Bleximenib

Bleximenib
Clinical data
Other names	JNJ-6617; JNJ-75276617
Legal status
Legal status	investigational;
Identifiers
	IUPAC name N-ethyl-5-fluoro-2-[[5-[2-[(3R)-6-[2-methoxyethyl(methyl)amino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide;
CAS Number	2654081-35-1;
PubChem CID	156498110;
IUPHAR/BPS	12866;
DrugBank	DB19328;
ChemSpider	129458099;
UNII	DCN5WEN78T;
KEGG	D13254;
ChEBI	CHEBI:759213;
ChEMBL	ChEMBL5314509;
Chemical and physical data
Formula	C32H50FN7O3
Molar mass	599.796 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CCN(C(C)C)C(=O)C1=C(C=CC(=C1)F)OC2=C(N=CN=N2)N3CCC4(C3)CN(C4)[C@H](CCCN(C)CCOC)C(C)C;
	InChI InChI=InChI=1S/C32H50FN7O3/c1-8-40(24(4)5)31(41)26-18-25(33)11-12-28(26)43-30-29(34-22-35-36-30)38-15-13-32(19-38)20-39(21-32)27(23(2)3)10-9-14-37(6)16-17-42-7/h11-12,18,22-24,27H,8-10,13-17,19-21H2,1-7H3/t27-/m1/s1; Key:PDUGAXSIWNMIBQ-HHHXNRCGSA-N;

Bleximenib is an investigational new drug that is being evaluated by Janssen Research & Development for the treatment of acute myeloid leukaemia (AML). It is a menin inhibitor preventing its interaction with KMT2A.^[1]^[2]^[3]

Pharmacology

Bleximenib is a selective inhibitor of menin preventing its interaction with the lysine methyltransferase KMT2A. The menin/KMT2A complex regulates gene expression in leukemia cells which keeps them in an immature state that is continually dividing.^[4]

Clinical trials

Bleximenib is in phase 3 clinical trials for AML. ^[5]

References

↑ "Bleximenib - Janssen Research & Development". AdisInsight. Springer Nature Switzerland AG.
↑ Peters DT, Hatfield J, Reese M, Zeidner JF (March 2026). "Menin Inhibitors: A New Era of Targeted Therapies in Acute Myeloid Leukemia". Current Treatment Options in Oncology. 27 (1). doi:10.1007/s11864-025-01378-6. PMID 41843240.
↑ Rockwell B, Konopleva M (June 2025). "Exploring new horizons in menin: it's bleximenib's turn". Haematologica. 110 (6): 1250–1251. doi:10.3324/haematol.2024.287142. PMC 12130784. PMID 40079087.
↑ Kwon MC, Thuring JW, Querolle O, Dai X, Verhulst T, Pande V, et al. (September 2024). "Preclinical efficacy of the potent, selective menin-KMT2A inhibitor JNJ-75276617 (bleximenib) in KMT2A- and NPM1-altered leukemias". Blood. 144 (11): 1206–1220. doi:10.1182/blood.2023022480. PMID 38905635.
↑ Clinical trial number NCT06852222 for "A Study of Bleximenib, Venetoclax and Azacitidine For Treatment of Participants With Newly Diagnosed Acute Myeloid Leukemia (AML)" at ClinicalTrials.gov

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[AdisInsight-1] "Bleximenib - Janssen Research & Development". AdisInsight. Springer Nature Switzerland AG.

[pmid41843240-2] Peters DT, Hatfield J, Reese M, Zeidner JF (March 2026). "Menin Inhibitors: A New Era of Targeted Therapies in Acute Myeloid Leukemia". Current Treatment Options in Oncology. 27 (1). doi:10.1007/s11864-025-01378-6. PMID 41843240.

[pmid40079087-3] Rockwell B, Konopleva M (June 2025). "Exploring new horizons in menin: it's bleximenib's turn". Haematologica. 110 (6): 1250–1251. doi:10.3324/haematol.2024.287142. PMC 12130784. PMID 40079087.

[pmid38905635-4] Kwon MC, Thuring JW, Querolle O, Dai X, Verhulst T, Pande V, et al. (September 2024). "Preclinical efficacy of the potent, selective menin-KMT2A inhibitor JNJ-75276617 (bleximenib) in KMT2A- and NPM1-altered leukemias". Blood. 144 (11): 1206–1220. doi:10.1182/blood.2023022480. PMID 38905635.

[5] Clinical trial number NCT06852222 for "A Study of Bleximenib, Venetoclax and Azacitidine For Treatment of Participants With Newly Diagnosed Acute Myeloid Leukemia (AML)" at ClinicalTrials.gov

[1]