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 1 Product   0 Diseases   1 Product   9 Trials   209 News 


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  • ||||||||||  Actimab-A (lintuzumab-Ac225) / Actinium
    ANTILEUKEMIC ACTIVITY OF CD33-DIRECTED MUTATION-AGNOSTIC LINTUZUMAB-AC225 IN KMT2A MUTANT AML (Poster Area (Hall 7)) -  May 15, 2024 - Abstract #EHA2024EHA_939;    
    Combination of CD33-targeted radionuclide therapy with menin inhibitorsignificantly improves AML control, demonstrating that targeted radiotherapy approaches can augment menin-targeted therapy. Based on these findings, the combination of lintuzumab-Ac225 with mutation-targetedagents may enhance anti-leukemic response compared to single-agent approaches.
  • ||||||||||  MI-503 / Kura Oncology
    Direct targeting of the COMPASS complex inhibits neuroblastoma growth by inhibiting cancer stem cells (Section 43) -  Mar 5, 2024 - Abstract #AACR2024AACR_6549;    
    Our data show that MI-503 or MEN1 knockdown leads to significant inhibition of NB growth by directly inhibiting NB CSCs in both in vitro and in vivo tumor models. Further developing these epigenetic-based therapeutic strategies and combining them with current therapies will pave the way for effectively managing NB.
  • ||||||||||  Zolinza (vorinostat) / Merck (MSD), ziftomenib (KO-539) / Kura Oncology, Blincyto (blinatumomab) / Astellas, Amgen
    Enrollment open:  TINI 2: Total Therapy for Infants With Acute Lymphoblastic Leukemia II (clinicaltrials.gov) -  Jan 4, 2024   
    P1/2,  N=90, Recruiting, 
    Recent phase Not yet recruiting --> Recruiting
  • ||||||||||  UM-164 / University of Michigan
    UHRF1-Mediated Epigenetic Reprogramming Regulates Glycolysis to Promote Progression of B-Cell Acute Lymphoblastic Leukemia (SDCC - Halls G-H) -  Nov 3, 2023 - Abstract #ASH2023ASH_5780;    
    Furthermore, UM164 demonstrated the ability to inhibit the proliferation of B-ALL cells both in vitro and in vivo, leading to prolonged survival in a B-ALL mouse model. In conclusion, we have unraveled the molecular mechanisms of epigenetic and metabolic rearrangements in relapsed/refractory B-ALL, and have provided potential targeted therapeutic strategies to improve its unfavorable prognosis.
  • ||||||||||  Zolinza (vorinostat) / Merck (MSD), ziftomenib (KO-539) / Kura Oncology, Blincyto (blinatumomab) / Astellas, Amgen
    Outcome of Infants Treated on Total Therapy for Infants with Acute Lymphoblastic Leukemia I: Results from a Non-Randomized Multi-Center Study (Grand Hyatt - Grand Hall C) -  Nov 3, 2023 - Abstract #ASH2023ASH_4974;    
    P1/2
    In this study, bortezomib and vorinostat were incorporated into an ALL chemotherapy backbone containing dexamethasone, mitoxantrone, and pegasparaginase during induction and reinduction chemotherapy cycles...Following induction intensification with cyclophosphamide, cytarabine, and mercaptopurine, 77% and 66% of all patients and KMT2Ar patients respectively were MRD negative at the time of count recovery...Although the study was not powered to evaluate outcomes, EFS and OS in KMT2Ar patients suggest a clinical signal worth pursuing given the low proportion of patients transplanted in first remission. The successor study, TINI 2 (NCT05848687), will build upon the bortezomib/vorinostat backbone by incorporating 2 cycles of blinatumomab and the menin inhibitor ziftomenib in combination with chemotherapy during reinduction.
  • ||||||||||  Zolinza (vorinostat) / Merck (MSD), ziftomenib (KO-539) / Kura Oncology, Blincyto (blinatumomab) / Astellas, Amgen
    Trial initiation date:  TINI 2: Total Therapy for Infants With Acute Lymphoblastic Leukemia II (clinicaltrials.gov) -  Sep 13, 2023   
    P1/2,  N=90, Not yet recruiting, 
    Collectively, these data suggest that MLL1 contributes to renal protection and functional recovery and promotes renal regeneration through a mechanism associated with activation of the EGFR signaling pathway. Initiation date: Jul 2023 --> Nov 2023
  • ||||||||||  Review, Journal:  Targeting the undruggable: menin inhibitors ante portas. (Pubmed Central) -  Jul 31, 2023   
    The clinical development of novel menin-MLL inhibitors is well in line with the currently ongoing paradigm shift towards targeted therapies seen in the AML treatment landscape. Moreover, the clinical assessment of combinations of these inhibitors with established therapy options in AML could be the fuel for an improved outcome of MLL/NPM1 patients.
  • ||||||||||  MI-503 / Kura Oncology
    Journal:  Clinically Defined Mutations in MEN1 Alter Its Tumor-suppressive Function Through Increased Menin Turnover. (Pubmed Central) -  Jul 30, 2023   
    We report that these mutations and variant promote tumor cell growth and gastrin expression by rendering menin protein unstable and prone to increased degradation. We demonstrate that the menin-MLL (mixed lineage leukemia) inhibitor MI-503 restores menin protein expression and function in vitro and in vivo, suggesting a potential novel therapeutic approach to target MEN1 GEP-NETs.
  • ||||||||||  Venclexta (venetoclax) / Roche, AbbVie, Walter and Eliza Hall Institute, ziftomenib (KO-539) / Kura Oncology
    KMT2A::ARHGEF12 RARE FUSION ASSOCIATED WITH A NOVEL GERMLINE DDX41 VARIANT IN ACUTE MYELOID LEUKEMIA () -  May 12, 2023 - Abstract #EHA2023EHA_2604;    
    We highlight both the importance of multiple methods, including RNA high throughput sequencing, to discover rare KMT2A rearrangements as well as systematic research of DDX41 mutation in myeloid neoplasm. Reporting unusual and rare genetic aberrations is important in order to improve knowledge of their prognosis and treatments modalities including new clinical trials.
  • ||||||||||  ziftomenib (KO-539) / Kura Oncology
    PRECLINICAL EVALUATION OF THE MENIN INHIBITOR ZIFTOMENIB IN PRIMARY AML SPECIMENS () -  May 12, 2023 - Abstract #EHA2023EHA_2540;    
    These findings suggest that ziftomenib-mediated targeting of AML cell populations, including LSCs, may be an effective strategy for preventing disease progression in patients who are refractory or relapse in response to initial ven/aza treatment. Combination of ziftomenib and venetoclax needs to be further studied but may also represent a viable strategy in the presence of known characteristics corresponding tovenetoclax resistance.
  • ||||||||||  MI-503 / Kura Oncology
    Epigenetic regulator Menin-MLL1 maintains cancer stem cells and promotes neuroblastoma growth (Section 35; Poster Board #5) -  Mar 14, 2023 - Abstract #AACR2023AACR_8002;    
    In our future efforts, we will develop concomitant therapeutic approaches by combining MI-503 with current chemotherapies to target both NB CSCs and bulk tumor cells. This will lead to the development of effective, targeted, and clinically tractable therapies for NB patients.
  • ||||||||||  revumenib (SNDX-5613) / Syndax Pharma, ziftomenib (KO-539) / Kura Oncology
    Characterization of acquired resistance mutations to menin inhibitors (Valencia BC - Convention Center) -  Mar 14, 2023 - Abstract #AACR2023AACR_5561;    
    P1, P1/2
    The Janssen chemotype shows a novel binding mode. Although it has 30-fold lower affinity for M327I, it shows little change in its bound position to M327I menin.Given the clinical validation of menin inhibition in AML, the design of next generation compounds that block MLL1 binding while avoiding acquired MEN1 mutations may be a strategy to overcome acquired resistance to first generation menin inhibitors.
  • ||||||||||  Journal:  Novel agents and regimens in acute myeloid leukemia: latest updates from 2022 ASH Annual Meeting. (Pubmed Central) -  Mar 9, 2023   
    Encouraging efficacy data were presented from first-in-human studies of two investigational menin inhibitors, SNDX-5613 and KO-539, in relapsed and refractory (R/R) acute myeloid leukemia (AML) with KMT2A rearrangement or mutant NPM1, with overall response rates (ORR) of 53% (32/60) and 40% (8/20), respectively. The addition of the novel drug pivekimab sunirine, a first-in-class antibody-drug conjugate targeting CD123, to azacitidine and venetoclax in R/R AML resulted in an ORR of 45% (41/91), which rose to 53% in those who were venetoclax na
  • ||||||||||  ziftomenib (KO-539) / Kura Oncology
    New trial:  Expanded Access to Ziftomenib (clinicaltrials.gov) -  Feb 22, 2023   
    P=N/A,  N=0, Available, 
  • ||||||||||  ziftomenib (KO-539) / Kura Oncology
    Enrollment change, Trial completion date, Trial primary completion date:  KOMET-001: First in Human Study of Ziftomenib in Relapsed or Refractory Acute Myeloid Leukemia (clinicaltrials.gov) -  Jan 26, 2023   
    P1/2,  N=199, Recruiting, 
    The addition of the novel drug pivekimab sunirine, a first-in-class antibody-drug conjugate targeting CD123, to azacitidine and venetoclax in R/R AML resulted in an ORR of 45% (41/91), which rose to 53% in those who were venetoclax na N=60 --> 199 | Trial completion date: Dec 2022 --> Sep 2025 | Trial primary completion date: Jun 2022 --> Sep 2024
  • ||||||||||  MI-503 / Kura Oncology
    Journal:  Epigenetic Regulation as a New Therapeutic Target for Middle Ear Cholesteatoma. (Pubmed Central) -  Jan 3, 2023   
    N=60 --> 199 | Trial completion date: Dec 2022 --> Sep 2025 | Trial primary completion date: Jun 2022 --> Sep 2024 These findings demonstrate an encouraging safety profile for the use of menin-MLL inhibitor for the conservative treatment of cholesteatoma.
  • ||||||||||  MI-503 / Kura Oncology
    Journal:  Inhibition of MLL1-menin interaction attenuates renal fibrosis in obstructive nephropathy. (Pubmed Central) -  Dec 18, 2022   
    Finally, MI-503 was effective in abrogating serum or TGFβ1-induced transformation of renal interstitial fibroblasts to myofibroblasts in vitro. Taken together, these results suggest that targeting disruption of the MLL1-menin interaction attenuates renal fibrosis through inhibition of partial EMT and renal fibroblast activation.