A menin-KMT2A inhibitor to overcome resistance

doi:10.1182/blood.2024025760

Editorial

. 2024 Sep 12;144(11):1139-1140.

doi: 10.1182/blood.2024025760.

A menin-KMT2A inhibitor to overcome resistance

Caroline A Heckman¹

Affiliations

PMID: 39264614
PMCID: PMC11419777 (available on 2025-09-12)
DOI: 10.1182/blood.2024025760

Editorial

A menin-KMT2A inhibitor to overcome resistance

Caroline A Heckman. Blood. 2024.

. 2024 Sep 12;144(11):1139-1140.

doi: 10.1182/blood.2024025760.

Author

Caroline A Heckman¹

Affiliation

¹ University of Helsinki.

PMID: 39264614
PMCID: PMC11419777 (available on 2025-09-12)
DOI: 10.1182/blood.2024025760

No abstract available

PubMed Disclaimer

Conflict of interest statement

Conflict-of-interest disclosure: C.A.H. declares no competing financial interests.

Comment on

Preclinical efficacy of the potent, selective menin-KMT2A inhibitor JNJ-75276617 (bleximenib) in KMT2A- and NPM1-altered leukemias.
Kwon MC, Thuring JW, Querolle O, Dai X, Verhulst T, Pande V, Marien A, Goffin D, Wenge DV, Yue H, Cutler JA, Jin C, Perner F, Hogeling SM, Shaffer PL, Jacobs F, Vinken P, Cai W, Keersmaekers V, Eyassu F, Bhogal B, Verstraeten K, El Ashkar S, Perry JA, Jayaguru P, Barreyro L, Kuchnio A, Darville N, Krosky D, Urbanietz G, Verbist B, Edwards JP, Cowley GS, Kirkpatrick R, Steele R, Ferrante L, Guttke C, Daskalakis N, Pietsch EC, Wilson DM, Attar R, Elsayed Y, Fischer ES, Schuringa JJ, Armstrong SA, Packman K, Philippar U. Kwon MC, et al. Blood. 2024 Sep 12;144(11):1206-1220. doi: 10.1182/blood.2023022480. Blood. 2024. PMID: 38905635 Free PMC article.

Cited by

Menin Inhibitors: New Targeted Therapies for Specific Genetic Subtypes of Difficult-to-Treat Acute Leukemias.
Niscola P, Gianfelici V, Giovannini M, Piccioni D, Mazzone C, Fabritiis P. Niscola P, et al. Cancers (Basel). 2025 Jan 4;17(1):142. doi: 10.3390/cancers17010142. Cancers (Basel). 2025. PMID: 39796769 Free PMC article. Review.
Insights into KMT2A rearrangements in acute myeloid leukemia: from molecular characteristics to targeted therapies.
Zehtabcheh S, Soleimani Samarkhazan H, Asadi M, Zabihi M, Parkhideh S, Mohammadi MH. Zehtabcheh S, et al. Biomark Res. 2025 May 13;13(1):73. doi: 10.1186/s40364-025-00786-y. Biomark Res. 2025. PMID: 40361241 Free PMC article. Review.

References

1. Kwon MC, Thuring JW, Querolle O, et al. Preclinical efficacy of the potent, selective menin-KMT2A inhibitor JNJ-75276617 (bleximenib) in KMT2A- and NPM1-altered leukemias. Blood. 2024;144(11):1206–1220. - PubMed
1. Yokoyama A, Somervaille TC, Smith KS, Rozenblatt-Rosen O, Meyerson M, Cleary ML. The menin tumor suppressor protein is an essential oncogenic cofactor for MLL-associated leukemogenesis. Cell. 2005;123(2):207–218. - PubMed
1. Kühn MW, Song E, Feng Z, et al. Targeting chromatin regulators inhibits leukemogenic gene expression in NPM1 mutant leukemia. Cancer Discov. 2016;6(10):1166–1181. - PMC - PubMed
1. Dempke WCM, Desole M, Chiusolo P, Sica S, Schmidt-Hieber M. Targeting the undruggable: menin inhibitors ante portas. J Cancer Res Clin Oncol. 2023;149(11):9451–9459. - PMC - PubMed
1. Issa GC, Aldoss I, DiPersio J, et al. The menin inhibitor revumenib in KMT2A-rearranged or NPM1-mutant leukaemia. Nature. 2023;615(7954):920–924. - PMC - PubMed

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[1] Kwon MC, Thuring JW, Querolle O, et al. Preclinical efficacy of the potent, selective menin-KMT2A inhibitor JNJ-75276617 (bleximenib) in KMT2A- and NPM1-altered leukemias. Blood. 2024;144(11):1206–1220. - PubMed

[2] Kwon MC, Thuring JW, Querolle O, et al. Preclinical efficacy of the potent, selective menin-KMT2A inhibitor JNJ-75276617 (bleximenib) in KMT2A- and NPM1-altered leukemias. Blood. 2024;144(11):1206–1220. - PubMed

[3] Yokoyama A, Somervaille TC, Smith KS, Rozenblatt-Rosen O, Meyerson M, Cleary ML. The menin tumor suppressor protein is an essential oncogenic cofactor for MLL-associated leukemogenesis. Cell. 2005;123(2):207–218. - PubMed

[4] Yokoyama A, Somervaille TC, Smith KS, Rozenblatt-Rosen O, Meyerson M, Cleary ML. The menin tumor suppressor protein is an essential oncogenic cofactor for MLL-associated leukemogenesis. Cell. 2005;123(2):207–218. - PubMed

[5] Kühn MW, Song E, Feng Z, et al. Targeting chromatin regulators inhibits leukemogenic gene expression in NPM1 mutant leukemia. Cancer Discov. 2016;6(10):1166–1181. - PMC - PubMed

[6] Kühn MW, Song E, Feng Z, et al. Targeting chromatin regulators inhibits leukemogenic gene expression in NPM1 mutant leukemia. Cancer Discov. 2016;6(10):1166–1181. - PMC - PubMed

[7] Dempke WCM, Desole M, Chiusolo P, Sica S, Schmidt-Hieber M. Targeting the undruggable: menin inhibitors ante portas. J Cancer Res Clin Oncol. 2023;149(11):9451–9459. - PMC - PubMed

[8] Dempke WCM, Desole M, Chiusolo P, Sica S, Schmidt-Hieber M. Targeting the undruggable: menin inhibitors ante portas. J Cancer Res Clin Oncol. 2023;149(11):9451–9459. - PMC - PubMed

[9] Issa GC, Aldoss I, DiPersio J, et al. The menin inhibitor revumenib in KMT2A-rearranged or NPM1-mutant leukaemia. Nature. 2023;615(7954):920–924. - PMC - PubMed

[10] Issa GC, Aldoss I, DiPersio J, et al. The menin inhibitor revumenib in KMT2A-rearranged or NPM1-mutant leukaemia. Nature. 2023;615(7954):920–924. - PMC - PubMed

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A menin-KMT2A inhibitor to overcome resistance

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A menin-KMT2A inhibitor to overcome resistance

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