Difference between revisions of "Selumetinib (Koselugo)"

Latest revision as of 23:29, 17 August 2023

Mechanism of action

Inhibits the enzyme MAPK kinase (MEK), specifically the MEK1 and MEK2 subtypes of the enzyme.

Diseases for which it is used

History of changes in FDA indication

Note: this is not an antineoplastic indication. This drug does have some preliminary data in cancer settings.

2020-04-10: Approved for pediatric patients, 2 years of age and older, with neurofibromatosis type 1 (NF1) who have symptomatic, inoperable plexiform neurofibromas (PN).

History of changes in EMA indication

2020-04-10: Initial marketing authorisation.

History of changes in PMDA indication

2022-09-26: Drugs with a new active ingredient indicated for the treatment of plexiform neurofibroma in patients with neurofibromatosis type 1.

Also known as

Code name: AZD-6244
Brand name: Koselugo

@@ Line 2: / Line 2: @@
 Inhibits the enzyme MAPK kinase (MEK), specifically the MEK1 and MEK2 subtypes of the enzyme.
-==Preliminary data==
+==Diseases for which it is used==
-===[[Ovarian cancer]]===
+*[[Low-grade serous ovarian cancer]]
-# Farley J, Brady WE, Vathipadiekal V, Lankes HA, Coleman R, Morgan MA, Mannel R, Yamada SD, Mutch D, Rodgers WH, Birrer M, Gershenson DM. Selumetinib in women with recurrent low-grade serous carcinoma of the ovary or peritoneum: an open-label, single-arm, phase 2 study. Lancet Oncol. 2013 Feb;14(2):134-40. Epub 2012 Dec 21. [https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3627419/ link to original article] [https://www.ncbi.nlm.nih.gov/pubmed/23261356 PubMed]
+*[[Differentiated thyroid cancer]]
+*[[Uveal melanoma]]
-===[[Uveal melanoma]]===
+==History of changes in FDA indication==
-# Carvajal RD, Sosman JA, Quevedo JF, Milhem MM, Joshua AM, Kudchadkar RR, Linette GP, Gajewski TF, Lutzky J, Lawson DH, Lao CD, Flynn PJ, Albertini MR, Sato T, Lewis K, Doyle A, Ancell K, Panageas KS, Bluth M, Hedvat C, Erinjeri J, Ambrosini G, Marr B, Abramson DH, Dickson MA, Wolchok JD, Chapman PB, Schwartz GK. Effect of selumetinib vs chemotherapy on progression-free survival in uveal melanoma: a randomized clinical trial. JAMA. 2014 Jun 18;311(23):2397-405. [https://jamanetwork.com/journals/jama/fullarticle/1881312 link to original article] [https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4249701/ link to PMC article] [https://www.ncbi.nlm.nih.gov/pubmed/24938562 PubMed]
+''Note: this is not an antineoplastic indication. This drug does have some preliminary data in cancer settings.''
-# '''SUMIT:''' Carvajal RD, Piperno-Neumann S, Kapiteijn E, Chapman PB, Frank S, Joshua AM, Piulats JM, Wolter P, Cocquyt V, Chmielowski B, Evans TRJ, Gastaud L, Linette G, Berking C, Schachter J, Rodrigues MJ, Shoushtari AN, Clemett D, Ghiorghiu D, Mariani G, Spratt S, Lovick S, Barker P, Kilgour E, Lai Z, Schwartz GK, Nathan P. Selumetinib in combination with dacarbazine in patients with metastatic uveal melanoma: a phase III, multicenter, randomized trial (SUMIT). J Clin Oncol. 2018 Apr 20;36(12):1232-1239. Epub 2018 Mar 12. [https://doi.org/10.1200/JCO.2017.74.1090 link to original article] '''contains verified protocol''' [https://www.ncbi.nlm.nih.gov/pubmed/29528792 PubMed]
+*2020-04-10: Approved for pediatric patients, 2 years of age and older, with neurofibromatosis type 1 (NF1) who have symptomatic, inoperable [[Plexiform neurofibroma|plexiform neurofibromas (PN)]].
+==History of changes in EMA indication==
+*2020-04-10: Initial marketing authorisation.
+==History of changes in PMDA indication==
+*2022-09-26: Drugs with a new active ingredient indicated for the treatment of [[plexiform neurofibroma]] in patients with neurofibromatosis type 1.
-===[[Thyroid cancer]]===
+==Also known as==
-# Ho AL, Grewal RK, Leboeuf R, Sherman EJ, Pfister DG, Deandreis D, Pentlow KS, Zanzonico PB, Haque S, Gavane S, Ghossein RA, Ricarte-Filho JC, Domínguez JM, Shen R, Tuttle RM, Larson SM, Fagin JA. Selumetinib-enhanced radioiodine uptake in advanced thyroid cancer. N Engl J Med. 2013 Feb 14;368(7):623-32. [https://www.nejm.org/doi/full/10.1056/NEJMoa1209288 link to original article] [https://www.ncbi.nlm.nih.gov/pubmed/23406027 PubMed]
+*'''Code name:''' AZD-6244
+*'''Brand name:''' Koselugo
 [[Category:Drugs]]
@@ Line 21: / Line 27: @@
 [[Category:MAP2K2 inhibitors]]
-[[Category:Ovarian cancer medications]]
+[[Category:Low-grade serous ovarian cancer medications]]
-[[Category:Thyroid cancer medications]]
+[[Category:Thyroid cancer, differentiated medications]]
+[[Category:Uveal melanoma medications]]
-[[Category:Investigational drugs]]
+[[Category:FDA approved in 2020]]
+[[Category:EMA approved in 2020]]
+[[Category:PMDA approved in 2022]]