User:Mr. Ibrahem/Selumetinib

Mr. Ibrahem/Selumetinib
Clinical data
Trade names	Koselugo
Other names	AZD6244, ARRY-142886
AHFS/Drugs.com	Monograph
MedlinePlus	a620030
License data	US DailyMed: Selumetinib;
Pregnancy; category	Contraindicated;
Routes of; administration	By mouth (capsules)
Drug class	Protein kinase inhibitor
Legal status
Legal status	US: ℞-only;
Pharmacokinetic data
Metabolism	liver (probably CYP3A4 and CYP2C19)
Metabolites	N‐desmethyl‐selumetinib (active metabolite)
Elimination half-life	5.3–7.2 hrs
Excretion	mostly via bile
Identifiers
	IUPAC name 6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide;
Chemical and physical data
Formula	C17H15BrClFN4O3
Molar mass	457.68 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO;
	InChI InChI=1S/C17H15BrClFN4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26) ; Key:CYOHGALHFOKKQC-UHFFFAOYSA-N ;
	(verify)

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

^ 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.

[Patel-1] 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-2] 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.

[AHFS2021-3] "Selumetinib Monograph for Professionals". Drugs.com. Archived from the original on 15 April 2021. Retrieved 12 October 2021.

[PI2021-4] "Koselugo- selumetinib capsule". DailyMed. 10 April 2020. Archived from the original on 18 April 2020. Retrieved 18 April 2020.

[5] "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.

[6] "Koselugo Prices, Coupons & Patient Assistance Programs". Drugs.com. Retrieved 12 October 2021.