预约演示
更新于：2025-11-01
Quizartinib Hydrochloride
奎扎替尼
更新于：2025-11-01
概要
基本信息
药物类型 小分子化药 |
别名 Quizartinib、AC-010220、AC-220 + [7] |
靶点 |
作用方式 抑制剂 |
作用机制 FLT3抑制剂(酪氨酸蛋白激酶受体FLT3抑制剂) |
非在研适应症 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (2019-06-18), |
最高研发阶段(中国)申请上市 |
特殊审评优先审评 (美国)、突破性疗法 (美国)、快速通道 (美国)、孤儿药 (美国)、特殊审批 (中国) |
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结构/序列
分子式C29H34Cl2N6O4S |
InChIKeyDHYPGRVMIOATAE-UHFFFAOYSA-N |
CAS号1132827-21-4 |
关联
47
项与 奎扎替尼 相关的临床试验NCT06824168
A Phase 2, Multicenter, Randomized, Open-label Trial to Evaluate Safety and Efficacy of Two Dose Levels of Quizartinib as Maintenance for Adult Patients With Newly Diagnosed FLT3-ITD (+) Acute Myeloid Leukemia in Complete Remission
NCT06769490
Phase 1 Dose Escalation and Expansion of Ziftomenib in Combination With Quizartinib in Acute Myeloid Leukemia
NCT06578247
A Phase 3, Double-Blind, Randomized, Placebo-Controlled Trial Of Quizartinib Administered in Combination With Induction and Consolidation Chemotherapy and Administered as Maintenance Therapy in Adult Patients With Newly Diagnosed FLT3-ITD Negative Acute Myeloid Leukemia
100 项与 奎扎替尼 相关的临床结果
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100 项与 奎扎替尼 相关的转化医学
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100 项与 奎扎替尼 相关的专利（医药）
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352
项与 奎扎替尼 相关的文献（医药）2026-09-01CURRENT MEDICINAL CHEMISTRY
An Innovative Telomere-associated Prognosis Model in AML:
Predicting Immune Infiltration and Treatment Responsiveness
Article
作者: Sun, Jian ; Song, Binyang ; Lu, Xiao ; Mu, Lijun ; Tang, Bo ; Lou, Jinzhan
Aims::
To build an innovative telomere-associated scoring model to predict
prognosis and treatment responsiveness in acute myeloid leukemia (AML).
Background::
AML is a highly heterogeneous malignant hematologic disorder with a
poor prognosis. While telomere maintenance is frequently observed in tumors, investigations
into telomere-related genes (TRGs) in AML remain limited.
Objectives::
This study aimed to identify prognostic TRGs using the least absolute shrinkage
and selection operator (LASSO) Cox regression and multivariate Cox regression,
evaluate their predictive value, explore the association between TRG scores and immune
cell infiltration, and assess the sensitivity of high-scoring AML patients to chemotherapeutic
agents.
Method::
Univariate Cox regression analysis was conducted on the TCGA cohort to identify
prognostic TRGs and to develop the TRG scoring model using LASSO-Cox and
multivariate Cox regression. Validation was performed on the GSE37642 cohort. Immune
cell infiltration patterns were assessed through computational analysis, and the sensitivity
to chemotherapeutic agents was evaluated.
Results::
Thirteen prognostic TRGs were identified, and a seven-TRG scoring model (including
NOP10, OBFC1, PINX1, RPA2, SMG5, MAPKAPK5, and SMN1) was developed.
Higher TRG scores were associated with a poorer prognosis, as confirmed in the
GSE37642 cohort, and remained an independent prognostic factor even after adjusting
for other clinical characteristics. The high-score group was characterized by elevated infiltration
of B cells, T helper cells, natural killer cells, tumor-infiltrating lymphocytes,
regulatory T (Treg) cells, M2 macrophages, neutrophils, and monocytes, along with reduced
infiltration of gamma delta T cells, CD4- T cells, and resting mast cells. Moreover,
high infiltration of M2 macrophages and Tregs was associated with poor overall
survival compared to low infiltration. Notably, high-risk AML patients were resistant to
Erlotinib, Parthenolide, and Nutlin-3a, but sensitive to AC220, Midostaurin, and Tipifarnib.
Additionally, using RT-qPCR, we observed significantly higher expression of
two model genes, OBFC1 and SMN1, in AML tissues compared to control tissues.
Conclusion::
This innovative TRG scoring model demonstrates considerable predictive
value for AML patient prognosis, offering valuable insights for optimizing treatment
strategies and personalized medicine approaches. The identified TRGs and associated
scoring models could aid in risk stratification and guide tailored therapeutic interventions
in AML patients.
2026-01-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Rational design of next-generation FLT3 inhibitors in acute myeloid leukemia: From laboratory to clinics
Review
作者: Gao, Shan ; Wang, Xueting ; Zhao, Xiang ; Xiao, Zhennan
Activating mutations of FMS-like tyrosine kinase-3 (FLT3) are among the most common genetic alterations in acute myeloid leukemia (AML), affecting approximately 30 % of patients and leading to a poor prognosis. The development of FLT3-targeted inhibitors has achieved significant progress. First-generation multi-kinase inhibitors like midostaurin and second-generation agents such as gilteritinib and quizartinib have shown success. However, drug resistance, often due to D835Y and F691L gatekeeper mutations, remains a major challenge. In response, a new generation of FLT3 inhibitors (FLT3i) have been designed to simultaneously target both FLT3 internal tandem duplication (ITD) and tyrosine kinase domain (TKD) mutations. This review examines the mechanisms of FLT3 in the regulation of AML and examines preclinical research on novel FLT3i over the past five years. It discusses how these agents, including small-molecule like STI-8591, compounds 36 and 80 and novel therapeutic strategies such as CLN-049, and SENTI-202, are designed to combat resistance. The goal is to provide a medicinal chemistry perspective to provide insights for the design of novel small-molecule FLT3i.
2025-11-01EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY
Validation of pharmacokinetic model for quizartinib quantified by UPLC-MS/MS in patients with FLT3-ITD negative newly diagnosed acute myeloid leukemia
Article
作者: Labrador, Jorge ; Boluda, Blanca ; Megías-Vericat, Juan Eduardo ; Gil, Jose Vicente ; Lopez-Nogueroles, Marina ; Poveda-Andrés, Jose Luis ; Rodenas-Rovira, Mario ; Martínez-Cuadrón, David ; Rodriguez-Veiga, Rebeca ; Iniesta-Navalón, Carles ; Cano-Ferri, Isabel ; Gil-Candel, Mayte ; Lloret-Madrid, Pilar ; Barragán, Eva ; Chovi-Trull, Maria ; Navarro-Vicente, Irene ; Solana-Altabella, Antonio ; Acuña-Cruz, Evelyn ; Torres-Miñana, Laura ; Montesinos, Pau ; Peris-Ribera, José Esteban
Abstract:
Purpose:
Quizartinib pharmacokinetics in FLT3-ITD negative acute myeloid leukemia (AML) remain largely unexplored. This study aims to validate a population pharmacokinetics model (popPK) for quizartinib in plasma samples of FLT3-ITD negative AML patients. To do so, an ultra-performance liquid chromatography coupled with tandem mass spectrometry (UPLC-MS/MS) method has been developed and validated for the quantification of quizartinib.
Methods:
Plasma samples were collected from FLT3-ITD negative newly diagnosed AML patients undergoing quizartinib therapy at induction in the QUIWI phase II clinical trial [NCT04107727, PETHEMA group] between March 2020 and February 2022. The UPLC-MS/MS method was developed and validated. A previously described popPK model was validated using external validation techniques and implemented using the software NONMEM v7.5.
Results:
The developed UPLC-MS/MS method demonstrated high accuracy and precision with a linear range of 6 to 200 ng/mL, with relative standard deviation between 3–11 and accuracy of 88–97% from nominal values. The external validation of the quizartinib popPK model showed minimal bias at the population level (MdPE: -9.86%; ME: 0.50 ng/mL, p = 0.964), but moderate imprecision (MdAPE: 32.28%) and suboptimal accuracy (F20: 24.5%; F30: 43.4%). Individual predictions improved performance, with negligible bias (MdPE: -0.50%), acceptable precision (MdAPE: 11.27%), and F20 (64.2%) and F30 (77.4%) exceeding predefined thresholds. Visual predictive checks confirmed adequate prediction of median concentrations, though some deviations occurred at extremes.
Conclusion:
This study presents a replicable UPLC-MS/MS method for the determination of quizartinib in plasma. The validated popPK model can be used to optimize dosing strategies in future clinical studies.
100 项与 奎扎替尼 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 肿瘤 | 加拿大 | 2025-05-01 | |
| 急性髓性白血病 | 英国 | 2024-03-12 | |
| 伴有 FLT3/ITD 突变的急性髓系白血病 | 日本 | 2019-06-18 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| FLT3阳性急性髓性白血病 | 临床3期 | 美国 | 2014-05-01 | |
| FLT3阳性急性髓性白血病 | 临床3期 | 澳大利亚 | 2014-05-01 | |
| FLT3阳性急性髓性白血病 | 临床3期 | 比利时 | 2014-05-01 | |
| FLT3阳性急性髓性白血病 | 临床3期 | 加拿大 | 2014-05-01 | |
| FLT3阳性急性髓性白血病 | 临床3期 | 克罗地亚 | 2014-05-01 | |
| FLT3阳性急性髓性白血病 | 临床3期 | 捷克 | 2014-05-01 | |
| FLT3阳性急性髓性白血病 | 临床3期 | 法国 | 2014-05-01 | |
| FLT3阳性急性髓性白血病 | 临床3期 | 德国 | 2014-05-01 | |
| FLT3阳性急性髓性白血病 | 临床3期 | 中国香港 | 2014-05-01 | |
| FLT3阳性急性髓性白血病 | 临床3期 | 匈牙利 | 2014-05-01 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 273 | 積簾鑰觸鬱膚鬱餘餘範(廠窪鑰憲網遞遞衊簾壓) = 簾餘艱淵餘憲糧簾繭淵 襯醖憲鑰顧範醖衊壓選 (選獵廠襯衊窪餘繭鹽餘 ) 更多 | 积极 | 2025-10-13 | |||
Placebo | 積簾鑰觸鬱膚鬱餘餘範(廠窪鑰憲網遞遞衊簾壓) = 構膚鹹齋艱襯製壓齋齋 襯醖憲鑰顧範醖衊壓選 (選獵廠襯衊窪餘繭鹽餘 ) 更多 | ||||||
临床3期 | 518 | 齋築夢齋願網膚艱衊衊(艱願窪繭壓衊簾醖網簾) = 繭憲憲鏇衊廠遞窪憲積 蓋廠鑰鏇齋願範範廠憲 (餘繭築餘鹹製顧壓選鏇 ) | 积极 | 2025-05-14 | |||
Placebo | 齋築夢齋願網膚艱衊衊(艱願窪繭壓衊簾醖網簾) = 淵衊積構膚網衊築襯積 蓋廠鑰鏇齋願範範廠憲 (餘繭築餘鹹製顧壓選鏇 ) | ||||||
临床3期 | 518 | 夢遞襯壓窪餘艱鹹網夢(顧鬱觸醖鑰襯廠醖範衊) = 製夢襯膚構鑰壓衊選構 窪壓繭壓糧艱衊膚製膚 (壓網鑰顧鑰鑰襯鑰壓製 ) 更多 | 积极 | 2024-12-09 | |||
Placebo | 夢遞襯壓窪餘艱鹹網夢(顧鬱觸醖鑰襯廠醖範衊) = 鬱築鹽顧積遞遞壓艱願 窪壓繭壓糧艱衊膚製膚 (壓網鑰顧鑰鑰襯鑰壓製 ) 更多 | ||||||
N/A | - | 糧願遞淵廠糧膚艱範網(窪壓衊醖製鹽餘製壓鬱) = In the R/R cohort, grade ≥3 non-hematologic toxicities regardless of attribution, in >10% of pts, included pneumonia (73%), neutropenic fever (53%), sepsis (18%), other infections involving the skin (18%)bacteremia (15%), and gastrointestinal tract (13%), with 8% experiencing grade 3 QTcF prolongations. Grade ≥3 non-hematologic toxicities was less common in the frontline cohort, with pneumonia (40%), neutropenic fever (50%), sepsis (10%), bacteremia (20%), and no grade 3 QTcF prolongations observed. 網糧簾壓繭顧醖窪積觸 (選艱顧顧築齋構構簾壓 ) | - | 2024-12-09 | |||
N/A | - | 顧遞壓範廠製範獵壓願(壓膚淵蓋糧衊簾鏇齋製) = 獵選醖網遞鑰膚齋窪憲 願範鬱膚獵憲遞窪構繭 (膚廠醖淵餘範鹹蓋繭構 ) 更多 | - | 2024-12-08 | |||
Placebo | 顧遞壓範廠製範獵壓願(壓膚淵蓋糧衊簾鏇齋製) = 選憲壓範膚網齋窪醖鏇 願範鬱膚獵憲遞窪構繭 (膚廠醖淵餘範鹹蓋繭構 ) 更多 | ||||||
临床2期 | 273 | 憲鏇願簾願鏇願糧鏇廠(蓋醖網鹹鬱願網選繭積) = 遞願網廠願網鬱夢憲鹹 簾鹹選鬱襯製網醖範選 (願網壓範廠襯網築蓋繭 ) 更多 | 积极 | 2024-12-07 | |||
Placebo | 憲鏇願簾願鏇願糧鏇廠(蓋醖網鹹鬱願網選繭積) = 製糧鹽蓋齋構願廠艱簾 簾鹹選鬱襯製網醖範選 (願網壓範廠襯網築蓋繭 ) 更多 | ||||||
临床2期 | 急性髓性白血病 FLT3-ITD突变 | 40 | 鏇積膚鹹鑰齋構繭壓憲(膚醖範築廠齋淵醖獵範) = 淵構壓願齋顧鹽選願鏇 膚網醖衊艱獵鬱憲餘構 (壓襯繭壓鏇餘範衊淵鬱 ) 更多 | 积极 | 2024-12-07 | ||
临床3期 | FLT3-ITD+ | 539 | 構襯醖獵壓顧構艱願顧(製製蓋選壓網糧積製觸) = 襯網願鑰鑰顧鬱憲網選 願膚糧顧醖膚淵顧衊積 (鏇顧願鬱衊窪範醖顧築 ) | 积极 | 2024-09-04 | ||
Placebo | 構襯醖獵壓顧構艱願顧(製製蓋選壓網糧積製觸) = 艱鏇製顧廠憲網襯鬱繭 願膚糧顧醖膚淵顧衊積 (鏇顧願鬱衊窪範醖顧築 ) | ||||||
临床3期 | 急性髓性白血病 FLT3-ITD+ | 539 | 淵醖憲淵獵窪衊製憲製(範蓋夢觸築簾廠鑰廠蓋) = Primary EFS analysis (42d from last induction cycle used to define induction treatment failure [ITF]) did not differ between treatment arms by age 鬱憲簾廠鏇簾廠醖膚壓 (築鑰鹽鏇齋觸鹹襯遞築 ) 更多 | 积极 | 2024-09-04 | ||
Placebo | |||||||
临床1期 | 12 | 廠繭廠醖窪窪願觸網醖(構鑰選窪廠憲願淵觸廠) = thrombocytopenia (n=5, 42 %), anemia (n=4, 33 %), lung infection (n=2, 17 %), skin infection (n=2, 17 %), hyponatremia (n=2, 17 %) and sepsis (n=2, 17 %). 糧顧鹹繭構夢網選憲醖 (遞鬱鏇範願遞衊蓋憲繭 ) 更多 | 积极 | 2024-07-01 |
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