Radotinib
Part of the metabolic pathway of Radotinib. See the timeline on the metabolic highway.
Overview
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⁺) chronic myeloid leukemia (CML). It was developed by Il-Yang Pharmaceutical Co., Ltd (South Korea) and is marketed domestically by Daewoong Pharmaceutical Co., Ltd. Radotinib was approved in South Korea in 2012 for patients with resistance or intolerance to other tyrosine kinase inhibitors such as imatinib.[1–4] WP
Uses, dosage and effects
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. Its use remains limited to South Korea, where it is prescribed under the brand name Supect.[4] WP
Pharmacology
Mechanism of action
Radotinib is a selective inhibitor of the Bcr-Abl tyrosine kinase, the abnormal fusion protein expressed in Ph⁺ CML. It also inhibits the platelet-derived growth factor receptor (PDGFR). By blocking Bcr-Abl–mediated signaling, radotinib suppresses proliferation of leukemic cells.[5] WP
Chemistry
- Formula
- C27H21F3N8O PC
- CAS number
- 926037-48-1 PC
- Molar mass (g/mol)
- 530.5 PC
- IUPAC name (computed by PubChem)
- 4-
methyl- PCN- [3- (4- methylimidazol- 1- yl) - 5- (trifluoromethyl) phenyl] - 3- [(4- pyrazin- 2- ylpyrimidin- 2- yl) amino] benzamide - SMILES
- CC1=C(C=C(C=C1)
C(=O) PCNC2=CC(=CC(=C2) C(F) (F) F) N3C=C(N=C3) C) NC4=NC=CC(=N4) C5=NC=CN=C5 - InChIKey
- DUPWHXBITIZIKZ-
UHFFFAOYSA- PCN - PubChem CID
- 16063245
Harm reduction information
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Sources
- Journal / agency Bronson J, Black A, Dhar TG, Ellsworth BA, Merritt JR. To Market, To Market – 2012: Radotinib (Anticancer). Annual Reports in Medicinal Chemistry. 2013. doi:10.1016/b978-0-12-417150-3.00028-4
- Other Il-Yang Pharmaceutical – Research & Development
- Other Yoon EK. Daewoong will market Il-Yang's new leukemia drug. 23 October 2012
- Journal / agency 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. Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors. Haematologica. July 2014. doi:10.3324/haematol.2013.096776 · PMID 24705186 · PMC4077080
- Other Radotinib hydrochloride. 2 February 2011
Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), PubChem (public domain). Each value links to the exact revision it came from.