Leukeran (chlorambucil) / GSK 
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  • ||||||||||  Review, Journal:  Management of Mycosis Fungoides and S (Pubmed Central) -  Mar 12, 2025   
    Off-label oral therapies include methotrexate, acitretin, and chlorambucil...Chlorambucil is mainly used to treat erythrodermic MF. Investigational oral therapies for MF include tenalisib, duvelisib, cerdulatinib, lenalidomide, bortezomib, and azacytidine, and direct comparison studies between these investigational agents and FDA-approved therapies should be undertaken to better understand their role in the management of MF and SS.
  • ||||||||||  Leukeran (chlorambucil) / GSK
    Journal:  Regulating the cytotoxicity of anticancer drugs by pillar[6]arene-based host-guest complex. (Pubmed Central) -  Feb 5, 2025   
    Herein, a delivery system for the chemotherapeutic drug chlorambucil (CLB) was developed using the host-guest interaction with amino-pillar[6]arene (NP6)...This process blocks drug efflux while releasing CLB, thereby synergistically enhancing the antitumor effects on HeLa cells. This "one stone, two birds" design strategy-where host-guest complexes facilitate both direct drug delivery and synergistic enhancement of antitumor properties via ATP binding, opens a new perspective for constructing multifunctional supramolecular chemotherapeutic platforms based on pillar[n]arene.
  • ||||||||||  Leukeran (chlorambucil) / GSK
    Journal:  Photoresponsive prodrug-based liposomes for controllable release of the anticancer drug chlorambucil. (Pubmed Central) -  Dec 11, 2024   
    Cell viability assays showed that LNC liposomes demonstrated very low cytotoxicity in the dark and high cellular toxicity upon light irradiation, with toxicity even higher than free CBL. Our results suggest that our photoresponsive lipid prodrug represents a promising strategy to construct controlled DDS for cancer therapy.
  • ||||||||||  Leukeran (chlorambucil) / GSK
    Journal, Companion diagnostic:  Self-Activated Cascade-Tailored Small Molecule for Cancer Therapy, Companion Diagnostics, and "Theranostic Correlation" Evaluation. (Pubmed Central) -  Dec 9, 2024   
    This activation triggers the production of the near-infrared dye Hcy-NH2, generating both near-infrared fluorescence and photoacoustic signals for monitoring the apoptosis process. The excellent "theranostic correlation" between the imaging signal and therapeutic response, as demonstrated in orthotopic breast tumors, highlights the potential of Cbl-DEVD-Hcy for effective tumor therapy and precise CDx in the body.
  • ||||||||||  Leukeran (chlorambucil) / GSK
    Review of Rare Association between Chronic Lymphocytic Leukemia and Chromic Myeloid Leukemia () -  Dec 7, 2024 - Abstract #ASH2024ASH_8840;    
    Cases of CLL First treated with wait and watch or chemotherapy 7/13 (54%) , chemotherapy protocols were FCR or Chlorambucil as most of reported cases before Bruton Tyrosine Kinase Inhibitors (BTK) era...More studies and collaboration with large number is needed to study the mechanism and pathophysiology of this association. Currently there is no guidelines on how to treat patients with simultaneously CLL and CML .
  • ||||||||||  Calquence (acalabrutinib) / AstraZeneca
    Validation and Implementation of Flow Cytometry Based Minimal Residual Disease (MRD) Assay for Chronic Lymphocytic Leukemia (CLL) Clinical Studies () -  Dec 7, 2024 - Abstract #ASH2024ASH_8798;    
    P3
    Patients with CR or CRi in the acalabrutinib-obinutuzumab arm achieved higher rates of undetectable MRD (uMRD) in peripheral blood samples vs patients with CR or CRi receiving acalabrutinib monotherapy and chlorambucil-obinutuzumab (40.9% vs 8.8% and 8.3%, respectively).Conclusions : Validated six- color flow cytometry CLL- MRD assay is a robust test that has been successfully implemented (exploratory) and proven useful for global clinical studies, as demonstrated by clinical results obtained in ELEVATE-TN study. This flow cytometry assay is being implemented in several global clinical studies as an endpoint (secondary) including in an ongoing phase 3 study AMPLIFY (ACE-CL-311; NCT03836261).
  • ||||||||||  Yinuokai (orelabrutinib) / InnoCare, Biogen
    Orelabrutinib-Bruton Tyrosine Kinase Inhibitor-Based Regimens in the Treatment of Marginal Zone Lymphoma: A Retrospective Study () -  Dec 7, 2024 - Abstract #ASH2024ASH_8369;    
    Among the 14 untreated pts with a median age of 58.5 years, the treatment regimens were as follows : orelabrutinib alone for 2 pts, orelabrutinib combined with anti-CD20 monoclonal antibody for 10 pts, orelabrutinib combined with anti-CD20 monoclonal antibody and lenalidomide for 1 pt, and orelabrutinib combined with chlorambucil for 1 pt...Regarding the 11 pts who received later-line therapy, the median age was 67 years, with treatment regimens including orelabrutinib monotherapy for 8 pts, orelabrutinib plus an anti-CD20 monoclonal antibody for 2 pts, and orelabrutinib plus BR (bendamustine and rituximab) for 1 pt...At the time of data cut-off, no deaths were observed.Conclusions : This retrospective data indicates promising anti-tumor activity of chemotherapy-free regimens based on orelabrutinib in MZL. Prospective studies are warranted to guide orelabrutinib in MZL.
  • ||||||||||  Leukeran (chlorambucil) / GSK
    Journal:  Dual stimuli-responsive biotinylated polymer-drug conjugate for dual drug delivery. (Pubmed Central) -  Nov 20, 2024   
    Fostered by the aforementioned conceptualization, our quest to develop an ideal polymer-drug conjugate has originated the present investigation of developing a reactive oxygen species (ROS) and esterase-responsive self-assembled polymer-drug (chlorambucil, CBL) conjugate with biotin pendants (DP2) for cancer cell targeting, surrogating another antineoplastic drug, doxorubicin (DOX) via physical encapsulation (DP2@DOX)...Furthermore, the selective internalization of the fluorophore-tagged DOX-loaded polymer (DP4@DOX) in HeLa cells compared to HEK 293T cells was confirmed by confocal microscopy and flow cytometry. In summary, the present investigation demonstrates a state-of-the-art self-assembled polymer-drug conjugate as a next-generation dual stimuli-responsive drug delivery vehicle.
  • ||||||||||  Leukeran (chlorambucil) / GSK
    Journal, Surgery:  Cell membrane-camouflaged nanoarchitectonics of photosensitizer nanoparticles for enhanced phototherapy in surgery. (Pubmed Central) -  Nov 19, 2024   
    Herein, we report the cancer membrane biomimetic nanoparticles assembled by Chlorin e6 (Ce6) and chlorambucil (CRB)...Intriguingly, surgical resection is performed after phototherapy in this treatment regimen, which can effectively reduce the wound area. Together, this work provided a feasible and creative method for tumor clinical therapy for its patient-centric and humanitarian focus.
  • ||||||||||  berzosertib (M6620) / EMD Serono, Leukeran (chlorambucil) / GSK
    Journal:  Targeting ATR Kinase as a Strategy for Canine Lymphoma and Leukaemia Treatment. (Pubmed Central) -  Nov 13, 2024   
    Berzosertib also acted synergistically with chlorambucil, probably by preventing DNA damage repair as a consequence of S-phase arrest abrogation. In conclusion, ATR inhibition may provide a new therapeutic option for the treatment of canine lymphomas and leukaemias, but further studies are required to determine potential biomarkers of their susceptibility.
  • ||||||||||  Leukeran (chlorambucil) / GSK
    Journal:  Evaluation of the Amount of Compounded Chemotherapy Drugs: A Comparison Between Nine Compounding Pharmacies. (Pubmed Central) -  Nov 13, 2024   
    Heterogeneity between different batches within the same pharmacy ranged from 0.4% to 58.3% for the 503A pharmacies and 5% to 14.8% for the 503B pharmacy. Although the drug amounts of compounded cyclophosphamide and chlorambucil manufactured by the 503B compounding pharmacy was more reliably maintained compared to that compounded by the 503A pharmacies, there was ultimately still potential for variability in drug amounts regardless of the pharmacy designation.
  • ||||||||||  Leukeran (chlorambucil) / GSK, Rituxan (rituximab) / Roche
    Clinical Outcomes in Consecutive Newly Diagnosed Patients with Waldenstrom's Macroglobulinemia Treated with Different Regimens in the Real-World Setting (Halls G-H (San Diego Convention Center)) -  Nov 6, 2024 - Abstract #ASH2024ASH_5096;    
    Results Out of the 711 NDWM pts, 63 (8.9%) were treated with BDR (n=35) / BDR-C (n=28), 263 (37.0%) with DRC, 57 (8.0%) with BTKi and 328 (46.1%) with other older regimens including chlorambucil-based combinations (n=159), chemoimmunotherapy regimens such as RCHOP/RCOP (n=58) and rituximab monotherapy (n=50)...The lack of overt OS benefit, may be due to the use of modern effective salvage therapies, the advanced age of a significant proportion of WM pts which is related to non-WM related mortality and the shorter follow up of the BTKi cohort. Our data suggest that the evaluation of the benefit of new treatments should not be restricted only to traditional endpoints such as PFS, OS and response rates, but should evaluate other patient-oriented metrics including QOL and toxicity burden, especially when continuous is compared to fixed duration treatments.
  • ||||||||||  Leukeran (chlorambucil) / GSK, Imbruvica (ibrutinib) / AbbVie, J&J
    The Impact of Therapeutic Selective Pressure on the Evolutionary Landscape of Chronic Lymphocytic Leukemia (Halls G-H (San Diego Convention Center)) -  Nov 6, 2024 - Abstract #ASH2024ASH_3907;    
    P3
    CONCLUSION Our analyses highlight the need to interrogate the molecular features of CLL in relation to the impact of therapeutic selective pressure imposed by BTK inhibition, which appear distinct from exposure to chemotherapy. Ongoing analyses aim to identify relationships between patterns of growth and subclonal growth rates molecular and clinical features.
  • ||||||||||  Leukeran (chlorambucil) / GSK, Rituxan (rituximab) / Roche
    Addition of Monoclonal Protein to MALT-IPI Improved Identification of MALT Patients at High Risk of Progression with Current First-Line Therapies (Room 6A (San Diego Convention Center)) -  Nov 6, 2024 - Abstract #ASH2024ASH_2304;    
    MALT international prognostic index (IPI) was derived from the IELSG-19 trial wherein patients (pts) were randomized to rituximab (R), chlorambucil, or their combination...ResultsThe study included 468 pts (72% aged ?70 years; 56% women; 42% stage 3/4), whose EMZL was treated with first-line R monotherapy (62%), R-bendamustine (29%), or RCHOP/RCVP (9%)...Measuring the presence of M-protein at diagnosis in all newly diagnosed pts may improve prognostication and influence the choice of therapy. Neither MALT-IPI nor EMZL-MPI provide sufficient prognostication for pts receiving combination immunochemotherapy, and novel prognostic biomarkers are needed for stratification in this setting.
  • ||||||||||  Leukeran (chlorambucil) / GSK, Rituxan (rituximab) / Roche
    Journal, Real-world evidence, Real-world:  Real-world data for marginal zone lymphoma patients in the French REALYSA cohort: The REALMA study. (Pubmed Central) -  Oct 1, 2024   
    At end of first line, overall response rate was 93% among treated patients with 75% of complete response. This French nationwide study provided for the first time prospective RWD on clinical characteristics, initial management and treatment response of MZL patients.
  • ||||||||||  Leukeran (chlorambucil) / GSK
    Journal:  Enhanced DNA damage and anti-proliferative activity of a novel ruthenium complex with a chlorambucil-decorated ligand. (Pubmed Central) -  Sep 2, 2024   
    Targeted studies were subsequently undertaken using 2 to elucidate mechanistic aspects, including the assessment of ruthenium cellular uptake, cell cycle arrest, production of reactive oxygen species (ROS), western blotting and DNA damage (comet test). Overall, data highlight that the anticancer activity provided by 2 primarily affects the mitochondria pathway with a potential additional contribution from DNA damage.
  • ||||||||||  Campath (alemtuzumab) / Sanofi, Leukeran (chlorambucil) / GSK
    T-Cell Prolymphocytic Leukemia: A Case Report (LEVEL 3, HALL B3) -  Aug 30, 2024 - Abstract #SOHO2024SOHO_509;    
    Interventions: We started chlorambucil plus prednisone while waiting for alemtuzumab. He didn't respond and died 4 months later.
  • ||||||||||  Leukeran (chlorambucil) / GSK
    Journal:  A metal-coordination stabilized small-molecule nanomedicine with high drug-loading capacity and synergistic photochemotherapy for cancer treatment. (Pubmed Central) -  Aug 13, 2024   
    Here, we propose a small-molecule nanomedicine (CMC NP) directly assembled using a chemotherapeutic drug (chlorambucil, CBL) and a phototherapeutic agent (chlorin e6, Ce6), and stabilized by metal coordination...Owing to the multifaceted efforts from photodynamic, photothermal and chemo-therapies, the CMC NP exhibits excellent antitumor efficacy with negligible systemic toxicity which is untenable in traditional CBL-induced chemotherapy. Therefore, this study provides a feasible strategy for overcoming existing challenges and presents a potential opportunity to augment the clinical therapeutic effectiveness associated with conventional nanomedicine.
  • ||||||||||  Leukeran (chlorambucil) / GSK
    Journal:  Therapeutic effect of F127-folate@PLGA/CHL/IR780 nanoparticles on folate receptor-expressing cancer cells. (Pubmed Central) -  Aug 7, 2024   
    This study reports the development of a novel multifunctional nanoparticle carrier system based on poly(?,?-lactic-co-glycolic acid) (PLGA) for the targeted delivery of the chemotherapeutic agent chlorambucil (CHL) and the imaging agent IR780...Additionally, the F127-folate@PLGA/CHL/IR780 nanoparticles exhibited a lower IC50 value against cancer cells than non-targeted F127@PLGA/CHL/IR780 nanoparticles. These findings suggest that the developed F127-folate@PLGA/CHL/IR780 nanoparticles hold promise as a theragnostic system for targeted cancer therapy and diagnosis, leveraging the advantages of PLGA, folate targeting, and the integration of therapeutic and imaging agents.
  • ||||||||||  Campath (alemtuzumab) / Sanofi, Adcetris (brentuximab vedotin) / Takeda, Pfizer, Leukeran (chlorambucil) / GSK
    Granulomatous Slack Skin: An Unusual Variant of Mycosis Fungoides  (Poster Area) -  Aug 5, 2024 - Abstract #EADV2024EADV_3086;    
    These findings suggest that the developed F127-folate@PLGA/CHL/IR780 nanoparticles hold promise as a theragnostic system for targeted cancer therapy and diagnosis, leveraging the advantages of PLGA, folate targeting, and the integration of therapeutic and imaging agents. Considering the patient
  • ||||||||||  Leukeran (chlorambucil) / GSK
    Preclinical, Journal:  Single-Photon Deep-Red Light-Triggered Direct Release of an Anticancer Drug: An Investigative Tumor Regression Study on a Breast Cancer Spheroidal Tumor Model. (Pubmed Central) -  Jun 24, 2024   
    Here, we present perylenemonoimide nanoparticle-based vehicles engineered for deep-red light activation, enabling direct chlorambucil release...The efficacy of the said drug delivery system was evaluated in both two-dimensional and three-dimensional spheroidal cancer models, demonstrating significant tumor regression attributed to apoptotic cell death induced by efficient drug release within cells and spheroids. This approach holds promise for advancing targeted breast cancer therapy, enhancing treatment efficacy and minimizing adverse effects.