Cancer drugs lapatinib

Johnston SR, Leary A. Lapatinib a novel EGFR/HER2 tyrosine kinase inhibitor for cancer. Drugs Today (Bare) 2006 42 441M53. 

A number of inhibitors of various tyrosine kinase enzymes are important new cancer drugs sunitinib (Sutent) is used for the treatment of certain kidney and GI cancers imatinib (Glivec) for chronic myeloid leukemia and GI tumours, and lapatinib (Tykerb/Tykerv) for breast and lung cancers. Bortezomib (Velcade), a proteasome inhibitor is used to treat multiple myeloma and is notable for being a boronic acid. 

Note that application in the particular indications is usually restricted either to patients expressing the target (e.g. trastuzumab, cetuximab, lapatinib, imatinib) and/or after failure of prior therapies (e.g. cetuximab, erlotinib, lapatinib, sutinib, dasatinib). Furthermore, for cancer treatment most tyrosine kinase inhibitors are applied in combination with conventional chemotherapeutic drugs, such as fluorouracil, taxanes, platin-based regimens, anthracylines and irinotecan or radiotherapy. 

Sources (1) Jarvis LM. Battling breast cancer, Chemical Engineering News 84 21-27 (2007). (2) FDA News, March 2007. http //www.fda.gov/bbs/topics/NEWS/2007/NEW01586.html, http //www.fda.gOv/cder/foi/label/2007/0220591bl.pdf [accessed September 20, 2007]. (3) Moy B, et al. Lapatinib, Nature Reviews Drug Discovery 6 431-432 (2007). 

A new synthesis of Lapatinib, an orally active drug for breast cancer, was described. The synthesis involved a palladium-catalyzed regioselective aryla-tion of furfural with 6-bromo-N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl) quinazolin-4-amine (14TL6007). 

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