8VA6

Menin in complex with Ziftomenib (KO-539)

Summary for 8VA6

• Entry DOI: 10.2210/pdb8va6/pdb
• Descriptor: Menin, Ziftomenib, DI(HYDROXYETHYL)ETHER, ... (8 entities in total)
• Functional Keywords: protein binding
• Biological source: Homo sapiens (human); More
• Total number of polymer chains: 1
• Total formula weight: 56425.33

Authors

Clegg, B.D.,Linhares, B.M.,Cierpicki, T.,Grembecka, J. (deposition date: 2023-12-11, release date: 2024-11-20, Last modification date: 2025-06-04)

Primary citation

Wang, E.S.,Issa, G.C.,Erba, H.P.,Altman, J.K.,Montesinos, P.,DeBotton, S.,Walter, R.B.,Pettit, K.,Savona, M.R.,Shah, M.V.,Kremyanskaya, M.,Baer, M.R.,Foran, J.M.,Schiller, G.,Ades, L.,Heiblig, M.,Berthon, C.,Peterlin, P.,Rodriguez-Arboli, E.,Salamero, O.,Patnaik, M.M.,Papayannidis, C.,Grembecka, J.,Cierpicki, T.,Clegg, B.,Ray, J.,Linhares, B.M.,Nie, K.,Mitra, A.,Ahsan, J.M.,Tabachri, M.,Soifer, H.S.,Corum, D.,Leoni, M.,Dale, S.,Fathi, A.T.
Ziftomenib in relapsed or refractory acute myeloid leukaemia (KOMET-001): a multicentre, open-label, multi-cohort, phase 1 trial.
Lancet Oncol, 25:1310-1324, 2024

PubMed Abstract: Ziftomenib (KO-539) is an oral selective menin inhibitor with known preclinical activity in menin-dependent acute myeloid leukaemia models. The primary objective of this study was to determine the recommended phase 2 dose in patients with relapsed or refractory acute myeloid leukaemia based on safety, pharmacokinetics, pharmacodynamics, and preliminary activity.

PubMed: 39362248
DOI: 10.1016/S1470-2045(24)00386-3

Experimental method

X-RAY DIFFRACTION (1.57 Å)