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Drug intelligence / Profile preview
radotinib
- Development stage
- Phase 3
- Lead developer
- Il-Yang Pharmaceutical
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Radotinib is an orally available, second-generation small molecule tyrosine kinase inhibitor primarily indicated for the treatment of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML), especially in patients who are resistant or intolerant to other Bcr-Abl tyrosine kinase inhibitors such as imatinib. Its mechanism of action involves selective inhibition of the Bcr-Abl fusion protein by binding to its ATP-binding site, thereby blocking its kinase activity and downstream signaling pathways that promote cancer cell proliferation. Radotinib also inhibits platelet-derived growth factor receptor (PDGFR) and has some activity against other kinases at higher concentrations. The drug was developed by Ilyang Pharmaceutical and is co-marketed by Daewoong Pharmaceutical in South Korea[1][3][4][5][6].
- Brand names
- Supect
- Other names
- radotinib hydrochloride
02
Targets
ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)DDR1 (Discoidin domain receptor 1)EPH (EPH receptor family)LYN (LYN proto-oncogene, Src family tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)
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