Uses
Bleximenib (JNJ-75276617; Menin-MLL inhibitor 24) is a potent, selective and orally active menin-KMT2A protein-protein interaction inhibitor with IC50 values of 0.1, 0.045, ≤0.066 nM for human, mouse, dog, respectively. Bleximenib shows antiproliferative activity and induces apoptosis. Bleximenib has the potential for the research of Acute myeloid leukemia (AML)[1][2].
in vivo
Bleximenib (30, 50, 100 mg/kg; PO; daily for 5 weeks) shows antitumor activity[1].
| Animal Model: | 6- to 8-week-old immune-compromised mice (MOLM-14 AML)[1] |
| Dosage: | 30, 50, 100 mg/kg |
| Administration: | PO; daily for 5 weeks |
| Result: | Induced tumor regressions of 70%, 97%, and 99% at 30, 50, and 100 mg/kg, respectively. |
References
[1] Kwon MC, et al. Preclinical efficacy of the potent, selective menin-KMT2A inhibitor JNJ-75276617 (bleximenib) in KMT2A- and NPM1-altered leukemias. Blood. 2024 Sep 12;144(11):1206-1220. DOI:
10.1182/blood.2023022480[2] Hogeling SM, et al. Bleximenib, the novel menin-KMT2A inhibitor JNJ-75276617, impairs long-term proliferation and immune evasion in acute myeloid leukemia. Haematologica. 2024 Dec 19. DOI:
10.3324/haematol.2024.285616