The Discovery and Development of the Triptans
The Discovery and Development of the Triptans
The drug discovery programs that led to the development of the triptans were determined by the membership of the American Headache Society to be the most important breakthrough in headache medicine in the last 50 years. Dr. Humphrey, who spearheaded the drug discovery, recounts the pioneering work that took place and examines its therapeutic impact.
The triptans are a class of drug specifically designed and developed for the acute treatment of migraine. All triptans are small, synthetic molecules that selectively activate 2 closely related subtypes of receptor (5-HT1B and 5-HT1D) for 5-hydroxytryptamine (also called serotonin). The prototypical triptan, sumatriptan, first became available in Europe in 1991 and revolutionized the treatment of this debilitating condition that affects millions of people throughout the world. As the first highly effective and well-tolerated drug for the acute treatment of migraine, it was hailed as a medical breakthrough. Many clinicians still describe, in both private and public forums, their first experience of witnessing at first hand the "miraculous" and rapid disappearance of their patient's symptoms after subcutaneous injection of sumatriptan during a severe migraine attack. To this day, no triptan can provide greater relief than that provided by parenterally administered sumatriptan. Early anecdotal stories abounded about people (often women) who suffered an attack as they were about to participate in an important meeting or event. Normally they would have had to go home in a taxi and not return for the rest of the day. However, the relief provided by a single injection of sumatriptan allowed them to effectively continue with their endeavors, without the previously inevitable day-off sick. Sumatriptan also proved to be effective by both the oral and intranasal routes and its clinical success provided the impetus for others to set about developing similar compounds. This led to the so called "triptan revolution" within the pharmaceutical industry and the availability of at least 7 triptans in the market place today. This also generated a massive increase in research on migraine both in industry and academia, a pleasing bonus from the therapeutic breakthrough itself. Importantly too, the discovery of sumatriptan confirmed, once and for all, that migraine truly is an organic disease and not just the figment of imagination of "neurotic" patients. Indeed, in the early days of sumatriptan's availability, it was hailed as diagnostic for whether or not a patient's headache was migrainous in origin.
The drug discovery programs that led to the development of the triptans were determined by the membership of the American Headache Society to be the most important breakthrough in headache medicine in the last 50 years. Dr. Humphrey, who spearheaded the drug discovery, recounts the pioneering work that took place and examines its therapeutic impact.
The triptans are a class of drug specifically designed and developed for the acute treatment of migraine. All triptans are small, synthetic molecules that selectively activate 2 closely related subtypes of receptor (5-HT1B and 5-HT1D) for 5-hydroxytryptamine (also called serotonin). The prototypical triptan, sumatriptan, first became available in Europe in 1991 and revolutionized the treatment of this debilitating condition that affects millions of people throughout the world. As the first highly effective and well-tolerated drug for the acute treatment of migraine, it was hailed as a medical breakthrough. Many clinicians still describe, in both private and public forums, their first experience of witnessing at first hand the "miraculous" and rapid disappearance of their patient's symptoms after subcutaneous injection of sumatriptan during a severe migraine attack. To this day, no triptan can provide greater relief than that provided by parenterally administered sumatriptan. Early anecdotal stories abounded about people (often women) who suffered an attack as they were about to participate in an important meeting or event. Normally they would have had to go home in a taxi and not return for the rest of the day. However, the relief provided by a single injection of sumatriptan allowed them to effectively continue with their endeavors, without the previously inevitable day-off sick. Sumatriptan also proved to be effective by both the oral and intranasal routes and its clinical success provided the impetus for others to set about developing similar compounds. This led to the so called "triptan revolution" within the pharmaceutical industry and the availability of at least 7 triptans in the market place today. This also generated a massive increase in research on migraine both in industry and academia, a pleasing bonus from the therapeutic breakthrough itself. Importantly too, the discovery of sumatriptan confirmed, once and for all, that migraine truly is an organic disease and not just the figment of imagination of "neurotic" patients. Indeed, in the early days of sumatriptan's availability, it was hailed as diagnostic for whether or not a patient's headache was migrainous in origin.