Radotinib

  1. Home
  2. Wiki
Radotinib
Structural formula
Clinical data
Trade namesSupect
Routes of
administration		Oral (by mouth)
Legal status
Legal status
  • Rx-only (South Korea)
Pharmacokinetic data
MetabolismHepatic
Elimination half-life~13–15 h[1]
ExcretionFecal and renal
Identifiers
  • 4-Methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyrazin-2-ylpyrimidin-2-yl)amino]benzamide
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
3D model (JSmol)
  • Cc1cn(-c2cc(NC(=O)c3ccc(C)c(Nc4nccc(-c5cnccn5)n4)c3)cc(C(F)(F)F)c2)cn1
  • 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), 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).[2] It was developed by Il-Yang Pharmaceutical Co., Ltd (South Korea) and is marketed domestically by Daewoong Pharmaceutical Co., Ltd.[3][4] Radotinib was approved in South Korea in 2012 for patients with resistance or intolerance to other tyrosine kinase inhibitors such as imatinib.[1]

Medical uses

[edit]

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.[1] Its use remains limited to South Korea, where it is prescribed under the brand name Supect.

Mechanism of action

[edit]

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).[5] By blocking Bcr-Abl–mediated signaling, radotinib suppresses proliferation of leukemic cells.

Clinical trials

[edit]

In 2011, Il-Yang initiated a Phase III, multinational, randomized study comparing radotinib with imatinib as first-line therapy in newly diagnosed Ph+ CML.[6] 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.[1]

Common adverse effects observed in clinical studies included hematologic toxicities (thrombocytopenia, neutropenia, anemia), gastrointestinal events, and elevations in liver transaminases.[1]

Regulatory status

[edit]

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

[edit]

References

[edit]
  1. ^ a b c d e 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.
  2. ^ 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.
  3. ^ "Il-Yang Pharmaceutical – Research & Development". Il-Yang Pharmaceutical. Archived from the original on 27 April 2015. Retrieved 10 September 2025.
  4. ^ Yoon EK (23 October 2012). "Daewoong will market Il-Yang's new leukemia drug". Daily Pharm News. Archived from the original on 3 March 2016.
  5. ^ "Radotinib hydrochloride". NCI Drug Dictionary. National Cancer Institute. 2 February 2011.
  6. ^ Clinical trial number NCT01511289 at ClinicalTrials.gov