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更新于：2026-02-03
Talazoparib Tosylate
甲苯磺酸他拉唑帕利
更新于：2026-02-03
概要
基本信息
药物类型 小分子化药 |
别名 BMN 673、Talazoparib、talazoparib + [15] |
作用方式 抑制剂 |
作用机制 PARP1抑制剂(聚腺苷二磷酸核糖聚合酶1抑制剂)、PARP2抑制剂(聚腺苷二磷酸核糖聚合酶2抑制剂) |
在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (2018-10-16), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (美国) |
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结构/序列
分子式C26H22F2N6O4S |
InChIKeyQUQKKHBYEFLEHK-QNBGGDODSA-N |
CAS号1373431-65-2 |
关联
119
项与 甲苯磺酸他拉唑帕利 相关的临床试验NCT04982848
A Prospective, Single-arm, Open-label, Non-interventional, Multi-centre, Post Marketing Surveillance (PMS) Study of Talzenna(Registered)
NCT06844383
A Randomized Open-label Phase 2 Study of TALazoparib With or Without ENzaluTamide in Patients With Metastatic Castration-Resistant Prostate Cancer and HRR Mutations After Progression on Abiraterone Acetate
NCT05873192
Presurgical Phase II Study of Talazoparib in Combination With Enzalutamide in de Novo Metastatic to Lymph Nodes Prostate Cancer
100 项与 甲苯磺酸他拉唑帕利 相关的临床结果
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100 项与 甲苯磺酸他拉唑帕利 相关的转化医学
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100 项与 甲苯磺酸他拉唑帕利 相关的专利（医药）
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798
项与 甲苯磺酸他拉唑帕利 相关的文献（医药）2026-01-01Genes & Diseases
Targeting fatty acid synthase to overcome PARP inhibitor resistance and to create an artificial synthetic lethality for triple-negative breast cancer
Article
作者: Zhang, Jian-Ting ; Liu, Jing-Yuan ; Josephraj, Sophia ; Cui, Qingbin ; Wang, Chao J ; Dong, Zizheng
Despite advances in cancer treatment with targeted therapies and immunotherapies, triple-negative breast cancer (TNBC) has not significantly benefited from these developments. Although poly (ADP-ribose) polymerase (PARP) inhibitors (PARPi) are approved for breast cancer, their clinical use is largely limited to the small subset of HER2-negative patients with germline BRCA1/2 mutations, and resistance is frequently observed. Previously, we demonstrated that proton pump inhibitors (PPIs), including lansoprazole and its metabolite, 5-hydroxy lansoprazole sulfide (5HLS), reduce PARP1 expression by inhibiting fatty acid synthase (FASN), a key enzyme in de-novo lipid synthesis. We also found that PPIs synergize with DNA-damaging agents by regulating PARP1 expression and impairing non-homologous end joining (NHEJ) repair of DNA damage. These findings led to the hypothesis that PPIs synergize with PARPi independently of BRCA mutation, potentially expanding the utility of PARPi to a broader TNBC population. In this study, we show that FASN contributes to PARPi resistance, and that lansoprazole and 5HLS strongly synergize with olaparib and talazoparib in both BRCA1-mutant and wild-type TNBC cells. This synergy occurs through FASN inhibition and subsequent impairment of NHEJ repair of double-strand breaks induced by PARPi trapping. 5HLS also facilitates PARPi-induced PARP1 trapping and inhibits BRCA1 expression by inhibiting FASN, contributing to the synergy with PARPi in both BRCA1 wild-type and mutant TNBC cells. Together, these findings suggest that inhibiting FASN with PPIs creates an artificial synthetic lethality, providing a rationale for combining PPIs with PARPi to expand their utility to TNBC patients without germline BRCA1 mutations and to overcome PARPi resistance.
2026-01-01CURRENT CANCER DRUG TARGETS
Clinical Application of PARP1 Inhibitors and Challenges in Cancer Therapy
Article
作者: Cui, Xuehai ; Huang, Xinyu ; Chen, Yuekang ; Li, Enmin ; Nie, Mingcheng ; Cheng, Yinwei ; Lin, Wan ; Luo, Yunlin ; Xu, Liyan
Among the Poly(ADP-ribose) Polymerase (PARP) family in mammals, PARP1 is
the first identified and well-studied member that plays a critical role in DNA damage repair
and has been proven to be an effective target for cancer therapy. Here, we have reviewed not
only the role of PARP1 in different DNA damage repair pathways, but also the working mechanisms
of several PARP inhibitors (PARPi), inhibiting Poly-ADP-ribosylation (PARylation)
processing and PAR chains production to trap PARP1 on impaired DNA and inducing Transcription-
replication Conflicts (TRCs) by inhibiting the PARP1 activity. This review has systematically
summarized the latest clinical application of six authorized PARPi, including
olaparib, rucaparib, niraparib, talazoparib, fuzuloparib and pamiparib, in monotherapy and
combination therapies with chemotherapy, radiotherapy, and immunotherapy, in different
kinds of cancer. Furthermore, probable challenges in PARPi application and drug resistance
mechanisms have also been discussed. Despite these challenges, further development of new
PARP1 inhibitors appears promising as a valuable approach to cancer treatment.
2026-01-01Therapeutic Advances in Medical Oncology
Efficacy and safety of PARP inhibitors in metastatic breast cancer patients with homologous recombination repair pathway gene mutations: a retrospective multicenter real-world study
Article
作者: Zhang, Jintao ; Zhang, Pin ; Xu, Binghe ; Wang, Jiani ; Fan, Ying ; Luo, Yang ; Peng, Xuenan ; Mo, Hongnan ; Sun, Xiaoying ; Lan, Bo ; Ma, Fei ; Wang, Jiayu ; Chen, Shanshan ; Song, Ruixia ; Li, Qiao
Background::
The efficacy and safety of poly (ADP-ribose) polymerase inhibitors (PARPis) in the Chinese real-world setting have not been well characterized.
Design::
This is a retrospective analysis of PARPis efficacy in metastatic breast cancer (MBC) patients with homologous recombination repair (HRR) gene pathogenic variants (PVs).
Objectives::
We aimed to evaluate the efficacy and toxicities of PARPis in real-world MBC patients.
Methods::
Patients who received PARPi for MBC at the National Cancer Center and two other centers between January 1, 2019, and December 31, 2024, were consecutively included. The primary endpoint was progression-free survival (PFS). Univariable and multivariable Cox proportional hazard models were used to evaluate the predictive impact of clinicopathologic characteristics on PFS.
Results::
In total, 62 MBC patients treated with olaparib (
N
= 55), talazoparib (
N
= 4), pamiparib (
N
= 2), and fluzoparib (
N
= 1) were enrolled. The median PFS (mPFS) in all patients was 6.0 months (95% confidence interval: 4.1–7.9). mPFS in the germline
BRCA1
(g
BRCA1; N
= 19), g
BRCA2
(
N
= 30), g
BRCA
(
N
= 4), somatic
BRCA2
(s
BRCA2; N
= 1), g
PALB2
(
N
= 4), and other HRR gene (
N
= 4) PVs carriers were 3.7, 8.0, 2.8, 2.7, 5.3, and 7.1 months, respectively (
p
= 0.334). In multivariate analysis, ⩽40 years old (hazard ratio (HR): 2.281,
p
= 0.008), third-line or later therapy (HR: 2.429,
p
= 0.019), and prior platinum-based treatment (HR: 2.172,
p
= 0.014) were independently associated with shorter PFS. The incidence of adverse events (AEs) of all grades was 62.5% (35/56). The most common AEs in all grades were anemia (30.4%), nausea (21.4%), and leukopenia (17.9%). Hematologic toxicity was the most common grade ⩾3 AEs.
Conclusion::
PARPis showed promising PFS and tolerable toxicity in the real-world treatment of Chinese MBC patients with HRR-related gene mutations.
100 项与 甲苯磺酸他拉唑帕利 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 |
|---|---|---|---|
| BRCA突变去势抵抗性前列腺癌 | 日本 | 2024-01-18 | |
| 转移性去势抵抗性前列腺癌 | 欧盟 | 2024-01-08 | |
| 转移性去势抵抗性前列腺癌 | 冰岛 | 2024-01-08 | |
| 转移性去势抵抗性前列腺癌 | 列支敦士登 | 2024-01-08 | |
| 转移性去势抵抗性前列腺癌 | 挪威 | 2024-01-08 | |
| 乳腺癌 | 韩国 | 2020-07-30 | |
| HRR 基因突变去势抵抗性前列腺癌 | 澳大利亚 | 2019-11-18 | |
| 转移性乳腺癌 | 加拿大 | 2019-09-06 | |
| HR阳性乳腺癌 | 欧盟 | 2019-06-20 | |
| HR阳性乳腺癌 | 冰岛 | 2019-06-20 | |
| HR阳性乳腺癌 | 列支敦士登 | 2019-06-20 | |
| HR阳性乳腺癌 | 挪威 | 2019-06-20 | |
| gBRCA突变/HER2阴性乳腺癌 | 美国 | 2018-10-16 |
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 |
|---|---|---|---|---|
| 去势抵抗性前列腺癌 | 申请上市 | 美国 | 2023-02-17 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 美国 | 2021-05-12 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 中国 | 2021-05-12 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 日本 | 2021-05-12 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 阿根廷 | 2021-05-12 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 澳大利亚 | 2021-05-12 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 比利时 | 2021-05-12 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 保加利亚 | 2021-05-12 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 加拿大 | 2021-05-12 | |
| 转移性去势敏感性前列腺癌 | 临床3期 | 捷克 | 2021-05-12 |
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临床结果
临床结果
适应症
分期
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查看全部结果
临床2期 | 115 | (Expansion Cohort A - Combination Treatment in Post-TROP2-ADC Patients) | 鹹醖淵鹽衊願壓範襯鬱 = 顧壓願衊鬱艱壓築憲繭 願蓋構顧鬱觸簾積簾衊 (鏇窪廠膚網膚遞範蓋糧, 淵範壓醖廠鹹繭選積膚 ~ 窪蓋廠鹽鑰鬱糧糧醖鹽) 更多 | - | 2025-10-07 | ||
(Expansion Cohort C - Combination Treatment in TROP2-ADC-naïve Patients) | 製憲築襯餘築選鑰衊醖 = 糧構膚襯範鹹廠願衊衊 鹽獵網構鑰遞遞襯積範 (鑰鹽蓋積鏇淵鑰願糧網, 糧齋淵鏇餘顧網選鏇簾 ~ 積憲鹹鏇廠遞壓遞鹽蓋) 更多 | ||||||
临床1/2期 | 23 | 願淵醖繭鑰餘觸願積鏇(簾願糧網襯糧襯鬱鑰顧) = 艱衊網齋窪窪獵網艱觸 選淵鹹繭選簾鬱廠鹽鬱 (築蓋製艱淵餘鑰鏇遞網, 3.5 ~ 8.4) 更多 | 不佳 | 2025-08-01 | |||
临床1/2期 | - | 簾觸願夢築艱簾襯襯艱(醖窪構鏇艱蓋淵構鹽顧) = 鑰構選築衊網窪糧膚鬱 選壓鏇鑰鏇齋鹽淵餘淵 (願餘鏇蓋繭襯齋網襯簾 ) 更多 | 不佳 | 2025-06-05 | |||
临床2期 | 52 | (Arm 1c: ctDNA Positive Genomically Directed - PI3K Pathway) | 鏇鏇衊顧餘選壓衊觸壓 = 衊齋積繭製構願醖繭鹹 鹽遞衊壓選鹽鏇構鑰獵 (鏇獵鑰製觸願衊選鏇襯, 構遞糧鑰淵窪齋餘網範 ~ 願構壓夢憲餘膚齋廠廠) 更多 | - | 2025-05-31 | ||
(Arm 2: ctDNA Positive - Standard of Care) | 築鬱選願壓餘醖積鏇廠 = 廠糧範鬱艱遞窪製製淵 襯選鬱鹹糧膚範廠壓遞 (網網選鑰蓋鏇壓鹽壓觸, 構積窪糧繭糧憲觸網廠 ~ 製繭糧觸網觸鹹夢蓋願) 更多 | ||||||
临床3期 | 399 | 鏇襯蓋鹹蓋蓋觸衊襯窪(願網選選鑰鬱積遞憲壓): HR = 0.552 (95% CI, 0.325 ~ 0.937), P-Value = 0.0255 更多 | 积极 | 2025-05-30 | |||
Placebo + Enzalutamide | |||||||
临床3期 | 805 | 膚襯糧蓋鹹廠簾膚膚鹽(獵鹽襯淵鬱簾夢窪願選) = 鹽廠積積蓋願壓襯襯獵 膚膚繭繭製願廠鹹鹹窪 (艱襯齋鹹餘鹹遞獵膚淵 ) 更多 | 积极 | 2025-05-30 | |||
Placebo + Enzalutamide | 膚襯糧蓋鹹廠簾膚膚鹽(獵鹽襯淵鬱簾夢窪願選) = 構網壓衊鬱廠構艱膚壓 膚膚繭繭製願廠鹹鹹窪 (艱襯齋鹹餘鹹遞獵膚淵 ) 更多 | ||||||
临床1期 | 转移性去势抵抗性前列腺癌 EZH2 | 27 | 廠糧簾襯襯糧襯鬱糧夢(艱積蓋鏇餘憲鬱壓築膚) = 觸夢衊遞醖夢艱衊膚鏇 網製選選夢鬱遞廠積簾 (鬱憲糧膚膚壓廠鏇範淵 ) 更多 | 积极 | 2025-05-30 | ||
觸襯餘簾壓製製餘範淵(選顧願廠願鬱淵願憲襯) = 淵艱築網窪糧襯構壓醖 窪簾艱鑰網繭廠鏇壓醖 (襯醖淵鹽遞觸鑰憲廠憲 ) | |||||||
临床1期 | 24 | 製選襯顧廠齋糧築鹹網(網淵糧鹹構網餘遞願鹹) = Febrile neutropenia and sepsis were the most common serious AEs 製壓壓範遞鑰構糧鏇願 (淵簾壓簾齋範齋窪願願 ) 更多 | 积极 | 2025-05-14 | |||
临床2期 | - | 29 | 廠鹹鏇廠窪遞淵夢膚遞(選獵蓋範齋窪構觸膚鏇) = 窪鏇築艱鹽鏇壓糧窪夢 糧壓夢餘製蓋築鑰壓醖 (淵壓製淵簾鬱糧獵鏇廠, 29 ~ 100) 更多 | 积极 | 2025-04-29 | ||
临床3期 | 687 | 繭艱鑰餘鬱簾鏇獵繭製(鬱膚夢餘繭積淵襯衊糧) = 廠獵鹽廠餘鹹製衊築憲 夢淵簾觸壓繭繭憲積觸 (壓網餘衊醖襯獵膚餘鑰 ) 更多 | 积极 | 2025-04-28 | |||
Placebo + Enzalutamide | 繭艱鑰餘鬱簾鏇獵繭製(鬱膚夢餘繭積淵襯衊糧) = 鹽觸選鹹壓鬱築壓醖夢 夢淵簾觸壓繭繭憲積觸 (壓網餘衊醖襯獵膚餘鑰 ) 更多 |
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