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nilotinib (Danziten)

✓ Approved

Azurity Pharmaceuticals, Inc. · ABL1 · 小分子

什么是 nilotinib？

nilotinib 是一种小分子，由Azurity Pharmaceuticals, Inc.研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名Danziten
公司Azurity Pharmaceuticals, Inc.
药物类别小分子
分子靶点ABL1, BCR, KIT, PDGFRA
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Azurity Pharmaceuticals, Inc.

作用机制

分子靶点

nilotinib 作用于 4 个分子靶点：

ABL1ABL proto-oncogene 1, non-receptor tyrosine kinase (c-ABL, bcr/abl)
BCRBCR activator of RhoGEF and GTPase (CML, ALL)
KITKIT proto-oncogene, receptor tyrosine kinase (MASTC, CD117)
PDGFRAplatelet derived growth factor receptor alpha (PDGFR-2, CD140A)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

nilotinib 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Chronic myeloid leukaemia✓ Approved

相关研究文献

PubMedValue in health regional issues2026-09-10

Cost-Effectiveness Analysis of Asciminib in Patients With Chronic Phase Chronic Myeloid Leukemia Previously Treated With 2 or More Tyrosine Kinase Inhibitors in Colombia.

Ceballos Mateo M, Abello Virginia V, Lasalvia Pieralessandro P, Jaramillo Paola P et al.

To assess the cost-effectiveness of asciminib in adult patients with chronic-phase chronic myeloid leukemia who have been treated with 2 or more tyrosine kinase inhibitors, from a third-party payer perspective in Colombia. A nonhomogeneous partitioned survival model was developed using ASCEMBL trial and matching-adjusted indirect comparisons. Outcomes included overall survival, progression-free survival, and safety. Overall survival was modeled using exponential functions based on 6-month major molecular response rates. Quality-adjusted life-years (QALYs) were estimated using phase-specific utilities. Direct medical costs were obtained from national public databases (2024-2025) and expressed in 2025 USD (USD 1 = COP 4053). A 30-year time horizon was applied. Base case compared asciminib with bosutinib and ponatinib. Scenario analyses included nilotinib and dasatinib because they are rarely used in third line in Colombia. Sensitivity analyses explored ponatinib dose deescalation, generic drug pricing, asciminib price thresholds, relative dose intensity, and alternative overall survival assumptions. Probabilistic sensitivity analyses were performed. Asciminib was dominant compared with bosutinib and ponatinib, yielding more QALYs (0.41 and 0.20) and lower costs (-USD 47 334 and -USD 88 554). Scenario analyses including nilotinib and dasatinib favored asciminib, with higher QALYs (0.32 and 0.25) and lower costs (-USD 43 785 and -USD 6400). Results remained robust across analyses, including ponatinib dose deescalation, generic pricing, relative dose intensity, and alternative overall survival assumptions. Asciminib was a dominant treatment option for patients with chronic-phase chronic myeloid leukemia who have been treated with 2 or more tyrosine kinase inhibitors, offering clinical and economic advantages over other pharmacological treatments.

PMID 42720643
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PubMedIndian journal of hematology & blood transfusion : an official journal of Indian Society of Hematology and Blood Transfusion2026-09-09

Validation of Eutos Long-Term Survival Score in Chronic Myeloid Leukemia Patients Treated with Second Generation Tyrosine-Kinase Inhibitor- Experience from A Low-Middle Income Country.

Zafar Sidra S, Shahani Waseem W, Nizamuddin Muhammad M, Zaidi Uzma U et al.

Chronic myeloid leukemia (CML) is a clonal disorder of myeloid lineage. Our study was done to compare the three risk groups and evaluate utility and applicability of the ELTS scoring system in predicting survival of CML in chronic phase(CP) on treatment with nilotinib in a resource limited setting. A cross sectional study was conducted at National Institute of Blood Diseases and Bone marrow transplantation, Karachi, Pakistan from January 2015 to December 2022. A total of 204 diagnosed CML patients were included. Risk stratification was done based on the Sokal, EUTOS and ELTS scores. A total of 204 patients were enrolled in the study. Out of total, 130 (64%) were males. The median age was 37(ranging 15-77 years). The median follow-up duration was 40 months and median spleen size was 5.6 (ranging, 1.6-14 cm). On the basis of ELTS score, 86 (42%) patients were stratified as low, intermediate 91 (45%), and 27 (13%) patients were high-risk group. Patients stratified as high-risk according to ELTS scoring had a substantial lower MMR accomplishment. Moreover, the 12 months MMR accomplishment rates were 50 (39%) in low, 55 (43%)(p = 0.03). ELTS and EUTOS scoring system was also able to anticipate the DMR accomplishment (p = < 0.001). Our study implied that the new ELTS score can be used to predict prognosis in CML patients in CP treated with upfront nilotinib specifically in terms of molecular response and must be incorporated at disease baseline to predict disease prognosis and choice of tyrosine kinase inhibitor (TKI).

PMID 42712768
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PubMedIndian journal of hematology & blood transfusion : an official journal of Indian Society of Hematology and Blood Transfusion2026-09-09

Efficacy and Safety of Ponatinib as a Second‑Line Treatment for Chronic‑Phase Chronic Myeloid Leukemia: Retrospective Study at Two Japanese Centers.

Ishii Yoshimi Y, Fujisawa Shin S, Fujimaki Katsumichi K, Miyazaki Takuya T et al.

The third-generation tyrosine kinase inhibitor (TKI) ponatinib has demonstrated efficacy in patients with chronic phase chronic myeloid leukemia (CML-CP). However, limited data were reported for the use of ponatinib as a second-line treatment in real world evidence. This observational, multicenter, retrospective study included patients aged ≥ 16 years with CML-CP who received ponatinib as second-line therapy between September 2016 and October 2023 at Yokohama City University Medical Center and Fujisawa City Hospital. The median age at the time of data collection was 53 (range, 20-79) years. The median duration of TKI treatment was 15 (range, 1-85) months. The TKIs administered as first-line treatment were as follows: bosutinib in eight patients (50%), dasatinib in six patients (38%), and nilotinib in two patients (13%). Reasons for switching to ponatinib included intolerance (in five patients, 31%) and resistance (in 11 patients, 69%). The median ponatinib exposure was 637 (range, 49-1384) days, with a median follow-up of 1,052 (range, 411-1,732) days. Among the patients, 13 (81%) achieved or maintained major molecular response. Five patients (31%) discontinued ponatinib. Ponatinib demonstrated high efficacy in treating CML-CP resistant or intolerant to second-generation TKIs.

PMID 42712751
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PubMedEJHaem2026-09-09

Prescription Behaviour and Drug Interactions of Acid Suppressants With Tyrosine Kinase Inhibitors in Patients With Leukaemia: Data From Germany.

Lapka Marek M, Khryakova Anna A, Nazmutdinova Anastasiia A, Charalambous Chrysostomos C et al.

Tyrosine kinase inhibitors (TKIs) are essential in treating chronic myeloid leukaemia (CML) and other malignancies. Their absorption, however, is highly pH-dependent, making them susceptible to interactions with acid-suppressing agents such as proton pump inhibitors (PPIs), histamine-2 receptor antagonists (H2RAs) and antacids. Despite clear warnings, real-world data show frequent co-administration, which may compromise therapeutic efficacy. This study combines two approaches-(1) a systematic review summarizing the impact of acid suppressants on TKI pharmacokinetics and clinical outcomes, and (2) an analysis of German prescription data from the Insight Health co-prescription database, focusing on TKIs primarily used for CML. Results indicate substantial co-prescription rates involving dasatinib, nilotinib, imatinib, bosutinib and ponatinib, with variations across years and agents. Pharmacokinetic evidence demonstrates that PPIs and H2RAs can significantly reduce systemic TKI exposure, with reported decreases of up to 96% in peak plasma concentration and 88% in overall exposure. These reductions have been associated with poorer clinical outcomes, including decreased survival. The findings highlight the need for improved prescriber awareness, adherence to guidelines and risk mitigation strategies such as therapeutic drug monitoring or alternative dosing. Collaborative efforts between clinicians and regulatory bodies are essential to minimize risks and optimize patient outcomes.

PMID 42713051
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PubMedBlood reviews2026-09-06

Reframing chronic myeloid leukemia outcomes beyond survival: a perspective of quality of life and patient-centered data.

Lipton Jeffrey H JH, Abruzzese Elisabetta E, Gale Robert Peter RP, Hillis Christopher C et al.

The introduction and refinement of tyrosine kinase inhibitors (TKIs) over the past 25 years have resulted in dramatic improvements in life expectancy in individuals with chronic myeloid leukemia (CML). There are now multiple effective and well-tolerated TKIs available, and because most patients will be receiving TKIs for their lifetime, quality-of-life (QoL) considerations are an increasing concern. Patients with CML receiving TKIs have worse QoL than the general population, but TKIs have a generally less negative impact on QoL factors than previously available treatments for CML. Commonly used TKIs (imatinib, nilotinib, dasatinib, bosutinib, ponatinib, asciminib, and olverembatinib) all have positive and negative impacts on QoL, each of which can be impacted by patient preference and priorities, as well as line of therapy. The inclusion of patient-reported QoL outcomes in clinical trials will be vital to helping physicians understand the patient experience of CML and thereby improve disease management.

PMID 42701040
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PubMedJournal of receptor and signal transduction research2026-09-04

Drug repurposing for TAK1 inhibition in inflammatory diseases and cancer: virtual screening identifies nilotinib and dabrafenib as potential candidates.

Alshehri Jaber A JA, Alfuhayr Turki T

TGF-beta-activated kinase 1 (TAK1) is a critical regulator of inflammatory and oncogenic signaling pathways and represents a promising therapeutic target for diseases ranging from chronic inflammation to cancer. However, existing therapies targeting downstream mediators often face limitations such as drug resistance and inconsistent efficacy. Here, we report on drug repurposing to discover FDA-approved compounds that can suppress TAK1 activity. Molecular docking of 3500 drugs from the DrugBank database was performed, followed by drug profiling, biological activity analysis, and 500-nanosecond molecular dynamics (MD) simulations via a multi-step computational protocol. The systematic screening identified a few hits where two drugs, nilotinib and dabrafenib, showed appreciable binding affinity to the ATP-binding site of TAK1 and showed appropriate drug profiles. Stable interaction analyses indicated consistent engagement of catalytic residues and structural motifs essential for ATP binding and subsequent TAK1 function. MD simulations further indicated stable TAK1-ligand complexes for both nilotinib and dabrafenib, with persistent hydrogen-bonding interactions and maintenance of protein compactness throughout the simulations. These findings support the repositioning of nilotinib and dabrafenib as potential TAK1-targeting compounds toward therapeutic development against inflammation-driven pathologies and cancer. Experimentally validating these insights at the level of cells, tissues, organs, and body systems is necessary to translate computational insights into practical use for therapeutic development.

PMID 42696479
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