{{Short description|Chemical compound}} {{Drugbox | drug_name = Radotinib | IUPAC_name = 4-Methyl-''N''-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyrazin-2-ylpyrimidin-2-yl)amino]benzamide | image = Radotinib.svg | image_class = skin-invert-image | width = 300 | caption = Structural formula | tradename = Supect | Drugs.com = | MedlinePlus = | pregnancy_AU = | pregnancy_US = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = Rx-only (South Korea) | routes_of_administration = Oral (by mouth) | bioavailability = <!-- data needed --> | protein_bound = <!-- data needed --> | metabolism = Hepatic | elimination_half-life = ~13–15 h<ref name="Kim2014"/> | excretion = Fecal and renal
| CAS_number = 926037-48-1 | PubChem = 16063245 | ChemSpiderID = 17222861 | UNII = I284LJY110 | StdInChI = 1S/C27H21F3N8O/c1-16-3-4-18(9-23(16)37-26-33-6-5-22(36-26)24-13-31-7-8-32-24)25(39)35-20-10-19(27(28,29)30)11-21(12-20)38-14-17(2)34-15-38/h3-15H,1-2H3,(H,35,39)(H,33,36,37) | StdInChIKey = DUPWHXBITIZIKZ-UHFFFAOYSA-N | smiles = Cc1cn(-c2cc(NC(=O)c3ccc(C)c(Nc4nccc(-c5cnccn5)n4)c3)cc(C(F)(F)F)c2)cn1 }}
'''Radotinib''' (INN; trade name '''Supect'''), also known by its investigational code '''IY5511''', is an oral Bcr-Abl tyrosine-kinase inhibitor used in the treatment of Philadelphia chromosome–positive (Ph<sup>+</sup>) chronic myeloid leukemia (CML).<ref name="Bronson2013">{{cite journal | journal = Annual Reports in Medicinal Chemistry | volume = 48 | pages = 523–524 | title = To Market, To Market – 2012: Radotinib (Anticancer) | vauthors = Bronson J, Black A, Dhar TG, Ellsworth BA, Merritt JR | doi = 10.1016/b978-0-12-417150-3.00028-4 | year = 2013 | isbn = 9780124171503}}</ref> It was developed by Il-Yang Pharmaceutical Co., Ltd (South Korea) and is marketed domestically by Daewoong Pharmaceutical Co., Ltd.<ref>{{Cite web | url=http://www.ilyang.co.kr/english/rnd/rnd03.asp | archive-url=https://web.archive.org/web/20150427165650/http://www.ilyang.co.kr/english/rnd/rnd03.asp | url-status=dead | title=Il-Yang Pharmaceutical – Research & Development | publisher=Il-Yang Pharmaceutical | archive-date=27 April 2015 | access-date=10 September 2025}}</ref><ref>{{cite web | vauthors = Yoon EK | date = 23 October 2012 |url=http://www.dailypharm.com/Users/News/EnglishNews.html?NewsID=3108&nStart=1023 |title= Daewoong will market Il-Yang's new leukemia drug |work = Daily Pharm News |archive-date=3 March 2016 | archive-url = https://web.archive.org/web/20160303221246/http://www.dailypharm.com/Users/News/EnglishNews.html?NewsID=3108&nStart=1023 |url-status=dead}}</ref> Radotinib was approved in South Korea in 2012 for patients with resistance or intolerance to other tyrosine kinase inhibitors such as imatinib.<ref name="Kim2014">{{cite journal | vauthors = Kim SH, Menon H, Jootar S, Saikia T, Kwak JY, Sohn SK, Park JS, Jeong SH, Kim HJ, Kim YK, Oh SJ, Kim H, Zang DY, Chung JS, Shin HJ, Do YR, Kim JA, Kim DY, Choi CW, Park S, Park HL, Lee GY, Cho DJ, Shin JS, Kim DW | display-authors = 6 | title = Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors | journal = Haematologica | volume = 99 | issue = 7 | pages = 1191–1196 | date = July 2014 | pmid = 24705186 | pmc = 4077080 | doi = 10.3324/haematol.2013.096776 }}</ref>
== Medical uses == Radotinib is indicated for the treatment of adult patients with Ph+ CML in the chronic phase who are resistant or intolerant to prior therapy with first-generation tyrosine kinase inhibitors such as imatinib.<ref name="Kim2014"/> Its use remains limited to South Korea, where it is prescribed under the brand name Supect.
== Mechanism of action == Radotinib is a selective inhibitor of the Bcr-Abl tyrosine kinase, the abnormal fusion protein expressed in Ph<sup>+</sup> CML. It also inhibits the platelet-derived growth factor receptor (PDGFR).<ref>{{Cite web | url = https://www.cancer.gov/drugdictionary?cdrid=723999 | work = NCI Drug Dictionary | publisher = National Cancer Institute | title = Radotinib hydrochloride | date = 2 February 2011}}</ref> By blocking Bcr-Abl–mediated signaling, radotinib suppresses proliferation of leukemic cells.
== Clinical trials == In 2011, Il-Yang initiated a Phase III, multinational, randomized study comparing radotinib with imatinib as first-line therapy in newly diagnosed Ph<sup>+</sup> CML.<ref>{{ClinicalTrialsGov|NCT01511289}}</ref> A Phase II trial demonstrated efficacy and safety in patients resistant or intolerant to other Bcr-Abl inhibitors, with major cytogenetic response rates comparable to second-generation drugs such as nilotinib.<ref name="Kim2014"/>
Common adverse effects observed in clinical studies included hematologic toxicities (thrombocytopenia, neutropenia, anemia), gastrointestinal events, and elevations in liver transaminases.<ref name="Kim2014"/>
== Regulatory status == Radotinib received regulatory approval in South Korea in 2012. As of 2025, it has not been approved by the U.S. Food and Drug Administration (FDA) or the European Medicines Agency (EMA).
== See also == * Imatinib * Nilotinib * Dasatinib * Bcr-Abl tyrosine-kinase inhibitors
== References == {{Reflist}}
{{Extracellular chemotherapeutic agents}} {{Growth factor receptor modulators}}
Category:Benzamides Category:Imidazoles Category:Pyrazines Category:Aminopyrimidines Category:Tyrosine kinase inhibitors Category:Trifluoromethyl compounds Category:Cancer treatments