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1m
BCR-ABL tyrosine kinase inhibitors associated acute kidney injury: a pharmacovigilance study based on the FAERS database with a case report. (PubMed, BMC Nephrol)
TKIs, including flumatinib, may cause AKI; however, FAERS-based disproportionality analysis does not indicate an increased renal safety signal compared to non-TKIs. Among TKIs, dasatinib and nilotinib have lower reporting disproportionality than imatinib does, suggesting a potential therapeutic advantage of their use for patients with kidney diseases.
Journal • Adverse events
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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dasatinib • imatinib • Iclusig (ponatinib) • Tasigna (nilotinib) • bosutinib • Hansoh Xinfu (flumatinib) • Supect (radotinib)
3ms
In silico repurposing of FDA-approved drugs against MEK1: structural and dynamic insights into lung cancer therapeutics. (PubMed, Front Pharmacol)
Radotinib and Alectinib exhibited superior docking scores (-10.5 and -10.2 kcal/mol), outperforming the reference MEK1 inhibitor Selumetinib (-7.2 kcal/mol). A limitation of this in silico study is the absence of experimental validation, which will be addressed in future work. Experimental validation is essential to confirm their efficacy and safety in MEK1-linked malignancies.
FDA event • Journal
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MAP2K1 (Mitogen-activated protein kinase kinase 1)
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Koselugo (selumetinib) • Alecensa (alectinib) • Supect (radotinib)
7ms
Trial completion
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Supect (radotinib)
12ms
Chemotherapeutic potential of radotinib against blood and solid tumors: A beacon of hope in drug repurposing. (PubMed, Bioorg Chem)
Several second-generation tyrosine kinase inhibitors (2GTKIs), such as nilotinib, dasatinib, bosutinib, and radotinib (RTB), followed the groundbreaking introduction of imatinib. This review is the first attempt that extensively presents a compilation of data on RTB and describes its therapeutic potential against blood and solid tumors. Further investigations on RTB could expand its chemotherapeutic usage in various solid tumors and enhance the possibility of drug repurposing in cancer therapy.
Review • Journal
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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dasatinib • imatinib • Tasigna (nilotinib) • bosutinib • Supect (radotinib)
1year
Clinical Trial to Investigate the Effects of Food on the Pharmacokinetics and Safety of Orally Administered Radotinib (clinicaltrials.gov)
P1, N=24, Active, not recruiting, Il-Yang Pharm. Co., Ltd. | Not yet recruiting --> Active, not recruiting
Enrollment closed
|
Supect (radotinib)
1year
New trial
|
Supect (radotinib)
1year
A Phase 3 Study for the Efficacy and Safety of Radotinib in CP-CML Patients With Failure or Intolerance to Previous TKIs (clinicaltrials.gov)
P3, N=173, Recruiting, Il-Yang Pharm. Co., Ltd. | Trial completion date: Apr 2025 --> Dec 2027 | Trial primary completion date: Jan 2025 --> Jun 2026
Trial completion date • Trial primary completion date
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
|
BCR-ABL1 mutation
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imatinib • Supect (radotinib)
1year
Targeting STAT3, FOXO3a, and Pim-1 kinase by FDA-approved tyrosine kinase inhibitor-Radotinib: An in silico and in vitro approach. (PubMed, Arch Pharm (Weinheim))
Two compounds, namely, radotinib and capmatinib, were identified as top compounds using molecular docking. The Western blot analysis assay showed that the phosphorylation level of STAT3 was significantly decreased upon radotinib treatment. Taken together, our findings suggest that radotinib, which is currently used in the treatment of chronic myeloid leukemia (CML), could be considered as a potential candidate for repurposing in the treatment of HCC.
FDA event • Preclinical • Journal
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STAT3 (Signal Transducer And Activator Of Transcription 3) • PIM1 (Pim-1 Proto-Oncogene) • FOXO3 (Forkhead box O3)
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Tabrecta (capmatinib) • Supect (radotinib)
over1year
Safety, Tolerability, Pharmacokinetics and Efficacy Study of Radotinib in Parkinson's Disease (clinicaltrials.gov)
P2, N=40, Recruiting, Il-Yang Pharm. Co., Ltd. | Trial completion date: May 2025 --> Dec 2026 | Trial primary completion date: Jun 2024 --> Dec 2025
Trial completion date • Trial primary completion date
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Supect (radotinib)
over1year
New P1 trial
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Supect (radotinib)
over1year
Hematopoietic cell kinase as a nexus for drug repurposing: implications for cancer and HIV therapy. (PubMed, J Biomol Struct Dyn)
Our findings highlighted the potential of Nilotinib and Radotinib as promising candidates against HCK that offer valuable insights into their binding mechanisms. This computational approach provides a comprehensive understanding of drug interactions with HCK and sets the stage for future experimental validation and drug development endeavors.Communicated by Ramaswamy H. Sarma.
Journal
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HCK (HCK Proto-Oncogene)
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Tasigna (nilotinib) • Supect (radotinib)
almost2years
Randomized Evaluation of Radotinib Versus Imatinib in Phase III Study for Efficacy With Chinese Patients (RERISE China) (clinicaltrials.gov)
P3, N=238, Active, not recruiting, Il-Yang Pharm. Co., Ltd. | Trial completion date: Dec 2023 --> Jun 2025
Trial completion date
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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imatinib • Supect (radotinib)