Radotinib Chemical Properties

Density 

1.40±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

≥26.55 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O

form 

solid

pka

12.94±0.70(Predicted)

Radotinib Usage And Synthesis

Description

Radotinib, an inhibitor of Bcr–Abl tyrosine kinase,was approved in January 2012 in Korea as a second-line treatment for chronic myeloid leukemia (CML). Radotinib is a TKI with a similar structure to the second-generation TKI, nilotinib, in which a pyridyl group has been replaced with a pyrazinemoiety. The in vitro activity of radotinib against a variety of tumor cell lines is disclosed in an issued patent. Radotinib was significantly more potent than imatinib in all of the cell lines tested. The synthesis of radotinib via amide coupling is described in the patent literature.

Originator

Il-Yang (Korea)

Uses

Radotinib is tyrosine kinase inhibitor. In a biological study, it can induce cytotoxicity in c-KIT-positive malignancies including acute myeloid leukemia and small cell lung cancer in human making it potential target agent for treatment of such malignancies. It is a COVID19-related research product.

Indications

Radotinib (Supect(R), Il-Yang Pharmaceutical) is a Bcr–Abl inhibitor that was approved in South Korea in 2012 for the treatment of imatinib-resistant CML. Radotinib, which has a terminal 4-(pyridine-2-yl) pyrimidine moiety, was developed based on the previously approved Bcr–Abl inhibitors nilotinib. Radotinib has equivalent efficacy with that of other second-generation Bcr–Abl inhibitors and is well tolerated in chronic-phase CML patients. The lower cost of radotinib compared with other FDA-approved Bcr–Abl inhibitors makes it an attractive alternative for the treatment of CML in developing nations.

brand name

Supect

in vitro

radotinib couples to bcr-abl and reduce the phosphorylation of bcr-abl target protein crkl. the pre-clinical studies shows superiority of radotinib to imatinib in both wild-type and mutant bcr-abl1 positive cml cell lines. [1]

References

1. kim sh, menon h, jootar s et al. efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to bcr-abl1 tyrosine kinase inhibitors. haematologica. 2014 jul;99(7):1191-6.

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