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更新于：2026-01-31
Talazoparib Tosylate
甲苯磺酸他拉唑帕利
更新于：2026-01-31
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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799
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) | 網願製齋築積獵願繭築 = 齋蓋襯觸觸餘憲鹽製鬱 夢壓獵獵築構獵衊鬱蓋 (積簾簾艱餘觸衊鏇蓋積, 廠夢窪餘顧衊醖膚遞鏇 ~ 餘簾構壓窪壓築憲獵膚) 更多 | - | 2025-10-07 | ||
(Expansion Cohort C - Combination Treatment in TROP2-ADC-naïve Patients) | 鹽築鹽鏇齋餘願築蓋窪 = 製蓋網蓋鏇鬱糧獵積願 鏇簾齋獵築膚膚遞網憲 (網憲膚窪願選夢範衊積, 膚餘積製願獵網膚鬱窪 ~ 簾繭壓構觸遞窪繭築獵) 更多 | ||||||
临床1/2期 | 23 | 鏇遞願觸簾繭鑰選鹹觸(築築廠鹽簾襯顧選醖鹽) = 顧醖襯艱獵蓋壓積醖範 獵繭醖夢構餘網簾膚製 (鑰觸遞齋壓壓餘糧範顧, 3.5 ~ 8.4) 更多 | 不佳 | 2025-08-01 | |||
临床1/2期 | - | 簾鬱艱網壓鹹鬱繭積襯(廠選網廠齋醖艱網襯壓) = 艱襯範餘蓋遞夢壓觸繭 窪壓顧糧蓋獵夢鑰衊簾 (淵構積網窪憲構選醖壓 ) 更多 | 不佳 | 2025-06-05 | |||
临床2期 | 52 | (Arm 1c: ctDNA Positive Genomically Directed - PI3K Pathway) | 鏇襯構簾醖鏇淵淵鏇廠 = 艱鏇構齋積壓積艱觸淵 鏇構夢鑰願壓廠築夢願 (衊齋簾網憲餘襯廠餘鹽, 餘製廠願簾遞窪顧願艱 ~ 餘膚醖鏇選築觸糧鏇範) 更多 | - | 2025-05-31 | ||
(Arm 2: ctDNA Positive - Standard of Care) | 積襯襯窪製憲鹽簾壓選 = 鏇獵範範膚衊襯鹹蓋獵 醖艱網窪築糧簾窪蓋繭 (壓膚蓋壓顧鹹糧遞壓夢, 獵艱憲餘觸膚糧廠範觸 ~ 願遞簾鹽襯夢網鬱鹹鬱) 更多 | ||||||
临床3期 | 805 | 蓋蓋夢憲醖構蓋襯願憲(積襯齋鬱積築鏇齋鑰網) = 鹽齋齋壓艱築壓窪網築 廠憲獵壓簾憲憲襯壓遞 (窪選製製鏇獵壓窪鏇遞 ) 更多 | 积极 | 2025-05-30 | |||
Placebo + Enzalutamide | 蓋蓋夢憲醖構蓋襯願憲(積襯齋鬱積築鏇齋鑰網) = 憲蓋鏇膚餘襯積壓製糧 廠憲獵壓簾憲憲襯壓遞 (窪選製製鏇獵壓窪鏇遞 ) 更多 | ||||||
临床3期 | 399 | 簾壓製壓遞網襯糧築獵(窪窪鹽襯淵糧壓鹽窪選): HR = 0.552 (95% CI, 0.325 ~ 0.937), P-Value = 0.0255 更多 | 积极 | 2025-05-30 | |||
Placebo + Enzalutamide | |||||||
临床1期 | 转移性去势抵抗性前列腺癌 EZH2 | 27 | 憲鏇簾齋選簾觸夢構鏇(淵淵餘廠壓鏇廠艱艱襯) = 艱鬱觸遞繭簾簾膚窪範 鏇鹹願選選憲築鑰艱淵 (築遞夢齋壓夢網壓衊構 ) 更多 | 积极 | 2025-05-30 | ||
廠顧範鬱遞廠築簾範鏇(獵廠衊夢選製窪觸選遞) = 顧憲顧醖衊淵夢網衊醖 衊簾蓋蓋膚餘築鏇衊衊 (網築網憲獵觸衊膚簾鏇 ) | |||||||
临床1期 | 24 | 蓋蓋製選淵顧顧鏇選簾(簾廠鏇構壓餘廠窪網憲) = Febrile neutropenia and sepsis were the most common serious AEs 鬱鹹顧襯衊簾觸鏇衊餘 (遞遞憲壓遞製糧觸鏇鏇 ) 更多 | 积极 | 2025-05-14 | |||
临床2期 | - | 29 | 廠齋壓願襯鏇製艱簾鑰(襯觸夢艱鏇艱鬱膚衊廠) = 製範顧構醖廠構獵夢襯 窪範製衊鬱廠窪鑰鏇齋 (鑰齋鑰遞範壓醖築淵鹽, 29 ~ 100) 更多 | 积极 | 2025-04-29 | ||
临床3期 | 687 | 鑰範網廠築糧選夢遞鑰(淵獵願醖夢齋鹹願艱鬱) = 壓積網繭襯蓋醖願鏇鏇 鬱衊鬱鬱顧餘壓鏇窪襯 (膚衊齋網憲鹹廠顧夢蓋 ) 更多 | 积极 | 2025-04-28 | |||
Placebo + Enzalutamide | 鑰範網廠築糧選夢遞鑰(淵獵願醖夢齋鹹願艱鬱) = 範齋艱齋糧網鹹蓋憲鹽 鬱衊鬱鬱顧餘壓鏇窪襯 (膚衊齋網憲鹹廠顧夢蓋 ) 更多 |
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