AUTHORS
Aaron D Goldberg, MD, PhD, Matthew L. Ulrickson, MD2, Suresh Kumar Balasubramanian, MD3, Ghayas C. Issa, MD4, Pau Montesinos, MD5, Eduardo Rodríguez-Arbolí, MD6, Olga Salamero7, Eric Tam, MD, MBA8, Kiran Naqvi9, Jacob Appelbaum, MD/PhD10, Kateryna Fedorov, MD11, Cristina Papayannidis, MD, PhD12, James K. McCloskey, MD13, Eunice Sue Wang, MD14, Francesco Lanza Sr, MD, PhD15, Tara L. Lin, MD16, Martha L. Arellano, MD17, Jessica K. Altman, MD18, Mohamad Khawandanah, MD19, Erin Jou, MD20, Jane Liesveld, MD21, Yair Levy, MD22, Teresa Bernal Del Castillo, MD, PhD23, Dane Van Domelen24, Tianle Chen, PhD25, Xiaoyan Yang26, Harris Soifer, PhD27, Ashley Dayoub, MS28, Marcie Riches, MD, MS29, Daniel Corum, PhD30, Mollie Leoni, MD31, Amer M. Zeidan, MD32
AFFILIATIONS
1 Memorial Sloan Kettering Cancer Center, New York, New York, United States
2 Banner MD Anderson Cancer Center, Gilbert, Arizona, United States
3 Karmanos Cancer Institute, Detroit, Michigan, United States
4 The University of Texas MD Anderson Cancer Center, Houston, Texas, United States
5 Hospital Universitari i Politècnic La Fe, Valencia, Spain
6 Hospital Universitario Virgen del Rocío, Instituto de Biomedicina de Sevilla (IBiS/CSIC), University of Seville, Seville, Spain
7 Hospital Universitari Vall d'Hebron and Institute of Oncology (VHIO), Universitat Autònoma de Barcelona, Barcelona, Spain
8 Norris Comprehensive Cancer Center, University of Southern California, Los Angeles, California, United States
9 Chao Family Comprehensive Cancer Center, University of California Irvine Health, Orange, California, United States
10 Fred Hutchinson Cancer Center, Seattle, Washington, United States
11 Vanderbilt University Medical Center, Nashville, Tennessee, United States
12 IRCCS, Azienda Ospedaliero Universitaria di Bologna, Istituto di Ematologia 'L e A Seràgnoli', Bologna, Italy
13 John Theurer Cancer Center at Hackensack University Medical Center, Hackensack, New Jersey, United States
14 Roswell Park Comprehensive Cancer Center, Buffalo, New York, United States
15 Hematology Unit, Ravenna Hospital, University of Bologna, Bologna, Italy
16 University of Kansas, Fairway, Kansas, United States
17 Winship Cancer Institute of Emory University, Atlanta, Georgia, United States
18 Feinberg School of Medicine, Northwestern University, Chicago, Illinois, United States
19 Stephenson Cancer Center, University of Oklahoma Health Sciences Center, Oklahoma City, Oklahoma, United States
20 Northwell Cancer Institute, Department of Medicine, Donald and Barbara Zucker School of Medicine at Hofstra/Northwell, Hempstead, NY, USA; 2, Hempstead, New York, United States
21 University of Rochester Medical Center, Rochester, New York, United States
22 Texas Oncology, Baylor Charles A. Sammons Cancer Center, Dallas, Texas, United States
23 Hospital Central de Asturias, ISPA, IUOPAs, Oviedo,, Oviedo, Spain
24 Kura Oncology, Inc., San Digeo, California, United States
25 Kura Oncology, Inc., San Diego, California, United States
26 Kura Oncology, Inc., San Diego, California, United States
27 Kura Oncology, Inc., San Diego, California, United States
28 Kura Oncology, Inc., San Diego, California, United States
29 Kura Oncology, Inc., San Diego, California, United States
30 Kura Oncology, Inc., San Diego, California, United States
31 Kura Oncology, Inc., San Diego, California, United States
32 Yale University and Yale Comprehensive Cancer Center, New Haven, Connecticut, United States
ABSTRACT
Introduction: NPM1 mutations drive leukemogenesis in ~30% of AML, and FLT3 mutations occur in ~50% of NPM1-mutated (NPM1-m) AML. Ziftomenib is a potent, selective, oral menin inhibitor approved as monotherapy for adults with relapsed/refractory (R/R) NPM1-m AML and has also shown encouraging clinical activity in combination. As FLT3 is downstream of the menin-MLL pathway, combining ziftomenib with a FLT3 inhibitor may enhance antitumor activity. KOMET-008 (NCT06001788) is an ongoing, open-label, phase 1a/b dose-escalation/expansion study evaluating ziftomenib in combination with standard-of-care therapies in R/R NPM1-m or KMT2A-r AML. Here we report the first results from phase 1a/b of KOMET-008 for ziftomenib plus the FLT3 inhibitor gilteritinib in patients with R/R NPM1-m/FLT3-m AML.
Methods: Adults (≥18y) with R/R NPM1 and FLT3 co-mutated AML received ziftomenib 100–600 mg once daily in combination with standard dose of gilteritinib per label. Primary endpoints were dose-limiting toxicities (DLTs) and adverse events (AEs). Secondary endpoints included complete remission with full/partial hematologic recovery (CR/CRh; ELN 2022) rate, composite CR (CRc) rate and duration of remission.
Results: As of June 16, 2026, 48 patients were treated across ziftomenib dose levels: 7 at 100 mg, 9 at 200 mg, 8 at 400 mg and 24 at 600 mg. Median age was 67y (range 43–83), 58% were female, 81% had ECOG PS 0–1; FLT3 mutations included 40 FLT3-ITD and 8 FLT3-TKD. Patients had received a median of 2 prior therapies (range 1–9); 29 (60%) had prior venetoclax and 30 (63%) had ≥1 prior FLT3 inhibitor (16 gilteritinib, 4 quizartinib, 15 midostaurin). Median follow-up was 4.6 months (range 0.3–17.8). Two DLTs were observed: differentiation syndrome (DS; Gr2) at 100 mg and increased ALT/AST/ALP (Gr3-4) at 400 mg; both patients resumed ziftomenib. Grade (Gr)≥3 TEAEs occurred in 46 patients (96%), most commonly febrile neutropenia (48%), thrombocytopenia (38%) and neutropenia (25%). Gr≥3 ziftomenib-related TEAEs occurred in 21 patients (44%), most commonly thrombocytopenia (15%) and neutropenia (13%). Gr3 DS occurred in 5 patients (10%) and Gr3 investigator-assessed QTc prolongation in 3 patients (6%; none ziftomenib-related); there were no Gr4/5 DS and QTc prolongation events and all resolved successfully.
Clinical activity was observed across all ziftomenib dose levels, particularly ≥200 mg. Among patients treated with ziftomenib ≥200 mg, overall response rate (ORR) was 68% (28/41), CRc was 41% (17/41) and CR/CRh was 34% (14/41). Activity was notable in patients treated after 1 prior therapy, with both CRc and CR/CRh rates of 50% each (9/18), compared with 35% (8/23) and 22% (5/23) respectively after ≥2 prior therapies, supporting further evaluation of this combination earlier in the R/R treatment course. Among patients with prior venetoclax, CRc and CR/CRh rates were 38% (10/26) and 31% (8/26), respectively. Among patients with prior FLT3 inhibitor, ORR was 67% (16/24), CRc was 33% (8/24) and CR/CRh was 25% (6/24), compared with 71% (12/17) ORR, 53% (9/17) CRc and 47% (8/17) CR/CRh in FLT3 inhibitor-naïve patients. Seven (15%) patients proceeded to on-study transplantation, of whom 3 subsequently received ziftomenib + gilteritinib maintenance. Median time to CRc was 8.4 weeks (range 3.7–25.1). Among CRc responders, median time to absolute neutrophil recovery ≥1.0 x 109/L was 26 days (IQR 16–72) and to platelet recovery ≥100 x 109/L was 56 days (IQR 39–85). Updated data across all dose levels, including measurable residual disease data and duration of remission, will be presented.
Conclusions: In the ongoing KOMET-008 study, ziftomenib combined with gilteritinib was well tolerated and showed encouraging clinical activity in R/R NPM1-m/FLT3-m AML. This combination had low rates of ziftomenib-related cytopenia; DS and QTc prolongation were manageable and resolved successfully. Clinical activity was observed across all ziftomenib dose levels, particularly ≥200 mg, with CRc and CR/CRh rates of 41% and 34%, respectively. Activity was notable in patients treated after 1 prior therapy, with CRc and CR/CRh rates of 50% each. The combination was also highly active in those with prior FLT3 inhibitor exposure, with 67% ORR and 25% CR/CRh rates. Together, these findings support continued dose optimization and further evaluation of ziftomenib plus gilteritinib, including potential use as first salvage therapy for patients with R/R NPM1-m/FLT3-m AML.
DISCLOSURES
Aaron D Goldberg, MD, PhD: DAVA Oncology - Honoraria; AbbVie, Aprea, Aptose, AROG, Celularity, Kura, Pfizer, Prelude, Remedy Plan - Research Funding; AbbVie, Astellas, BMS, Cardinal Health, Daiichi Sankyo, Geron, Ikena Oncology, Kura Oncology, Molecular Partners, Pfizer, Remedy Plan Therapeutics, Rigel, Systimmune, Syndax, Tanabe Pharma - Consultancy (Includes expert testimony)