Radotinib (INN; trade nameSupect), also known by its investigational codeIY5511, is an oralBcr-Abl tyrosine-kinase inhibitor used in the treatment ofPhiladelphia 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 asimatinib.[1]
Radotinib is indicated for the treatment of adult patients withPh+ 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.
Radotinib is a selective inhibitor of theBcr-Abl tyrosine kinase, the abnormal fusion protein expressed in Ph+ CML. It also inhibits theplatelet-derived growth factor receptor (PDGFR).[5] By blocking Bcr-Abl–mediated signaling, radotinib suppresses proliferation of leukemic cells.
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]
^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.ISBN9780124171503.
