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December 8, 2025BloodOpen Access

A first-in-class oral clinical candidate targeting MLLT1 and 3 degradation for the treatment of advanced AML and ALL including menin inhibitor resistant / refractory disease

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Authors

GAGloria Akosua AnsaGCGraham Craggs

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Overview

Novel MLLT-TPD shows potent anti-cancer activity and apoptosis in leukemia cells, suggesting a promising combination therapy.

Key Points

  • MLLT-TPD induces significant apoptosis and differentiation in acute leukemia cells, leading to tumor regression.
  • The compound demonstrates strong selectivity and degradation of MLLT1 and 3, enhancing transcription regulation.
  • Combination therapy with MLLT-TPD and agents like venetoclax shows synergistic anti-cancer activity across tested cell lines.
  • Mouse models indicate excellent oral bioavailability with minimal toxicity, marking a significant advancement in leukemia treatment.

Cite This Study

Ansa et al. (2025) studied this question.

synapsesocial.com/papers/69362f364fa91c937236d353https://doi.org/10.1182/blood-2025-754
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1MLLT1/3 targeted protein degradation as the best-in-class approach for targeting the super elongation complex (SEC) in acute leukemia, including menin inhibitor refractory disease2025
  2. 2Protein degradation of MYC/GSPT1 combined with menin inhibition overcomes resistance to menin inhibition in KMT2A-rearranged Acute Myeloid Leukemia2025 · 1 citations
  3. 3Synergistic targeting of KMT2A-rearranged AML with combined LSD1 and menin inhibitors2025
  4. 4Preclinical activity of investigational menin inhibitor DSP-5336 (Enzomenib)-based combinations against MLL1-rearranged (MLL-r) or mutant-NPM1 AML models2025 · 1 citations
  5. 5Investigating KAT2A protac therapy for targeting leukemic blast differentiation in acute myeloid leukaemia.2025