Radotinib

Radotinib
Clinical data
Trade names	Supect
ATC code	None;
Identifiers
	IUPAC name 4-Methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyrazin-2-ylpyrimidin-2-yl)amino]benzamide;
CAS Number	926037-48-1;
PubChem CID	16063245;
ChemSpider	17222861;
UNII	I284LJY110;
CompTox Dashboard (EPA)	DTXSID90239069 ;
Chemical and physical data
Formula	C27H21F3N8O
Molar mass	530.515 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Cc1cn(-c2cc(NC(=O)c3ccc(C)c(Nc4nccc(-c5cnccn5)n4)c3)cc(C(F)(F)F)c2)cn1;
	InChI InChI=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); Key:DUPWHXBITIZIKZ-UHFFFAOYSA-N;

Radotinib (INN; trade name Supect), and sometimes referred to by its investigational name IY5511, is a drug for the treatment of different types of cancer, most notably Philadelphia chromosome-positive (Ph⁺) chronic myeloid leukemia (CML)^[1] with resistance or intolerance of other Bcr-Abl tyrosine-kinase inhibitors, such as patients resistant or intolerant to imatinib.

Radotinib is being developed by Ilyang Pharmaceutical Co., Ltd of South Korea^[2] and is co-marketed by Daewoong Pharmaceutical Co. Ltd, in South Korea.^[3] Radotinib completed a multi-national Phase II clinical trial study in 2012^[4] and in August 2011, Ilyang initiated a Phase III, multinational, multi-center, open-label, randomized study for first-line indication.^[5] Its mechanism of action involves inhibition of the Bcr-Abl tyrosine kinase and of platelet-derived growth factor receptor (PDGFR).^[6]

References

^ Bronson J, Black A, Dhar TG, Ellsworth BA, Merritt JR (2013). "To Market, To Market - 2012: Radotinib (Anticancer)". Annual Reports in Medicinal Chemistry. 48: 523–524. doi:10.1016/b978-0-12-417150-3.00028-4. ISBN 9780124171503.
^ "Il-Yang Pharmaceutical".
^ Yoon EK (23 October 2012). "Daewoong will market Ilyang's new leukemia drug". Daily Pharm News. Archived from the original on 2016-03-03.
^ Kim SH, Menon H, Jootar S, Saikia T, Kwak JY, Sohn SK, et al. (July 2014). "Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors". Haematologica. 99 (7): 1191–1196. doi:10.3324/haematol.2013.096776. PMC 4077080. PMID 24705186.
^ Clinical trial number NCT01511289 for "A Phase 3 Multinational, Multi-center, Open-Label, Randomized Study of the Efficacy of Radotinib Versus Imatinib in Newly Diagnosed Ph+ CML Patients in Early Chronic Phase" at ClinicalTrials.gov
^ "Radotinib hydrochloride". NCI Drug Dictionary. National Cancer Institute. 2011-02-02.

[1] Bronson J, Black A, Dhar TG, Ellsworth BA, Merritt JR (2013). "To Market, To Market - 2012: Radotinib (Anticancer)". Annual Reports in Medicinal Chemistry. 48: 523–524. doi:10.1016/b978-0-12-417150-3.00028-4. ISBN 9780124171503.

[2] "Il-Yang Pharmaceutical".

[3] Yoon EK (23 October 2012). "Daewoong will market Ilyang's new leukemia drug". Daily Pharm News. Archived from the original on 2016-03-03.

[4] Kim SH, Menon H, Jootar S, Saikia T, Kwak JY, Sohn SK, et al. (July 2014). "Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors". Haematologica. 99 (7): 1191–1196. doi:10.3324/haematol.2013.096776. PMC 4077080. PMID 24705186.

[5] Clinical trial number NCT01511289 for "A Phase 3 Multinational, Multi-center, Open-Label, Randomized Study of the Efficacy of Radotinib Versus Imatinib in Newly Diagnosed Ph+ CML Patients in Early Chronic Phase" at ClinicalTrials.gov

[6] "Radotinib hydrochloride". NCI Drug Dictionary. National Cancer Institute. 2011-02-02.

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