Background: Ketoprofen, a potent anti-inflammatory, analgesic and anti-pyretic
drug belonging to the propionic acid class was synthesized in 1968. Rapid absorption, simple
metabolism, faster blood brain barrier crossing and high antinociceptive activity are the
features responsible for its high use. But, free acidic moiety present in its structure is the
major factor that declines its popularity by causing various gastric side effects. Many researchers
have chemically modified this drug with the aim to discover an improved and safe
NSAID candidate or a new drug with altered activity. We thoroughly searched the literature
and found that during the period 2004-2016, more than fifty reports are available on chemical
modification of ketoprofen. Along with this, many patents involving chemical modification
of ketoprofen have also been reported. However, it was very surprising to note that
there are only a few review articles available covering only its pharmacological and clinical
properties. There is no review article available covering the chemistry part of ketoprofen.
This motivated us to compile the information available on ketoprofen and its derivatives.
The purpose of this article is to present an updated review about this topic.
Methods: We thoroughly searched the peer reviewed research literature and compiled all
such reportings (2004 onwards) for the benefit of researchers who further want to work on
ketoprofen or other NSAIDs.
Results: Studies have been conducted to invent strategies to reduce the ulcerogenic properties
of ketoprofen and in the course of time, its modified and improved derivatives have
been synthesized in search of safer NSAIDs. Along with the aim of reducing the gastric
side-effects, researchers have also done chemical modifications in the structure of ketoprofen
to improve its solubility, to alter its blood brain-barrierr permeability, to improve its
pharmacodynamic profile and to get derivatives possessing antioxidant, antiviral, anticancer
and immunomodulatory activities.
Conclusion: The findings of the review confirm that chemical modifications of ketoprofen
decrease ulcer producing side effect while maintaining its desirable actions. Some derivatives
were also found to possess better activity profile compared to the parent drug.