User:Mr. Ibrahem/Selumetinib
Clinical data | |
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Trade names | Koselugo |
Other names | AZD6244, ARRY-142886 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a620030 |
License data |
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Pregnancy category |
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Routes of administration | By mouth (capsules) |
Drug class | Protein kinase inhibitor |
Legal status | |
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Pharmacokinetic data | |
Metabolism | liver (probably CYP3A4 and CYP2C19)[2] |
Metabolites | N‐desmethyl‐selumetinib (active metabolite)[1] |
Elimination half-life | 5.3–7.2 hrs[1] |
Excretion | mostly via bile[1] |
Identifiers | |
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Chemical and physical data | |
Formula | C17H15BrClFN4O3 |
Molar mass | 457.68 g·mol−1 |
3D model (JSmol) | |
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Selumetinib, sold under the brand name Koselugo, is a medication used to treat plexiform neurofibromas found in neurofibromatosis type I (NF-1).[3] It may be used in those over the age of 1 year.[3] It is taken by mouth twice per day.[4]
Common side effects include headache, abdominal pain, tiredness, muscle pain, rash, fever, and itchiness.[4] Other side effects may include inflammation of the heart, eye problems, muscle breakdown, and bleeding.[4] Use in pregnancy may harm the baby.[4] It works by blocking mitogen-activated protein kinase kinase 1 and 2.[3]
Selumetinib was approved for medical use in the United States in 2020 and Europe in 2021.[3][5] In the United States a year of treatment at a dose of 25 mg twice per day costs about 150,000 USD as of 2021.[6]
References[edit]
- ^ a b c Patel, Y. T.; Daryani, V. M.; Patel, P.; Zhou, D.; Fangusaro, J.; Carlile, D. J.; Martin, P. D.; Aarons, L.; Stewart, C. F. (2017). "Population Pharmacokinetics of Selumetinib and Its Metabolite N-desmethyl-selumetinib in Adult Patients With Advanced Solid Tumors and Children With Low-Grade Gliomas". CPT: Pharmacometrics & Systems Pharmacology. 6 (5): 305–314. doi:10.1002/psp4.12175. PMC 5445231. PMID 28326681.
- ^ Dymond, Angela W.; Howes, Colin; Pattison, Christine; So, Karen; Mariani, Gabriella; Savage, Mark; Mair, Stuart; Ford, Gill; Martin, Paul (2016). "Metabolism, Excretion, and Pharmacokinetics of Selumetinib, an MEK1/2 inhibitor, in Healthy Adult Male Subjects". Clinical Therapeutics. 38 (11): 2447–2458. doi:10.1016/j.clinthera.2016.09.002. PMID 27751676.
- ^ a b c d e f "Selumetinib Monograph for Professionals". Drugs.com. Archived from the original on 15 April 2021. Retrieved 12 October 2021.
- ^ a b c d e "Koselugo- selumetinib capsule". DailyMed. 10 April 2020. Archived from the original on 18 April 2020. Retrieved 18 April 2020.
- ^ "EU/3/18/2050: Orphan designation for the treatment of neurofibromatosis type 1". Archived from the original on 25 June 2019. Retrieved 12 October 2021.
- ^ "Koselugo Prices, Coupons & Patient Assistance Programs". Drugs.com. Retrieved 12 October 2021.