Kinase-impaired BTK mutations are susceptible to clinical-stage BTK and IKZF1/3 degrader NX-2127
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Increasing use of covalent and noncovalent inhibitors of Bruton’s tyrosine kinase (BTK) has elucidated a series of acquired drug-resistant BTK mutations in patients with B cell malignancies. Here we identify inhibitor resistance mutations in BTK with distinct enzymatic activities, including some that impair BTK enzymatic activity while imparting novel protein-protein interactions that sustain B cell receptor (BCR) signaling. Furthermore, we describe a clinical-stage BTK and IKZF1/3 degrader, NX-2127, that can bind and proteasomally degrade each mutant BTK proteoform, resulting in potent blockade of BCR signaling. Treatment of chronic lymphocytic leukemia with NX-2127 achieves >80% degradation of BTK in patients and demonstrates proof-of-concept therapeutic benefit. These data reveal an oncogenic scaffold function of mutant BTK that confers resistance across clinically approved BTK inhibitors but is overcome by BTK degradation in patients.
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Downstream signaling is preserved in CLL cells with kinase impaired BTK mutations through novel protein interactions between mutant BTK and alternative kinases, as was demonstrated with BTK L528W.
“Downstream signaling is preserved in CLL cells with kinase impaired BTK mutations through novel protein interactions between mutant BTK and alternative kinases, as was demonstrated with BTK L528W (41).”
From Resistance Mechanisms and Approach to Chronic Lymphocytic Leukemia after BTK Inhibitor Therapy (2025) · cites this paper as [41]
The section on novel BTK protein interactions reports that L528W mutant BTK interacts with HCK and ILK and that these kinases help sustain downstream BCR signaling. However, the interaction experiments described there used TMD8 cells, not CLL cells, so the claim’s CLL-specific wording goes beyond what those experiments demonstrate. (LLM, conf=0.86)
Experimental — accuracy not yet measuredIn a phase 1 first-in-human trial of NX-2127 in patients with CLL, more than 80% BTK degradation was achieved and clinical responses occurred in 79% of evaluable patients.
“Preliminary results of a phase 1, first-in-human clinical trial of NX-2127 in patients with CLL have demonstrated that >80% BTK degradation was achieved, and clinical responses were seen in 79% of evaluable patients (41, 90).”
From Resistance Mechanisms and Approach to Chronic Lymphocytic Leukemia after BTK Inhibitor Therapy (2025) · cites this paper as [41]
The Clinical benefit section (page not provided) describes a first-in-human phase 1 trial in patients with CLL and reports >90% BTK degradation in one patient. It also reports improvement in target-lesion measurements in 11 of 14 evaluable patients (79%), but does not establish that all 11 had clinical responses; it identifies a formal partial response in one patient. (LLM, conf=0.83)
Experimental — accuracy not yet measuredBTK mutations may be classified as kinase proficient (e.g., T474I/S and C481S) or kinase impaired (e.g., M437R, V416L, C481Y/R/F, and L528W).
“BTKmutations may be classified as kinase proficient (e.g., T474I/S and C481S) or kinase impaired (e.g., M437R, V416L, C481Y/R/F, and L528W) (41–43).”
From Resistance Mechanisms and Approach to Chronic Lymphocytic Leukemia after BTK Inhibitor Therapy (2025) · cites this paper as [41]
Several mutations in the BTK kinase domain such as L528W, M437R, and V416L demonstrate greatly reduced BTK enzymatic function.
“In addition, several mutations in the BTK kinase domain such as L528W, M437R, and V416Ldemonstrate greatly reduced BTK enzymatic function(41).”
From Resistance Mechanisms and Approach to Chronic Lymphocytic Leukemia after BTK Inhibitor Therapy (2025) · cites this paper as [41]
BTK degraders eliminate both the enzymatic activity and the scaffolding function of BTK, unlike BTK inhibitors.
“In contrast to BTKi, BTK degraders eliminate both the enzymatic activity and scaffolding function of BTK (41).”
From Resistance Mechanisms and Approach to Chronic Lymphocytic Leukemia after BTK Inhibitor Therapy (2025) · cites this paper as [41]
NX-2127 is an orally bioavailable small-molecule BTK degrader effective against both wild-type and mutant forms of BTK.
“NX-2127 is an orally bioavailable, small molecule BTK degrader that is effective against both WT and mutant forms of BTK (41).”
From Resistance Mechanisms and Approach to Chronic Lymphocytic Leukemia after BTK Inhibitor Therapy (2025) · cites this paper as [41]
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PI3K Inhibitors in Hematology: When One Door Closes…
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Breaking Bad Proteins—Discovery Approaches and the Road to Clinic for Degraders
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HSD3B1, prostate cancer mortality and modifiable outcomes
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Recent advances in PROTAC-based antiviral and antibacterial therapeutics
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Proteolysis‐Targeting Chimera (PROTAC): A Revolutionary Tool for Chemical Biology Research
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Chronic Lymphocytic Leukemia: Novel Therapeutic Targets Under Investigation
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A double-edged sword of neo-substrate degradation in PROTACs
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Pirtobrutinib in the treatment of chronic lymphocytic leukemia or small lymphocytic lymphoma
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PROTAC‐Based HDAC Degradation: A Paradigm Shift in Targeted Epigenetic Therapies
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Targeted protein degradation with small molecules for cancer immunotherapy
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IKZF2 Degradation: It′s Time to Take into Account it When Designing Cereblon‐Based PROTACs
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KinasePred: A Computational Tool for Small-Molecule Kinase Target Prediction
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Resistance Mechanisms and Approach to Chronic Lymphocytic Leukemia after BTK Inhibitor Therapy
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“BTK mutations may be classified as kinase proficient (e.g. t474i/S and c481S) or kinase impaired (e.g. M437R, v416l, c481Y/R/F, and l528w) [40–42].”
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The Development of Novel Therapies for Chronic Lymphocytic Leukaemia in the Era of Targeted Drugs
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Advances in Bruton tyrosine kinase (Btk) inhibition are steered by Bruton tyrosine kinase phylogeny
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Tandem‐Activatable PROTAC Prodrug for Tumor Biomarker‐Driven Near‐Infrared Opto‐Proteolysis
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Covalent and Non-Covalent BTK Inhibition in Chronic Lymphocytic Leukemia Treatment
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Self-citationResistance Mutations in CLL: Genetic Mechanisms Shaping the Future of Targeted Therapy
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Current and emerging treatment perspectives for adults with Waldenström macroglobulinemia
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Resistance to Bruton Tyrosine Kinase Inhibitors
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Bruton Tyrosine Kinase Degraders in B-Cell Malignancies
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Updates on the Biological Heterogeneity of Mantle Cell Lymphoma
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Self-citationManagement of Relapsed and/or Refractory Chronic Lymphocytic Leukemia
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Targeting of kinases to treat neurodegenerative diseases
Shomali, T., & Trempe, J.-F. (2026) · Pharmacological Reviews · doi:10.1016/j.pharmr.2026.100128 · Cited by 4 · see citing works
- Authors
- Montoya, S., Bourcier, J., Noviski, M., Lu, H., Thompson, M. C., Chirino, A., Jahn, J., Sondhi, A. K., Gajewski, S., Tan, Y. S. (., Yung, S., Urban, A., Wang, E., Han, C., Mi, X., Kim, W. J., Sievers, Q., Auger, P., Bousquet, H., Brathaban, N., Bravo, B., Gessner, M., Guiducci, C., Iuliano, J. N., Kane, T., Mukerji, R., Reddy, P. J., Powers, J., Sanchez Garcia de los Rios, M., Ye, J., Barrientos Risso, C., Tsai, D., Pardo, G., Notti, R. Q., Pardo, A., Affer, M., Nawaratne, V., Totiger, T. M., Pena-Velasquez, C., Rhodes, J. M., Zelenetz, A. D., Alencar, A., Roeker, L. E., Mehta, S., Garippa, R., Linley, A., Soni, R. K., Skånland, S. S., Brown, R. J., Mato, A. R., Hansen, G. M., Abdel-Wahab, O., & Taylor, J.
- Affiliations
- University of Miami (US)
- Memorial Sloan Kettering Cancer Center (US)
- Nurix (United States) (US)
- Oslo University Hospital (NO)
- The Jackson Laboratory for Genomic Medicine (US)
- Nurix Therapeutics, San Francisco, CA, USA.
- Sylvester Comprehensive Cancer Center, University of Miami Miller School of Medicine, Miami, FL, USA.
- Rockefeller University (US)
- Molecular Pharmacology Program, Sloan Kettering Institute, Memorial Sloan Kettering Cancer Center, New York, NY, USA.
- Northwell Health (US)
- University of Liverpool (GB)
- Herbert Irving Comprehensive Cancer Center (US)
- Corresponding author
- Montoya, Skye
- Bourcier, Jessie
- Noviski, Mark
- Lu, Hao
- Hansen, Gwenn M.
- Abdel-Wahab, Omar
- Taylor, Justin
- ORCID
- Montoya, Skye
- Bourcier, Jessie
- Noviski, Mark
- Lu, Hao
- Thompson, Meghan C.
- Chirino, Alexandra
- Jahn, Jacob
- Sondhi, Anya K.
- Gajewski, Stefan
- Tan, Ying Siow (May)
- Urban, Aleksandra
- Wang, Eric
- Han, Cuijuan
- Mi, Xiaoli
- Kim, Won Jun
- Sievers, Quinlan
- Auger, Paul
- Brathaban, Nivetha
- Guiducci, Cristiana
- Iuliano, James N.
- Kane, Tim
- Mukerji, Ratul
- Reddy, Panga Jaipal
- Ye, Jordan
- Barrientos Risso, Carla
- Tsai, Daniel
- Notti, Ryan Q.
- Affer, Maurizio
- Nawaratne, Vindhya
- Totiger, Tulasigeri M.
- Rhodes, Joanna M.
- Zelenetz, Andrew D.
- Alencar, Alvaro
- Roeker, Lindsey E.
- Mehta, Sanjoy
- Garippa, Ralph
- Linley, Adam
- Soni, Rajesh Kumar
- Skånland, Sigrid S.
- Brown, Robert J.
- Mato, Anthony R.
- Hansen, Gwenn M.
- Abdel-Wahab, Omar
- Taylor, Justin
- Venue
- Science
- Published
- 2024-02-02
- Volume
- 383
- Issue
- 6682
- Pages
- eadi5798-eadi5798
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- PMC
- PMC11103405
- OpenAlex
- W4391428485
- Cited by
- 175
- References
- 71
- Citations by year
- 2026: 56 · 2025: 74 · 2024: 45
- FWCI
- 49.54
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Science (publishedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- Digital Commons-TMC (Texas Medical Center) (submittedVersion)
- The Mouseion at the JAXlibrary (Jackson Laboratory) (submittedVersion)
- Funders
- Memorial Sloan-Kettering Cancer Center (P30-CA08748)
- Edward P. Evans Foundation (R01 HL128239)
- Philippe Foundation
- Cycle for Survival (P50 CA254838)
- Sylvester Comprehensive Cancer Center, University of Miami Health Systems
- Fondation de France
- Norges Forskningsråd (294916, 322898)
- National Institutes of Health (1s10od026941-01, CA08748, CA240139, KL2TR001865)
- Marie-Josée and Henry R. Kravis Center for Molecular Oncology
- National Heart, Lung, and Blood Institute (HL128239, R01HL128239)
- National Cancer Institute (CA254838-01, CA240139, P30-CA-08748, CA242020, K08CA230319, R01CA242020, F31CA275378, CA08748, R01CA251138, P30CA008748, P50CA254838, R35CA304457, P30CA240139)
- National Center for Advancing Translational Sciences (P30 CA08748)
- Topics
- Health Sciences › Medicine › Genetics › Chronic Lymphocytic Leukemia Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
- Health Sciences › Medicine › Pathology and Forensic Medicine › Lymphoma Diagnosis and Treatment
- Keywords
- Bruton's tyrosine kinase, BTK mutations, B cell receptor signaling, chronic lymphocytic leukemia, acquired drug resistance, proteasomal degradation, protein-protein interaction, BTK inhibitors
- MeSH terms
- Agammaglobulinaemia Tyrosine Kinase, Humans, Mutation, Phosphorylation, Transcription Factors, Signal Transduction, Leukemia, Lymphocytic, Chronic, B-Cell, Drug Resistance, Neoplasm, Protein Kinase Inhibitors, Ikaros Transcription Factor, Proteolysis
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