bosutinib / Generic mfg. - LARVOL DELTA

Characterization of adverse cutaneous effects in the setting of ponatinib, bosutinib, andasciminib for chronic myeloid leukemia patients (AACR 2026) - "BCR-ABL tyrosine kinase inhibitors (TKIs) are used in the treatment of chronic myeloid leukemia (CML) and include second- and third-generation agents: ponatinib, bosutinib, and asciminib. While cutaneous adverse events (cAEs) of first-generation TKIs such as imatinib are well-documented, real-world reports involving newer agents remain limited and poorly described...The significantly increased risk in females aligns with prior literature, possibly due to differences in body type, medication adherence, or reporting. Our limitations include retrospective design and single institution use."

Clinical • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology • Squamous Cell Carcinoma • ABL1 • BCR

Targeted compound screening for the exploration of actionable vulnerabilities in LUSC (ESMO-TAT 2026) - "IC50 values were established for both agents and for gemcitabine and docetaxel. These findings provide a strong translational rationale for repurposing bosutinib and ENMD-2076, alone or in combination with chemotherapy, as biomarker-informed therapeutic strategies for LUSC."

IO biomarker • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • MMP9

Asciminib vs bosutinib in chronic-phase chronic myeloid leukemia previously treated with at least two tyrosine kinase inhibitors: longer-term follow-up of ASCEMBL. (PubMed, Leukemia) - "Fewer grade ≥3 adverse events (AEs) (56.4% vs 68.4%) and AEs leading to treatment discontinuation (7.7% vs 26.3%) occurred with asciminib than with bosutinib. A higher proportion of patients on asciminib than bosutinib remained on treatment and continued to derive benefit over time, supporting asciminib as a standard of care for patients with CML-CP previously treated with ≥2 TKIs."

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

Asciminib (ASC) Demonstrates Favorable Safety and Tolerability Compared with Each Investigator-Selected Tyrosine Kinase Inhibitor (IS TKI) in Newly Diagnosed Chronic Myeloid Leukemia in Chronic Phase (CML-CP) in the Pivotal Phase 3 ASC4FIRST Study (ASH 2024) - "Introduction : About 1/3rd of patients (pts) with newly diagnosed CML discontinue/switch treatments (Tx) regardless of TKI (imatinib [IMA], nilotinib [NIL], dasatinib [DAS], or bosutinib [BOS]). ASC's superior efficacy vs all IS TKIs and more favorable safety/tolerability compared with each IS TKI (IMA, NIL, DAS, and BOS) suggests that ASC may transform the CML Tx paradigm. Key secondary endpoints, including MMR rate at wk 96, and other long-term secondary efficacy and safety/tolerability results, will be presented at ASH 2024."

Clinical • P3 data • Atherosclerosis • Cardiovascular • Chronic Myeloid Leukemia • Congestive Heart Failure • Coronary Artery Disease • Gastroenterology • Gastrointestinal Disorder • Heart Failure • Hematological Disorders • Hematological Malignancies • Immunology • Leukemia • Myocardial Infarction • Oncology • Pancreatitis • Respiratory Diseases • Thrombocytopenia

Identification of Potential Therapeutic Agents for Primary Amebic Meningoencephalitis Using Text Mining and Bioinformatics Analyses. (PubMed, Anal Cell Pathol (Amst)) - "In addition, arsenic trioxide, bortezomib, dasatinib, bosutinib, bevacizumab, paclitaxel, midostaurin, tamoxifen, copanlisib, and pazopanib were identified as potential drugs targeting PAM using PanDrugs software. Our analyses revealed that text mining-related PAM genes were enriched in several pathways, such as peroxisomes and protein localization. We suggest that PAM is linked to other diseases, such as Zellweger's syndrome, leishmaniasis, and periodontitis, and provide potential drugs for effective treatment."

Journal • Atherosclerosis • Cardiovascular • CNS Disorders • Dental Disorders • Gastroenterology • Gastrointestinal Disorder • Immunology • Infectious Disease • Inflammation • Inflammatory Arthritis • Inflammatory Bowel Disease • Malaria • Nephrology • Periodontitis • Rheumatoid Arthritis • Rheumatology

Systematic analysis of UBE2D3 and its association with prognosis, tumor microenvironment, and drug sensitivity in renal clear cell carcinoma. (PubMed, Transl Androl Urol) - "Drug sensitivity analysis revealed that UBE2D3-low tumors were more responsive to vincristine, bosutinib, and ambazone [median inhibitory concentration difference (IC50 diff.) P<0.01], supported by favorable molecular docking affinities. Correspondingly, its loss appears to correlate with advanced disease, an immunosuppressive tumor microenvironment (TME), and unfavorable prognosis. This potential role in modulating immune cell dynamics and drug sensitivity positions UBE2D3 as a promising biomarker for prognostication and personalized therapy selection in KIRC."

Biomarker • Journal • Clear Cell Carcinoma • Clear Cell Renal Cell Carcinoma • Oncology • Renal Cell Carcinoma • Solid Tumor • UBE2D3

How to Optimize CML Treatment in 2026: ELN 2025 and Molecular Guidance (ICKSH 2026) - "Any of the five TKIs, (imatinib, dasatinib, nilotinib, bosutinib, asciminib) approved for frontline therapy of CML -CP may be selected. With the availability of generic imatinib and generic second -generation TKIs, all patients with CML should have access to effective therapies. Allogeneic stem cell transplantation should be considered in patients with CML who progress to accelerated or blast phase (in combination with chemotherapy) after TKI therapy failure and those who have CML resistance to second - or third - generation TKIs while still in chronic phase."

Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • ABL1

Optimizing Frontline Therapy in Ph+ ALL: The Role of Ponatinib and Beyond (ICKSH 2026) - "Several TKIs are available for the treatment of Ph+ ALL, including imatinib (first -generation TKI), dasatinib, nilotinib and bosutinib (second -generation TKIs), and ponatinib (third -generation TKI)...For example, long -term survival >80% has been observed with the combination of dasatinib and blinatumomab in adu lts with newly diagnosed Ph+ ALL...The evolution of therapy for Ph+ ALL is particularly remarkable considering that Ph+ ALL was once considered to be one of the most aggressive forms of leukemia, necessitating treatment with intensive chemotherapy and consolidative allogeneic SCT. However, now chemotherapy -free regimens may perhaps be even more effective than traditional approaches using an intensive chemotherapy backbone."

Acute Lymphocytic Leukemia • Hematological Malignancies • Leukemia • ABL1

Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR) (clinicaltrials.gov) - P2 | N=720 | Recruiting | Sponsor: Canadian Cancer Trials Group | Trial primary completion date: Jan 2026 ➔ Dec 2026

Pan tumor • Trial primary completion date • Tumor mutational burden • B Cell Non-Hodgkin Lymphoma • Hematological Malignancies • Lymphoma • Multiple Myeloma • Non-Hodgkin’s Lymphoma • Oncology • Solid Tumor • BRAF

ASC4FIRST: A Study of Oral Asciminib Versus Other TKIs in Adult Patients With Newly Diagnosed Ph+ CML-CP (clinicaltrials.gov) - P3 | N=406 | Active, not recruiting | Sponsor: Novartis Pharmaceuticals | Trial completion date: Jan 2028 ➔ Jan 2031

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

A Patient guided dose reduction strategy of tyrosine kinase inhibitors in chronic myeloid leukaemia: RODEO study (clinicaltrialsregister.eu) - P3/4 | N=136 | Active, not recruiting | Sponsor: Stichting Radboud universitair medisch centrum | Not yet recruiting ➔ Active, not recruiting

Enrollment closed • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology

A MUC1-ALIX complex regulates extracellular vesicle cargo loading with activated SRC to enhance pancreatic cancer progression. (PubMed, Cancer Lett) - "EVs from SRC inhibitor Bosutinib treated cells showed reduced effects on cell viability, migration, and invasion of MUC1 knockout cells as compared to EVs from untreated cells...Collectively, our findings identify a previously unrecognized role for MUC1 in influencing EV composition and function: influencing loading of oncogenic protein cargoes into EVs. Our data highlight a novel mechanism controlling tumor-specific EV cargo loading and demonstrate that oncogenic cargo in MUC1-associated EVs contributes to pancreatic cancer progression."

Journal • Oncology • Pancreatic Cancer • Solid Tumor • MUC1 • PDCD6IP

Bosutinib-induced palmoplantar keratoderma treated with acitretin. (PubMed, JAAD Case Rep) - No abstract available

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

Key points in selecting first-line therapy for chronic myeloid leukemia (PubMed, Rinsho Ketsueki) - "In Japan, five agents-imatinib (Glivec®), dasatinib (Sprycel®), nilotinib (Tasigna®), bosutinib (Bosulif®), and STAMP inhibitor asciminib (Scemblix®)-are currently approved for first-line therapy. Looking forward, immunologic determinants of TFR and novel therapeutic approaches, including targeting CML stem cells with agents such as asciminib or demethylating drugs, may offer prospects for cure. This review summarizes the current evidence and practical considerations in selecting first-line therapy for chronic-phase CML, with a focus on optimizing long-term outcomes and advancing toward individualized and potentially curative strategies."

Journal • Cardiovascular • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology • ABL1

BosuPeg: Long-acting Low Dose Ropeginterferon for Chronic Myeloid Leukemia Treated With Bosutinib From Diagnosis (clinicaltrials.gov) - P2 | N=212 | Not yet recruiting | Sponsor: St. Olavs Hospital

New P2 trial • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology • ABL1 • BCR

BosuPeg: Long-acting Low Dose Ropeginterferon for Chronic Myeloid Leukemia Treated With Bosutinib From Diagnosis (clinicaltrials.gov) - P2 | N=212 | Completed | Sponsor: St. Olavs Hospital | Recruiting ➔ Completed | Trial completion date: Mar 2028 ➔ Dec 2024 | Trial primary completion date: Feb 2024 ➔ Dec 2024

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

BosuPeg: Long-acting Low Dose Ropeginterferon for Chronic Myeloid Leukemia Treated With Bosutinib From Diagnosis (clinicaltrials.gov) - P2 | N=212 | Recruiting | Sponsor: St. Olavs Hospital | Trial primary completion date: Mar 2023 ➔ Feb 2024

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

BosuPeg: Long-acting Low Dose Ropeginterferon for Chronic Myeloid Leukemia Treated With Bosutinib From Diagnosis (clinicaltrials.gov) - P2 | N=212 | Recruiting | Sponsor: St. Olavs Hospital | Not yet recruiting ➔ Recruiting | Trial completion date: Dec 2028 ➔ Mar 2028

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

Tussilagone inhibits MRGPRX2-mediated mast cell degranulation and suppresses pseudo-allergic reactions. (PubMed, Toxicol Appl Pharmacol) - "Mechanistically, Tus inhibited tolimidone-induced Lyn kinase activation and suppressed SP-and Tween 80-induced β-hexosaminidase release, exhibiting an inhibitory profile comparable to that of the Lyn/Btk antagonist bosutinib. Additionally, Tus attenuated the phosphorylation levels of MRGPRX2 downstream signal molecules, including Btk, PLCγ1, PKC, p38 MAPK, IκB-α and NF-κB (p65). In conclusion, Tus attenuates SP-and Tween 80-induced mast cell activation and pseudo-allergic reactions by targeting the Lyn/Btk/PLCγ1 and p38/NF-κB pathways, highlighting its therapeutic potential for pseudo-allergy."

Journal • Allergy • Immunology • Oncology • CCL2 • CXCL8 • LYN • TNFA

Second- and Third-Generation BCR-ABL Tyrosine Kinase Inhibitors and the Risk of Pulmonary Arterial Hypertension: A Prevalent New-User Design. (PubMed, Circulation) - "Six thousand six hundred twenty-five dasatinib (age 59.7±15.2 years, 44.0% women), 5205 nilotinib (age 55.4±15.0 years, 44.2% women), 2421 bosutinib (age 63.8±14.2 years, 42.1% women),1358 ponatinib (age 57.3±14.9 years, 46.1% women), and 922 asciminib (age 64.3±13.8 years, 43.7% female) new users were each matched with the maximum of available imatinib users on time-conditional propensity score and on duration of prior imatinib use (prevalent users). This study, designed to emulate a randomized trial, suggests that, in French patients with chronic myeloid leukemia treated with BCR-ABL TKIs, dasatinib use is associated with a higher risk of PAH compared with imatinib, while bosutinib and ponatinib exposure may aggravate or trigger a recurrence of PAH in patients with preexisting dasatinib exposure. Whether bosutinib and ponatinib could induce PAH without preexposure to dasatinib remains to be explored."

Journal • Cardiovascular • Chronic Myeloid Leukemia • Hematological Malignancies • Hypertension • Leukemia • Oncology • Pulmonary Arterial Hypertension • Pulmonary Disease • Respiratory Diseases • ABL1 • BCR

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

Efficacy and Safety of Asciminib in Chronic Myeloid Leukemia in Chronic Phase (CML-CP): Interim Results from the Phase 2 ASC2ESCALATE Trial in the Cohort of Patients (Pts) after 1 Prior Tyrosine Kinase Inhibitor (TKI) (ASH 2024) - P2 | "Pts had received prior treatment with imatinib (32.6%), dasatinib (48.8%), nilotinib (16.3%), or bosutinib (2.3%); 76.7% had received their prior TKI for ≥12 mo. These promising results support asciminib as a potential treatment option in these pts. Updated data (data cutoff June 28, 2024) will be presented at the ASH 2024 Annual Meeting."

Clinical • P2 data • Cardiovascular • Chronic Myeloid Leukemia • Cough • Fatigue • Hematological Malignancies • Hypertension • Leukemia • Oncology • Respiratory Diseases

ASCIMINIB (ASC) PROVIDES SUPERIOR EFFICACY AND EXCELLENT SAFETY AND TOLERABILITY VS TYROSINE KINASE INHIBITORS (TKI) IN NEWLY DIAGNOSED CHRONIC MYELOID LEUKEMIA (CML) IN THE PIVOTAL ASC4FIRST STUDY (EHA 2024) - P3 | "ASC, the first BCR::ABL1 inhibitor to Specifically Target theABL Myristoyl Pocket (STAMP), was intentionally designed to be highly specific and minimize off-target effects.We report primary results from ASC4FIRST (NCT04971226), a randomized ph 3 study of ASC vs all currentstandard-of-care frontline TKIs in pts with newly diagnosed CML.Aims:The two primary objectives were to demonstrate superior major molecular response (MMR) rate at wk 48 withASC vs investigator-selected (IS) TKI and ASC vs IS TKI within the stratum of pts with imatinib (IMA) as theirprerandomization-selected (PRS) TKI (ASCIMA vs IS TKIIMA). Pts received ASC (n=201: ASCIMA, n=101; ASC2G, n=100) or an IS TKI (n=204: IS TKIIMA, n=102; IS TKI2G,n=102 [nilotinib, 48%; dasatinib, 41%; and bosutinib, 11%]). Median follow-up was 16.3 and 15.7 mo with ASCand IS TKIs, respectively. At cutoff (Nov 28, 2023), Tx was ongoing in 86%, 62%, and 75% of pts receiving ASC,IMA, and 2G TKIs, respectively (Figure).MMR..."

Clinical • Anemia • Chronic Myeloid Leukemia • Hematological Disorders • Hematological Malignancies • Leukemia • Neutropenia • Oncology • Thrombocytopenia

ASC4FIRST, a pivotal phase 3 study of asciminib (ASC) vs investigator-selected tyrosine kinase inhibitors (IS TKIs) in newly diagnosed patients (pts) with chronic myeloid leukemia (CML): Primary results. (ASCO 2024) - P3 | " Adults with CML were randomly assigned 1:1 to receive ASC 80 mg once daily or an IS TKI at standard label doses, stratified by ELTS risk category and prerandomization selected (PRS) TKI (imatinib [IMA] or second-generation [2G] TKIs), which was selected by investigators before randomization, accounting for pt preference... Pts received ASC (n=201: ASC IMA , n=101; ASC 2G , n=100) or IS TKI (n=204: IS TKI IMA , n=102; IS TKI 2G , n=102 [nilotinib, 48%; dasatinib, 41%; bosutinib, 11%])... ASC is the only agent to show a statistically significant superior efficacy and excellent safety and tolerability vs all current standard-of-care frontline Tx, with potential to be the therapy of choice for CML."

Clinical • Late-breaking abstract • P3 data • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology • ABL1

Efficacy and Safety Results from ASC4MORE, a Randomized Study of Asciminib (ASC) Add-on to Imatinib (IMA), Continued IMA, or Switch to Nilotinib (NIL) in Patients (Pts) with Chronic-Phase Chronic Myeloid Leukemia (CML-CP) Not Achieving Deep Molecular Responses (DMRs) with ≥1 Year of IMA (ASH 2022) - P2, P3 | "In the phase 3 ASCEMBL study, ASC led to superior major molecular response vs bosutinib (BOS) at wk 24 and 96...Top reasons for discontinuation were pt decision in the ASC 40-mg add-on arm (9.5%), AEs in the ASC 60-mg add-on and NIL arms (14.3% and 23.8%, respectively), and physician decision in the IMA arm (57.1%) (pts who crossed over to the ASC 60-mg add-on arm were considered discontinued for IMA arm)... More pts achieved DMR at wk 48 with ASC add-on to IMA vs continued IMA or switch to NIL in pts not achieving DMR with IMA alone for ≥1 y. In this population of pts tolerating IMA for ≥1 y, ASC add-on was generally well tolerated. While not powered to identify the best arm for achievement of DMR in this setting, the high rate of DMR in the ASC add-on arms is promising. Further studies are needed to assess if ASC alone can provide equivalent efficacy and better tolerability vs add-on to IMA."

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