Supect (radotinib) / IL-Yang Pharm, R-Pharm - LARVOL DELTA

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 | Sponsor: Il-Yang Pharm. Co., Ltd. | Trial completion date: Jun 2025 ➔ Dec 2027

Trial completion date • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology • ABL1 • BCR

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 | Sponsor: Il-Yang Pharm. Co., Ltd. | Trial completion date: Dec 2027 ➔ Jun 2028 | Trial primary completion date: Jun 2026 ➔ Jun 2027

Trial completion date • Trial primary completion date • Chronic Myeloid Leukemia • Leukemia • Oncology

Safety, Tolerability, Pharmacokinetics and Efficacy Study of Radotinib in Parkinson's Disease (clinicaltrials.gov) - P2 | N=43 | Active, not recruiting | Sponsor: Il-Yang Pharm. Co., Ltd. | Recruiting ➔ Active, not recruiting | Trial completion date: Dec 2026 ➔ Apr 2027 | Trial primary completion date: Dec 2025 ➔ Sep 2026

Enrollment closed • Trial completion date • Trial primary completion date • CNS Disorders • Movement Disorders • Parkinson's Disease

Efficacy and Safety of Dose Redution of Radotinib as a First Line Treament in Ph+ CML (clinicaltrials.gov) - P=N/A | N=169 | Active, not recruiting | Sponsor: Il-Yang Pharm. Co., Ltd. | Recruiting ➔ Active, not recruiting | Trial completion date: Dec 2026 ➔ Dec 2027 | Trial primary completion date: Sep 2026 ➔ Jul 2027

Enrollment closed • Trial completion date • Trial primary completion date • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology

Physiologically Based Pharmacokinetic Modeling for Mechanistic Analysis of Food Effects: A Case Study with Radotinib. (PubMed, Pharm Res) - "These findings demonstrate the utility of PBPK modeling for prediction of food effect on radotinib pharmacokinetics."

Journal • PK/PD data

EX VIVO DRUG SENSITIVITY PROFILING OF BONE MARROW CELLS OBTAINED AT DIAGNOSIS FROM PATIENTS WITH CML USING AN AI-ASSISTED MICROFLUIDIC PLATFORM (EHA 2026) - "Discrete concentration gradients of multiple TKIs (imatinib, dasatinib, radotinib, and asciminib) were generated using a programmable pneumatic pumping system, delivering each concentration to 100 chambers. This translational approach may complement molecular diagnostics by providing timely phenotype-based drug response information. Prospective validation in larger cohorts is warranted."

Preclinical • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • ABL1

ANALYSIS OF THE IMPACT OF TYROSINE KINASE INHIBITORS ON RENAL FUNCTION IN PATIENTS WITH CHRONIC-PHASE CHRONIC MYELOID LEUKEMIA (EHA 2026) - "In the first-line setting, 263 patients were treated with imatinib, 128 with flumatinib, 87 with nilotinib, 21 with dasatinib, and 4 with other TKIs (2 asciminib, 2 radotinib)...In the second-line setting, the most frequently used TKI was dasatinib (n=88), followed by nilotinib (n=11), flumatinib (n=11), and olverembatinib (n=1)...This discrepancy may be attributable to the relatively small sample size of dasatinib-treated patients in the first-line group. . Longitudinal changes in eGFR over time in patients receiving first-line TKI therapies"

Clinical • Chronic Kidney Disease • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Nephrology • Renal Disease

OPTIMAL TIMING AND PARAMETERS FOR TYROSINE KINASE INHIBITOR DOSE DE-ESCALATION AFTER ACHIEVING MAJOR MOLECULAR RESPONSE IN CHRONIC MYELOID LEUKEMIA (EHA 2026) - "Patients were initially treated with imatinib (400–800 mg once daily), nilotinib (150–300 mg twice daily), radotinib (200–400 mg twice daily), dasatinib (50–140 mg once daily), or ponatinib (45 mg once daily). Dose reduction effectively alleviates AEs while maintaining durable molecular responses. Further studies are warranted to identify predictors of molecular relapse following TKI dose de-escalation."

Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia

Drug repurposing for glucosyltransferase inhibition for targeted oral biofilm disruption. (PubMed, NPJ Biofilms Microbiomes) - "Importantly, Radotinib selectively inhibited S.m. growth while preserving commensal species. This study identified at least two compounds capable of specifically inactivating a primary virulence factor of S.m. without inhibiting its growth, with a much lower selective pressure for drug resistance development, while simultaneously providing a growth advantage to commensal species that promote oral health."

Journal

Modulating IL-1β-induced pro-atherogenic endothelial responses through drug repurposing. (PubMed, Inflammopharmacology) - "Our findings highlight radotinib and lomitapide as promising repurposed small-molecule inhibitors of IL-1β signaling. By preserving endothelial integrity and dampening inflammatory responses, these compounds may serve as cost-effective and orally available alternatives to current biologic therapies. Further in vivo and mechanistic studies are needed to advance their potential clinical application."

Journal • Atherosclerosis • Cardiovascular • Inflammation • CDH5 • IL1B • IL1R1

Clinical pharmacokinetic characteristics and the food effect of radotinib. (PubMed, Invest New Drugs) - P1, P3 | "The results of the study provide essential pharmacokinetic information for the clinical use of radotinib in the treatment of CML patients. ClinicalTrials.gov, Identifier NCT06461078, NCT03722420."

Journal • PK/PD data • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology • ABL1 • BCR

Computational Repurposing of Nilotinib and Radotinib as SIRT2 Inhibitors for Neurodegenerative Diseases. (PubMed, J Mol Neurosci) - No abstract available

Journal • CNS Disorders

Intramolecular Interactions of Twenty-Eight Amide Derivatives with the C-ALB Kinase using a Theoretical Model as a Therapeutic Alternative to Treat Cancer. (PubMed, Drug Res (Stuttg)) - "Besides, bosutinib, dasatinib, imatinib, nilotinib, and radotinib were used as controls in the DockingServer program.The results displayed different types of aminoacid residues involved in the interaction of amide derivatives with the 1iep protein surface compared to the controls. Finally, the Ki for amide derivatives 1, 19, and 21 were lower compared with bosutinib, dasatinib, imatinib, and nilotinib.Theoretical data indicate that amide derivatives such as 1, 15, 16, 18, 19, and 21 might have a higher affinity for the 1iep protein surface. This phenomenon could be translated as c-Abl kinase inhibition, resulting in a decrease in cancer cell growth."

Journal • Oncology • ABL1

Preliminary safety and efficacy of ELVN-001, a selective active site inhibitor of BCR::ABL1, in patients with CML driven by atypical fusion transcripts (ASH 2025) - P1 | "Thepatient discontinued prior imatinib and nilotinib due to lack of efficacy, had a concurrent diagnosis ofMDS (treated with dasatinib plus azacitidine), a prior allogeneic myeloablative stem cell transplant, andwas last treated with asciminib (discontinued due to lack of efficacy)...The patient discontinued prior nilotinib, dasatinib,ponatinib, asciminib and a combination of asciminib and ponatinib due to lack of efficacy...ELVN-001 demonstrated encouraging anti-CML activity in patients with atypical transcripts, including inpatients with the e13a3 transcript, which is resistant to TKIs targeting the myristoyl pocket."

Clinical • Chronic Myeloid Leukemia • ABL1

Population Pharmacokinetics of Radotinib in Healthy Volunteers and Patients with Chronic Myeloid Leukemia. (PubMed, Pharmaceuticals (Basel)) - "A 400 mg once-daily regimen was predicted to provide comparable systemic exposures to those of other TKIs with similar physiochemical and pharmacological properties to radotinib, and a 36% lower exposure than that of the current 300 mg twice-daily regimen. The model developed in this study adequately describes the population pharmacokinetics of radotinib and provides a basis for optimal, individualized radotinib therapy for patients with CML."

Journal • PK/PD data • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology

Flumatinib for the Treatment of Adult Patients with Resistant or Intolerant Chronic-Phase Chronic Myeloid Leukemia: Results from Real-World Data (ASH 2023) - "Prior therapies included imatinib, dasatinib, nilotinib, olverembatinib, radotinib and ponatinib. Of the 58 patients, only Grade 1 AEs were reported, including diarrhea, rash and eye edema. Conclusion Flumatinib has good efficacy and safety in the treatment of adult patients with resistant or intolerant Chronic-Phase Chronic Myeloid Leukemia, it will be a good choice for second-line or above treatment for CML-CP In clinical practice."

Clinical • Real-world • Real-world evidence • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology • ABL1 • BCR

Improvement of Treatment-Free Remission Rate Following Discontinuation of BCR::ABL1 Tyrosine Kinase Inhibitors in Chronic Phase, Chronic Myeloid Leukemia (ASH 2023) - " Among patients newly diagnosed with CP-CML and treated at least one of TKIs (Imatinib, Nilotinib, Dasatinib, Bosutinib, and Radotinib) as the first treatment, patients who maintained MR4.5 (BCR::ABL1 IS ≤0.0032%) continuously for at least 6 years through qRT-PCR tests were enrolled in this study. Our result demonstrates that TFR rate can be improved in patients who received TKI treatment for approximately 10 years and maintained DMR for more than 6 years regardless of the type of TKI. Based on results, we can confirm one of important factors for safer TFR in CP-CML patients."

Clinical • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology • ABL1

A More Rapid Initial Decline of BCR::ABL1 Transcripts and Longer Treatment Duration with Improvement of Treatment-Free Remission Rate after Discontinuation of Tyrosine Kinase Inhibitors in Chronic Myeloid Leukemia (ASH 2024) - "Methods : Among patients newly diagnosed with CP-CML and treated at least one of TKIs (Imatinib, Nilotinib, Dasatinib, Bosutinib, and Radotinib) as the first treatment, patients who maintained MR4.5 (BCR : : ABL1 IS ≤0.0032%) continuously for at least 4 years through reverse transcriptase quantitative polymerase chain reaction (RT-qPCR) tests were enrolled in this study. Conclusion : Our result demonstrates that TFR rate can be improved in patients who received TKI treatment for approximately 10 years and maintained DMR for more than 6 years regardless of the type of TKI. Based on results, we can confirm that a more rapid initial BCR : : ABL1 decline after commencing TKI and total duration of TKI therapy correlated with an increased probability of achieving TFR eligibility."

Clinical • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology • ABL1

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."

Adverse events • Journal • Acute Kidney Injury • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Nephrology • Oncology • Renal Disease • ABL1 • BCR

Tyrosine kinase inhibitors, nilotinib and radotinib, suppress both catalytic function and mRNA expression of human cytochrome P450 2J2 and 2C8. (PubMed, Drug Metab Pharmacokinet) - "Among the TKIs, nilotinib and radotinib strongly inhibited CYP2J2-dependent astemizole O-demethylation and rivaroxaban hydroxylation, and CYP2C8-mediated paclitaxel 6α-hydroxylation (<20 %), with competitive inhibition constants of 0.41 and 0.22 μM, respectively (for astemizole O-demethylation). Given that their inhibition constants are lower than their reported plasma concentrations, both may substantially suppress CYP2J2 and CYP2C8 functional enzyme levels and enzymatic activities in clinical settings. This suppression could potentially alter vasodilation by affecting 14,15-EET production, influencing CYP2J2 and CYP2C8-mediated drug-disease (conditions) and drug-drug interactions."

Journal • Hematological Malignancies • Leukemia • Oncology

Electric Field-Driven Modulation of Nanomechanical Interactions Between Tyrosine Kinase Inhibitors and Human Serum Albumin: Insights from AFM-Based Force Spectroscopy. (PubMed, Molecules) - "In this study, we investigated how varying electric field strengths (0-100 mV/mm) influence the interfacial interaction between human serum albumin (HSA) and six tyrosine kinase inhibitors (TKIs): imatinib, bosutinib, dasatinib, nilotinib, ponatinib, and radotinib. Notably, more hydrophobic TKIs showed greater responsiveness. These findings highlight the potential of electric fields to modulate protein-drug interactions in a controllable manner, offering a new strategy for the development of electrically tunable drug delivery systems and smart biomedical interfaces."

Journal

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 • Lung Cancer • Oncology • Solid Tumor • MAP2K1

Dose Optimization of Tyrosine Kinase Inhibitors for Chronic Myeloid Leukemia. (PubMed, Clin Pharmacol) - "This review will classify the dose optimization of all approved TKIs (imatinib, dasatinib, nilotinib, bosutinib, ponatinib, asciminib, radotinib) at different stages of treatment based on clinical trials and real-life studies, including dose optimization prior to attempting TFR. In addition, we briefly describe the application of therapeutic drug monitoring in dose optimization and the potential benefits of dose optimization on health-related quality of life."

Journal • Review • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology

REAL-WORLD TREATMENT PATTERNS OF TYROSINE KINASE INHIBITORS IN KOREAN PATIENTS WITH CHRONIC MYELOGENOUS LEUKEMIA (EHA 2025) - "Approval of nilotinib and radotinib (2012) for reimbursement in Korea led to a shift in treatment patterns between 2012-2017. These results provide insights on treatment decision-making and choosing the optimal TKI sequence in pts with CML based in Korea, taking into account the unique treatment landscape."

Clinical • HEOR • Real-world • Real-world evidence • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology • Pulmonary Disease • Respiratory Diseases

PATIENTS WITH CHRONIC MYELOID LEUKEMIA WHO HAVE NOT ACHIEVED MAJOR MOLECULAR RESPONSE HAD SIGNIFICANTLY INCREASED RISK OF DISEASE PROGRESSION WHEN RECEIVING DE-ESCALATION TYROSINE KINASE INHIBITORS (TKIS) TREATMENT (EHA 2025) - "The definition of a lower dosage includes: imatinib < 400 mg/d, nilotinib < 600 mg/d, dasatinib < 100 mg/d, flumatinib < 600 mg /d, radotinib < 600 mg /d, asciminib < 80 mg/d. Compared with patients who reduced the maintenance dose of TKI after achieving MMR, patients receiving TKIs with lower dosage before achieving MMR or discontinued TKI treatment before reaching the TFR criteria had significantly increased risk of treatment failure and disease progression."

Clinical • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology