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Tytuł:
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Selumetinib: First Approval.
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Autorzy:
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Markham A; Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand. .
Keam SJ; Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.
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Źródło:
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Drugs [Drugs] 2020 Jun; Vol. 80 (9), pp. 931-937.
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Typ publikacji:
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Journal Article; Review
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Język:
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English
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Imprint Name(s):
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Publication: Auckland : Adis, Springer International
Original Publication: New York, ADIS Press [etc.]
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MeSH Terms:
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Drug Approval*
MAP Kinase Kinase 1/*antagonists & inhibitors
MAP Kinase Kinase 2/*antagonists & inhibitors
Neurofibromatosis 1/*drug therapy
Protein Kinase Inhibitors/*pharmacology
Humans ; MAP Kinase Kinase 1/metabolism ; MAP Kinase Kinase 2/metabolism ; Molecular Structure ; Neurofibromatosis 1/metabolism ; Protein Kinase Inhibitors/chemistry
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Substance Nomenclature:
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0 (Protein Kinase Inhibitors)
EC 2.7.1.- (MAP2K2 protein, human)
EC 2.7.12.2 (MAP Kinase Kinase 1)
EC 2.7.12.2 (MAP Kinase Kinase 2)
EC 2.7.12.2 (MAP2K1 protein, human)
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Entry Date(s):
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Date Created: 20200607 Date Completed: 20210101 Latest Revision: 20210101
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Update Code:
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20240104
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DOI:
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10.1007/s40265-020-01331-x
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PMID:
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32504375
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Selumetinib (KOSELUGO TM ; AZD6244, ARRY-142886) is a mitogen-activated protein kinase 1 and 2 (MEK1/2) inhibitor being developed by AstraZeneca for the treatment of tumours associated with neurofibromatosis and various cancers. Selumetinib has been granted orphan drug status as adjuvant treatment for thyroid cancer (in the USA) and as treatment for neurofibromatosis type 1 (in the USA and the EU) and, based on the results of the phase II SPRINT trial, was recently approved in the USA in paediatric patients with neurofibromatosis type 1 and symptomatic, inoperable plexiform neurofibromas. This article summarizes the milestones in the development of selumetinib leading to this first approval for the treatment of paediatric patients aged ≥ 2 years with neurofibromatosis type 1 who have symptomatic, inoperable plexiform neurofibromas.