Ibuprofen is almost synonymous with painkillers. Almost every household will keep a few strips of ibuprofen, and the first-aid kit will not feel complete without it. The drug was listed as the top ten best selling generic molecules globally with annual sales of USD $1.98 billion in 2011. Although the patent for ibuprofen expired in 1984, the demand for branded ibuprofen (Nurofen) is still going strong. Without ibuprofen, treatment for pain and inflammation may be very different from what we practice today.

However, how many of us know the inventor of ibuprofen?

In this article, we will go through the remarkable story of Dr Stewart Adams, the pharmacist who gave the world one of the most popular painkillers of all time.

The brilliant minds behind ibuprofen

Ibuprofen was invented by Dr Steward Adams OBE, a British pharmacist who was hailed as the first researcher to look into the field of NSAID (Non-steroidal anti-inflammatory drug). Together with his colleague, Dr John Nicholson, an organic chemist, they filed the ibuprofen patent in 1961 that officially kickstarted a new chapter in the treatment for pain and inflammation.

Dr Steward Adams began his apprenticeship at Boots pharmacy at the young age of 16. He proceeded to complete a B.Pharm degree in University College Nottingham (now The University of Nottingham). Upon graduation, he worked briefly on the production of penicillin antibiotics but was transferred to Boots' Bioassay Division of the Research Department where he began his research career. Subsequently, Dr Adams successfully undertook his PhD from the University of Leeds where he explored the relationship between heparin and histamine.

The journey to discovery

Dr Adams returned to Boots after his PhD study and was tasked to look for new treatments for rheumatoid arthritis. He first hatched the idea in mid-1953, that a compound would be chemically different to cortisone/cortical steroids but still retain the class therapeutic effects. His inspiration came from the anti-inflammatory property of aspirin, which he felt was “special”.

He said “Nobody really talked about anti-inflammatory activity in those days; if you look at Pharmacopoeias, you’ll find that up until 1962 aspirin was always analgesic antipyretic, so it was original to be thinking about anti-inflammatory activity’.

Dr John Nicholson from the Chemistry Division in Boots joined the research effort a few years later and had been working with Dr Adams for over 20 years since. Their research effort was first focused on salicylate, then attention turned to compounds with carboxylic acid groupings. The team produced and tested over 600 different analogues but none of them was successful.

"I did get depressed on more than one occasion," said Dr Adams.

Later efforts were concentrated on phenylpropionics where Dr Nicholson and Dr Adams patented a variety of compounds for “Anti-Inflammatory Agents” in 1961, which included ibuprofen (2-(4-isobutylphenyl)propionic acid) (6). Within three years of the patent filing, Dr Adams and his team had looked at the toxicity of these compounds, and ibuprofen was chosen for detailed investigation. Owing to a very different health and safety regulation in those days, Dr Adams had, in more than one occasion, tested the compound on himself which he claimed: "there are certain side effects that you can't study from animal testing, for example rash, nausea and headaches,".

Ibuprofen was later tested in clinical trials and it was approved in the UK in 1969 to treat rheumatic diseases. It was later approved for other non-rheumatic painful conditions and eventually become an over-the-counter drug after extensive trials.

Dr Steward Adams, the inventor of ibuprofen, received an honorary doctorate of science from the University of Nottingham, two blue Chemical Landmark plaques from the Royal Society of Chemistry, appointed OBE (Officer of the Order of the British Empire), and was made an Honorary Freeman of Nottingham, the highest honour a council can bestow. MIMS

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Sources:
http://www.fiercepharma.com/special-report/top-20-generic-molecules-worldwide
http://www.economist.com/news/finance-and-economics/21604575-drug-companies-are-adept-extending-lifespan-patents-consumers
Halford GM, Lordkipanidzé M, Watson SP. 50th anniversary of the discovery of ibuprofen: an interview with Dr Stewart Adams. Platelets. 2012 Sep 18;23(6):415–22.
http://www.bbc.com/news/health-34798438
Robinson J. The man who discovered ibuprofen. Pharm J. 2016;296(7887).
Nicholson J, Adams S. Anti-Inflammatory Agents. United Kingdom: The Patent Office London; 971,700, 1961.
http://www.rsc.org/AboutUs/News/PressReleases/2013/ibuprofen-chemical-landmark.asp
https://www.gov.uk/honours/types-of-honours-and-awards