally finding ibuprofen.

In 1962, they successfully applied for a patent for an anti-inflammatory drug that covered a range of compounds, including ibuprofen, the compound known as ibuprofen.

Anti-inflammatory drug patent applied by Adams (Source: Author)

In the following three years, Adams' team continued to study these "phenylpropionic acid" compounds and found that ibuprofen was very effective and had relatively few side effects on humans.

However, what led to ibuprofen's later success was Adams's experience with a hangover. At that time, in order to treat the headache caused by the hangover, he took 600 mg of ibuprofen, and the effect was unexpectedly good. This also made Adams the first person to take ibuprofen.

Ibuprofen then became the fifth compound to enter clinical trials and was eventually approved as an over-the-counter drug for global distribution.

Ibuprofen advertisement in 1969 (Source: Author)

02

Patent expiration

Generic drugs make ibuprofen more readily available

Recently, there has been a rumor on the Internet that the inventor of ibuprofen gave up applying for a patent. How selfless and great!

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It is great that Adams' team developed a drug like ibuprofen. But Adams' team was working for Boots at the time, and as a company, Boots certainly could not give up the patent (as can be seen from the previous content, the patent for ibuprofen was applied for and approved in 1962).

Then why can pharmaceutical companies around the world now produce ibuprofen?

This is because the global patent for ibuprofen expired as early as 1985. Once the patent expired, generic drug manufacturers around the world began to produce ibuprofen, making the drug readily available. We can easily buy ibuprofen in hospitals and pharmacies, thanks to these generic drug manufacturers. Of course, the demand for ibuprofen may have increased sharply in some places recently, leading to tight supply, but I believe this situation will ease soon.

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It should be noted that after the patent protection period of a drug expires, pharmaceutical companies other than the original research company can produce the drug. These drugs produced by non-original research companies are called generic drugs, not counterfeits, so you can rest assured.

Also, the name ibuprofen is a non-patent name, also known as an "international non-proprietary name". To use an inappropriate analogy, it is like you cannot apply for patent names for things like "peach" and "water". "Ibuprofen" made by various manufacturers can all be called ibuprofen. That's why you see ibuprofen in various "positions".

03

How does ibuprofen work?

——Ask one by one

So why does ibuprofen relieve pain? How does it find your pain points?

In fact, some common pains in our lives, such as toothache, headache, joint pain, dysmenorrhea, etc., are related to a substance called "prostaglandin". Prostaglandin is a pain-causing substance that can bind to corresponding receptors to generate pain signals and transmit them to the brain, causing people to feel pain.

When ibuprofen is first taken orally, it is absorbed into the blood and transported throughout your body, knocking on your door one by one and asking: Does it hurt? Do you need help? Therefore, after taking ibuprofen, your pain will not be relieved immediately. At this time, you have to wait patiently for a while.

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Once ibuprofen finds the "pain point", it will bind to cyclooxygenase and block the synthesis of prostaglandins (cyclooxygenase in our body is the key enzyme that catalyzes the conversion of arachidonic acid into prostaglandins). Without prostaglandins, there will be no pain signals, and naturally you will not continue to feel pain.

However, ibuprofen cannot control those prostaglandins that have already been synthesized, and can only be left to time to slowly resolve the problem.

Ibuprofen is an over-the-counter drug that can be purchased at pharmacies without a prescription. Ibuprofen and other similar anti-inflammatory analgesics can be used to treat mild to moderate pain.

But please note that ibuprofen is not a panacea. If your pain is not relieved after taking ibuprofen, if your condition changes, or if adverse reactions occur, you should seek medical attention immediately.

Author｜Science Scraps

Review | Li Jing, Chief Pharmacist of Emergency General Hospital, Wei Guoyi, Chief Pharmacist of Anzhen Hospital

References:

[1] https://www.theguardian.com/science/2019/feb/13/stewart-adams-obituary

https://pharmaceutical-journal.com/article/infographics/a-brief-history-of-ibuprofen

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