Imatinib - History

History

Imatinib was developed in the late 1990s by biochemist Nicholas Lydon, a former researcher for Novartis, and oncologist Brian Druker of Oregon Health & Science University (OHSU). Other major contributions to imatinib development were made by Carlo Gambacorti-Passerini, a physician scientist and hematologist at University of Milano Bicocca, Italy, John Goldman at Hammersmith Hospital in London, UK, and later on by Charles Sawyers of Memorial Sloan-Kettering Cancer Center. Druker led the clinical trials confirming its efficacy in CML.

Imatinib was developed by rational drug design. After the Philadelphia chromosome mutation and hyperactive bcr-abl protein were discovered, the investigators screened chemical libraries to find a drug that would inhibit that protein. With high-throughput screening, they identified 2-phenylaminopyrimidine. This lead compound was then tested and modified by the introduction of methyl and benzamide groups to give it enhanced binding properties, resulting in imatinib.

Gleevec received FDA approval in May 2001. On the same month it made the cover of TIME magazine as the "magic bullet" to cure cancer. Druker, Lydon and Sawyers received the Lasker-DeBakey Clinical Medical Research Award in 2009 for "converting a fatal cancer into a manageable chronic condition".

Gleevec also holds the record for the drug with the fastest approval time by the FDA. According to Brian Druker, one of the developers of Imatinib, the biggest obstacle to being approved was the name of the drug. At that time, the drug was being called "Glivec", which is also the current spelling in most parts of the world. However, the United States Food and Drug Administration did not want people to mispronounce "Glivec" as "GLIE-VEC" which could be confused with a diabetic drug at the time. Therefore, Novartis, the pharmaceutical company who markets Gleevec, changed the name of "Glivec" to include two "e's" and avoid the phonetic confusion: Gleevec. Shortly thereafter, Gleevec was approved by the FDA.