Radotinib Property

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)

color 

Light yellow to yellow

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H317May cause an allergic skin reaction

H318Causes serious eye damage

H334May cause allergy or asthma symptoms or breathing difficulties if inhaled

H335May cause respiratory irritation

H341Suspected of causing genetic defects

H361Suspected of damaging fertility or the unborn child

H370Causes damage to organs

H413May cause long lasting harmful effects to aquatic life

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P272Contaminated work clothing should not be allowed out of the workplace.

P273Avoid release to the environment.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P284Wear respiratory protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P341IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P308+P313IF exposed or concerned: Get medical advice/attention.

P310Immediately call a POISON CENTER or doctor/physician.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P333+P313IF SKIN irritation or rash occurs: Get medical advice/attention.

P342+P311IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician.

P363Wash contaminated clothing before reuse.

P405Store locked up.

P501Dispose of contents/container to..…

Radotinib Chemical Properties,Usage,Production

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.