盐酸托泊替康(Topotecan Hydrochloride) - 药物靶点：TOP1_在研适应症：实体瘤，卵巢上皮癌，复发性宫颈癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

9-[(dimethylamino)methyl]-10-hydroxy-(4S)-camptothecin、Nogitecan hydrochloride (JAN)、topotecan

+ [26]

靶点

TOP1

作用机制

TOP1抑制剂(DNA拓扑异构酶I抑制剂)

治疗领域

肿瘤内分泌与代谢疾病呼吸系统疾病+ [7]

在研适应症

实体瘤卵巢上皮癌复发性宫颈癌+ [18]

非在研适应症

习惯性流产急性髓性白血病晚期宫颈癌+ [46]

原研机构

GSK Plc

在研机构

FUJIFILM Pharmaceuticals USA, Inc.Pfizer Europe MA EEIGActavis Group PTC ehf.

+ [10]

非在研机构

GSK PlcTeva Pharmaceuticals Europe BV

Genentech, Inc.

+ [8]

最高研发阶段批准上市

首次获批日期

美国 (1996-05-28),

卵巢癌小细胞肺癌宫颈癌

最高研发阶段(中国)批准上市

特殊审评孤儿药 (美国)

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结构/序列

分子式C23H24ClN3O5

InChIKeyDGHHQBMTXTWTJV-BQAIUKQQSA-N

CAS号119413-54-6

关联

381

项与盐酸托泊替康相关的临床试验

NCT06666712

/ Not yet recruiting临床1期IIT

Chronic Convection Enhanced Delivery of Topotecan for Recurrent Malignant Glioma

The primary goal of this study is to establish the safety of chronic Convection Enhanced Delivery (CED) of the chemotherapeutic drug Topotecan for patients with recurrent malignant glioma that harbors the Isocitrate Dehydrogenase mutation (IDH-mut). The secondary goal of the study is to study drug distribution and assess the tumor response to prolonged continuous CED of Topotecan.
Convection Enhanced Delivery is a novel method of drug delivery that allows administration of a drug directly to the brain. In CED, a drug pump is placed under the skin in the chest or abdominal region. The pump is connected to a catheter that is tunneled underneath the skin to the brain. The tip of the catheter then infuses Topotecan directly onto the brain tumor. There will be a total of four treatment infusions over the course of 23-29 days, with a 5-7-day rest period between each infusion. Throughout this period, patients' health will be monitored through imaging, blood draws, and regular exams. At the end of the treatment period, the pump will be removed, followed by resection of the tumor. Patients will be followed for the duration of their lives.
This is the investigator's second clinical trial studying CED of TPT in recurrent glioma. In the prior Phase 1b trial, chronic pulsatile CED safely and effectively delivered Topotecan to patients with IDH mutant recurrent Glioblastoma (WHO grade 4).

开始日期2025-10-04

申办/合作机构

Columbia University

NCT06647953

/ Not yet recruiting临床3期IIT

Prospective Treatment of Types I, II and III Pleuropulmonary Blastoma (PPB)

This phase III trial tests how well surgery plus chemotherapy compared to surgery alone works in treating patients with type I pleuropulmonary blastoma (PPB), and tests how well surgery plus standard chemotherapy with the addition of topotecan works compared to surgery plus standard chemotherapy alone in treating patients with type II and III PPB.
Historically, most children with type I PPB had surgery and approximately 40% of children with type I PPB received chemotherapy following their surgery, usually for 22-42 weeks. There has not been a consistent standard for which children with type I PPB receive chemotherapy after surgery. For patients whose tumor has been removed completely with surgery, observation without chemotherapy may work as well as giving chemotherapy after surgery in preventing a return of the PPB tumor.
The standard chemotherapy for patients with types II or III PPB in the United States is four cycles of IVADo (ifosfamide, vincristine, dactinomycin, and doxorubicin) followed by 8 cycles of IVA (ifosfamide, vincristine and dactinomycin). Ifosfamide is in a class of medications called alkylating agents. It works by slowing or stopping the growth of tumor cells in the body. Vincristine is in a class of medications called vinca alkaloids. It works by stopping tumor cells from growing and dividing and may kill them. Dactinomycin is a type of antibiotic that is only used in cancer chemotherapy (antineoplastic antibiotic). It works by damaging the cell's deoxyribonucleic acid (DNA) and may kill tumor cells. Doxorubicin is in a class of medications called anthracyclines. Doxorubicin damages the cell's DNA and may kill tumor cells. It also blocks a certain enzyme needed for cell division and DNA repair. Topotecan is in a class of medications called topoisomerase I inhibitors. It works by interfering with tumor cell DNA which kills them. Giving topotecan in addition to standard IVADo and IVA chemotherapy regimens may shrink the cancer as well as or better than the standard therapy or could decrease the chance the tumor spreads while causing fewer side effects.

开始日期2025-03-17

申办/合作机构

The Children's Oncology Group Foundation, Inc.

NCT06425419

/ Not yet recruiting临床1期IIT

The Safety and Efficacy of Intravitreal Topotecan for the Treatment of Proliferative Vitreoretinopathy

The goal of this clinical trial is to evaluate the safety and efficacy of intravitreal topotecan for the treatment of patients with rhegmatogenous retinal detachment due to proliferative vitreoretinopathy (PVR) or resulting from an open globe injury, and compare the outcomes to those who do no receive intravitreal topotecan. The main objectives it aims to achieve are:
* to study the safety profile of intravitreal topotecan in the treatment of PVR
* to evaluate the efficacy of intravitreal topotecan in treating PVR.
Post-consent, participants will:
* undergo vitrectomy (with or without scleral buckle) as part of standard treatment for retinal detachment.
* receive intravitreal topotecan at the time of surgery, post-operative day 7 and post-operative day 28 (if randomized to receive the medication)
* come in at post-operative day 1, 7, 28, 56, 84, 126 and 168 to undergo a complete ophthalmic exam along with a fundus photography and optical coherence tomography of the macula, have their intraocular pressure and visual acuity measured and their adverse events monitored, if any.
Researchers will compare participants who receive intravitreal topotecan for PVR to those who do not to see if there is a significant variability in recurrence of retinal detachment, rate of retinal reattachment and PVR grade 6 months after surgery.

开始日期2025-01-01

申办/合作机构

Massachusetts Eye & Ear Infirmary, Inc.

100 项与盐酸托泊替康相关的临床结果

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100 项与盐酸托泊替康相关的转化医学

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100 项与盐酸托泊替康相关的专利（医药）

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3,400

项与盐酸托泊替康相关的文献（医药）

2025-02-01·EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structure-activity relationship study of novel evodiamine amino acid conjugates with potent anti-colorectal cancer efficacy

Article

作者: Hu, Zecheng ; Jiang, Weifan ; Wang, Zhen ; Peng, Xue ; Zhuo, Linsheng ; Xiong, Yongxia ; An, Zhigang ; Zhang, Siyi ; Lei, Zhengwen ; Chen, Shuting ; Mo, Hanxuan ; Wei, Xiuzhen ; Wu, Junbo ; Zhang, Xi ; Peng, Ying

Evodiamine has been a promising lead structure with broad-spectrum antitumor activity. Druggability optimization is the most challenging part of evodiamine-based lead-to-candidate campaign. Amino acids as building blocks for conjugates are widely incorporated into approved drug and drug candidates, demonstrating highly attractive druggability. Herein, a series of evodiamine amino acid conjugates were designed and synthesized based on the evodiamine lead compound (±)-8b discovered in our previous work. The structure-activity relationship (SAR) studies culminated in the identification of a promising conjugate (-)-15h featuring a N-Boc-l-glutamine group and a chiral carbon atom (sinister), which exhibited nanomolar antiproliferative activity against LoVo and RKO colorectal cancer cells. Moreover, (-)-15h could inhibit topoisomerases I, arrest the cell cycle in the G2/M phase, and induce apoptosis. Importantly, (-)-15h (tumor growth inhibition rate was 82.53 % in 40 mpk) showed better efficacy and tolerability to that of parent compound (-)-8b (tumor growth inhibition rate was 51.22 % in 40 mpk) in LoVo xenograft model. Further, (-)-15h (tumor growth inhibition rate was 70.09 % in 40 mpk) showed comparable efficacy and better tolerability to that of topotecan (tumor growth inhibition rate was 70.67 % in 0.5 mpk) in HT-29 xenograft model. Collectively, this study further provided a strong scientific basis for amino acid-based structural modifications and a drug lead for anti-colorectal cancer applications.

2025-01-01·RETINA-THE JOURNAL OF RETINAL AND VITREOUS DISEASES

HIGH-DOSE INTRAVITREAL TOPOTECAN FOR RECURRENT RETINOBLASTOMA, SUBRETINAL SEEDS, AND VITREOUS SEEDS

Article

作者: Valdes-Perez, Nicole ; Medina, Robert ; Burak acar, Ahmet ; Shields, Jerry A. ; Shields, Carol L. ; Lally, Sara E. ; Evans, Haley ; Bansal, Rolika

Purpose::

To evaluate the efficacy and safety of high-dose intravitreal topotecan (IvitTopo) for recurrent retinoblastoma.

Methods::

There were 13 patients with recurrent retinoblastoma treated with high-dose IvitTopo (90 micrograms [μg]/0.18cc–100 µg/0.20cc). The primary outcome measures were tumor control, globe salvage, and treatment complications.

Results::

At date first seen, median patient age was 9 months, and the affected eye was classified as International Classification of Retinoblastoma Group B (n = 2, 15%), Group C (n = 3, 23%), or Group D (n = 8, 62%) retinoblastoma with initial therapy of intravenous chemotherapy (n = 9, 69%) or intraarterial chemotherapy (n = 4, 31%). Recurrent tumor was detected at median 10 months as solid tumor (n = 3), subretinal seeds (n = 10), and/or vitreous seeds (n = 3) and high-dose IvitTopo (median three injections) delivered at monthly intervals. Additional chemotherapy was delivered by intraarterial (n = 8, 62%) or intravenous (n = 1, 8%) routes, and one eye received additional cryotherapy (n = 1, 8%). In three cases (23%), there was no additional therapy. At mean follow-up of 9 months, regression of solid tumor, subretinal seeds, and vitreous seeds was achieved in 12 cases (92%), and globe salvage was achieved in all cases (n = 13, 100%). Of those three eyes treated with high-dose IvitTopo alone, tumor control was initially achieved in all cases (100%), but one case that previously demonstrated massive vitreous seeding showed late recurrence of a solitary vitreous seed at 8 months. There were no complications.

Conclusion::

High-dose IvitTopo is an effective and safe therapy for recurrent retinoblastoma, in conjunction with other therapy, and possibly as a stand-alone therapy.

2025-01-01·AMERICAN JOURNAL OF OPHTHALMOLOGY

Single- Versus Triple-Agent Intra-Arterial Chemotherapy for Retinoblastoma

Article

作者: Aldhawi, Abeer ; Zaarour, Christian ; Feng, Zhao Xun ; Kletke, Stephanie N ; Gallie, Brenda L ; Muthusami, Prakash ; Alshahrani, Najah O ; Parra-Farinas, Carmen ; Chau, Kelvin ; Mallipatna, Ashwin ; Alshahrani, Najah O. ; Kletke, Stephanie N. ; Shaikh, Furqan ; Gallie, Brenda L.

PURPOSE:

To compare the ocular and systemic outcomes of single- (melphalan) versus triple-agent (melphalan, topotecan, carboplatin) intra-arterial chemotherapy (IAC) for retinoblastoma (RB) eye salvage.

DESIGN:

Retrospective single-institutional clinical cohort study.

METHODS:

Children <18 years with RB who underwent one or more IAC procedures between 2016 and 2024 with minimum 6-month follow-up were reviewed. Data included clinical features, IAC procedural details, additional eye-saving treatments, complications, and follow-up. Primary outcomes included ocular and systemic complications of IAC, intraocular recurrence, extraocular extension, metastasis, and death. Secondary outcomes were tumor response, ocular survival, and recurrence-free ocular survival. Comparative analysis was performed for single- versus triple-agent groups. A SWIMMER^rb plot graphically illustrated additional treatments following IAC.

RESULTS:

Thirty-eight eyes of 37 children (24 unilateral RB) were reviewed. Two eyes (2 children) had single- followed by multi-agent IAC and were excluded. Of 35 included children, one had bilateral triple-agent IAC. IAC (median, 3 doses; range, 1-4) was employed as primary (n = 21 eyes) or secondary (n = 15 eyes) treatment. Chemotherapy was single-agent in 13 eyes and triple-agent in 23 eyes. Following IAC, 25 eyes required additional eye-saving treatments (69% single- v 70% triple-agent, P = .983). At final follow-up, the triple-agent group was more likely to achieve very good partial or complete tumor response (91% v 62%, P = .030). Two-year recurrence-free ocular survival was 63.3% (95% CI 45.7-80.9), similar for both groups (P = .700). Globe salvage was 72%. Two-year ocular survival was 72.2% (95% CI 57.2-87.2), higher for the triple-agent group (82.6% v 53.8%; P = .059). Ocular complications occurred in 31% of eyes in the single- and 52% of eyes in the triple-agent group (P = .215). The rate of systemic complications was 38% versus 74% in the single- versus triple-agent groups, respectively (P = .036). No extraocular extension, metastasis, or death were observed at median 34.2 months (range, 14.5-87.0) follow-up.

CONCLUSIONS:

Triple-agent IAC was associated with improved RB tumor response and ocular survival, though similar recurrence-free ocular survival compared to single-agent. While there were more complications with triple-agent IAC, most were mild or transient.

257

项与盐酸托泊替康相关的新闻（医药）

2025-01-08

·Business Wire

Asher Bio Announces Clinical Trial Collaboration and Supply Agreement on Etakafusp Alfa (AB248) in Combination with Bispecific T-cell Engager in Patients with Small Cell Lung Cancer

SOUTH SAN FRANCISCO, Calif.--( BUSINESS WIRE )--Asher Biotherapeutics, a biotechnology company developing precisely-targeted immunotherapies for cancer and infectious diseases, today announced a clinical trial collaboration and supply agreement with Amgen (NASDAQ:AMGN) to evaluate etakafusp alfa (formerly known as AB248), Asher Bio’s investigational CD8+ T cell targeted interleukin-2 (IL-2) immunotherapy, in combination with IMDELLTRA ® (tarlatamab), Amgen’s DLL3-targeting Bispecific T-cell Engager (BiTE ® ) therapy, in patients with extensive-stage small cell lung cancer (ES-SCLC). “ This clinical trial collaboration and supply agreement with Amgen allows us to further expand on the Phase 1 results for etakafusp alfa in a new combination with IMDELLTRA ® in a global Phase 1b study in ES-SCLC,” said Don O’Sullivan, Ph.D., Chief Business Officer of Asher Bio. “ Based on emerging data to date, we believe etakafusp alfa has the potential to improve the efficacy of T cell engagers (TCEs) by selectively expanding the CD8+ T cell population, improving effector function, tumor infiltration and reversing TCE-induced T cell desensitization. We look forward to collaborating with Amgen to assess the potential for the novel combination to improve outcomes for patients with ES-SCLC.” As part of this collaboration agreement, Amgen will sponsor and operationalize a global Phase 1b study to evaluate the safety and early efficacy of etakafusp alfa in combination with IMDELLTRA ® in patients with ES-SCLC. Asher Bio will retain full ownership of etakafusp alfa and will supply Amgen with etakafusp alfa at no cost. About SCLC SCLC is one of the most aggressive and devastating solid tumor malignancies, with a median survival of approximately 12 months following initial therapy and a 3% five-year relative survival rate for ES-SCLC. 1,2,3 Current second-line treatments impart a short duration of response (median DoR: 3.3–5.3 months) and limited survival (median OS: 5.8-9.3 months), while current third-line treatments for SCLC, which consist primarily of chemotherapy, yield a short median DoR of 2.6 months and a median OS of 4.4-5.3 months. 4-8 SCLC comprises ~15% of the 2.4 million plus patients diagnosed with lung cancer worldwide each year. 9-11 Despite initial high response rates to first-line platinum-based chemotherapy, most patients quickly relapse within months and require subsequent treatment options. 13 About Etakafusp Alfa ( AB248) Etakafusp Alfa ( AB248 ) is a novel CD8+ T cell selective IL-2, generated by fusing a reduced potency IL-2 mutein to an anti-CD8β antibody. It was specifically engineered to selectively and potently activate CD8+ T-cells which are the immune cells that drive anti-tumor efficacy, while avoiding natural killer (NK) cells, which can act as a pharmacological sink and contribute to toxicity, and regulatory T (Treg) cells, which are immunosuppressive. Asher Bio is currently evaluating etakafusp alfa in a Phase 1a/1b clinical trial, AB248-101. The trial consists of a dose escalation and expansion phase to investigate the safety, pharmacokinetics (PK), pharmacodynamics (PD), and anti-tumor activity of etakafusp alfa alone and in combination with pembrolizumab in subjects with locally advanced/metastatic solid tumors who failed prior therapies. Initial pharmacokinetic and pharmacodynamic data from the ongoing Phase 1a/1b clinical trial support etakafusp alfa’s proof of mechanism and activity with a highly differentiated clinical profile. Early data shows potent and selective CD8+ T cell activation without substantial changes to Treg and NK cell numbers and initial evidence of anti-tumor activity, including confirmed objective responses, with a generally well-tolerated safety profile. Please refer to www.clinicaltrials.gov (NCT05653882) for additional details related to this Phase 1a/1b clinical trial. About Asher Bio Asher Bio is a biotechnology company developing therapies to precisely engage specific immune cells to fight cancer and chronic viral infection. We utilize our proprietary cis-targeting platform to develop therapies engineered to overcome limitations of other immune-based treatments by selectively activating specific immune cell types with validated disease fighting functionality. Our candidates feature an antibody connected to a modified immunomodulatory protein, such as a cytokine. Our candidate design is intended to enable our candidates to selectively activate the desired immune cells and not other cells that contribute to toxicity or immune suppression. Our lead program etakafusp alfa (AB248), an IL-2 molecule specifically targeted to CD8+ effector T cells, is currently in Phase 1 trials for oncology. Our broader portfolio includes AB821, an IND-ready CD8-targeted IL-21 immunotherapy, and early-stage programs targeting CAR-T cells, myeloid cells and CD4+ T cells. Asher Bio was founded by Ivana Djuretic and Andy Yeung with support from Third Rock Ventures and is located in South San Francisco. For more information, please visit http://www.asherbio.com and follow us on X (formerly Twitter) @ AsherBio and on LinkedIn . 1 American Cancer Society. Lung Cancer Survival Rates. 2 Paz-Ares L, Chen Y, Reinmuth N, et al. Durvalumab, with or without tremelimumab, plus platinum-etoposide in first-line treatment of extensive-stage small-cell lung cancer: 3-year overall survival update from CASPIAN. ESMO Open. 2022;7:100408. 3 Liu SV, Reck M, Mansfield AS, et al. Updated Overall Survival and PD-L1 Subgroup Analysis of Patients With Extensive-Stage Small-Cell Lung Cancer Treated With Atezolizumab, Carboplatin, and Etoposide (IMpower133). J Clin Oncol. 2021;39:619-630. 4 Trigo J, Subbiah V, Besse B, et al. Lurbinectedin as second-line treatment for patients with small-cell lung cancer: a single-arm, open-label, phase 2 basket trial. Lancet Oncol. 2020;21(5):645-654. 5 Von Pawel J, Schiller JH, Shepherd FA, et al. Topotecan versus cyclophosphamide, doxorubicin, and vincristine for the treatment of recurrent small-cell lung cancer. J Clin Oncol. 1999;17(2):658-67. 6 Von Pawel J, Jotte R, Spigel DR, et al. Randomized phase III trial of amrubicin versus topotecan as second-line treatment for patients with small-cell lung cancer. J Clin Oncol. 2014;32(35):4012-9. 7 Coutinho AD, Shah M, Lunacsek OE, et al. Real-world treatment patterns and outcomes of patients with small cell lung cancer progression after 2 lines of therapy. Lung Cancer. 2019;127:53-58. 8 Borghaei H, Pundole X, Anderson E, et al. Treatment patterns and outcomes in recent US clinical practice for SCLC patients after two prior lines of therapy. Presentation at World Conference on Lung Cancer 2023. September 9-12, 2023; Singapore, SGP. Poster #EP13.07-03. 9 Oronsky B, Abrouk N, Caroen S, et al. A 2022 Update on Extensive Stage Small-Cell Lung Cancer (SCLC). J Cancer. 2022;13:2945-2953. 10 World Health Organization. Lung. 2020. 11 Sabari JK, Lok BH, Laird JH, et al. Unravelling the biology of SCLC: implications for therapy. Nat Rev Clin Oncol. 2017;14:549-561.

临床1期免疫疗法临床3期临床2期

2025-01-08

·优尼特尔制药

优尼特尔制药—公司介绍

优尼特尔中国制药—公司介绍法国优尼特尔制药集团是全球领先的BFS(吹灌封)技术解决方案提供商，专注于为原研药和仿制药客户进行委托生产(CDMO)。我们的产品线涵盖滴眼液、鼻腔护理液及雾化吸入药物等无菌单剂量制剂，以及条形袋装口服液体制剂。集团在全球拥有八家工厂，分别位于法国、美国、巴西和中国，并在法国波尔多设有创新研发中心。此外，我们在法国巴黎、美国罗切斯特、巴西圣保罗和中国南京设有商务办公室，以推动全球业务的扩展。每年，我们的吹灌封技术产品产量超过50亿支，销售网络遍布全球100个国家和地区。集团现有员工超过2000人，年营业额达到4.5亿欧元以上。在中国，优尼特尔制药集团以南京作为其运营的核心基地。优尼特尔南京制药有限公司坐落于风景秀丽的六朝古都南京，具体位置在国家级高新区南京市江宁经济技术开发区将军大道169号，占地面积达5.78万平方米。自2004年成立以来，公司注册资金为2.3669亿人民币，目前拥有近170名员工。2020年8月，法国优尼特尔制药集团正式收购南京瑞年百思特制药有限公司。2024年10月，集团完成了对该公司的全资股权收购。优尼特尔南京制药作为集团全球的第七家工厂，也是其在中国的控股工厂。此次并购将使我们能够为中国眼科和呼吸系统市场的本土及跨国制药公司提供CDMO服务，生产无菌、不含防腐剂的单剂量制剂。优尼特尔南京制药有限公司依托法国的先进技术和经验，致力于在BFS吹灌封技术领域保持领先地位。公司拥有4条进口生产线Rommelag321 & Brevetti Angela Srl和2台Rommelag BP460设备，这些设备将升级以支持眼科、呼吸科、鼻科用药等多领域产品的生产。我们的产品包括盐酸丙美卡因滴眼液、氧氟沙星滴眼液、妥布霉素滴眼液、聚乙烯醇滴眼液、酮咯酸氨丁三醇滴眼液，以及口服固体制剂如甘草锌颗粒、盐酸托泊替康胶囊等。联系我们以获取更多信息! 优尼特尔制药 Single Best Way to Deliver

并购

2025-01-07

·癌度

小细胞肺癌是一种侵袭性肺癌亚型，尽管小细胞肺癌占所有肺癌的15%左右，但是小细胞肺癌的预后很差。大多数小细胞肺癌与吸烟有关，超过三分之二的小细胞肺癌确诊的时候已经是广泛期小细胞肺癌，广泛期小细胞肺癌难以根治性治疗，只能通过药物尽量延长患者的生存时间。小细胞肺癌的一线标准治疗包括依托泊苷联合顺铂，以及联合PD-L1抑制剂如度伐利尤单抗或阿替利珠单抗，但即便是这些治疗小细胞肺癌2年生存率也仅为20%左右，大多数情况下小细胞肺癌初始一线治疗效果很好，但是6个月内都会复发。一旦复发则进行二线治疗的小细胞肺癌选择有限，1996年获批的拓扑替康属于二线治疗的标准疗法，但是这个药物疗效有限且具有血液学毒性。小细胞肺癌二线治疗的另外一种选择是鲁比奈克定，根据一项二期临床试验结果，鲁比奈克定被美国食品药品监督管理局FDA加速批准，但是后面的临床研究表明这款药相比化疗没有能改善生存率，所以对应小细胞肺癌的二线治疗来说很缺乏好的治疗方案。下面给大家介绍的是一款名为戈沙妥珠单抗药（Sacituzumab govitecan，简写SG）。研究结果刊登在最新的国际学术期刊。参考文献刊例示意图 1、戈沙妥珠单抗二线治疗小细胞肺癌戈沙妥珠单抗是一款靶向TROP-2的抗体偶联药，杀灭癌细胞的活性分子为拓扑异构酶I抑制剂伊立替康的活性代谢物SN-38，针对癌细胞的特异性则是一个靶向TROP-2的抗体。具有杀灭癌细胞的活性强，且能引起周围肿瘤微环境改变（旁观者效应）。这款药在全球获批治疗既往接受过治疗的转移性乳腺癌。这一项二期临床试验入组的患者为之前接受过一线治疗后病情进展的广泛期小细胞肺癌，主要研究戈沙妥珠单抗治疗小细胞肺癌的治疗应答率、总生存期和安全性。临床试验中患者肿瘤病灶缩小情况这一项研究共计入组了43名患者，药物治疗的数据如上面的图示，有41.9%的患者可评估肿瘤病灶缩小超过30%（治疗应答率），中位无进展生存时间为4.4个月，中位总生存时间为13.6个月。在治疗应答率方面，如果患者一线使用铂类化疗有效则治疗应答率为47.8%，如果患者一线使用铂类化疗效果不好则二线使用戈沙妥珠单抗的治疗应答率为35%。没有患者因为治疗的不良反应而停药。 2、可以期待的更多联合用药这个研究有点遗憾的是入组的患者数量较少，不过相信三期临床试验应该会招募更多的患者，大家可以在下面的全球临床试验去报名或关注这款药的最新临床试验信息。此外这款药与其他的药物组合也是具有想象力的研究，比如将戈沙妥珠单抗联合免疫治疗，也许会让患者在二线治疗获益更多，关于这个方面的信息欢迎大家关注癌度，及时了解全球肿瘤诊疗的最新进展！癌度与吉因加启动的“基因检测人人可及”计划里，仅需要3000元就能检测36个基因，大家可以联系癌度或扫描上面的二维码咨询癌度医学顾问，了解基因检测的相关问题。参考文献： Dowlati A, et al., Phase 2 Open- Label Study of Sacituzumab Govitecan as Second-Line Therapy in Patients With Extensive-Stage Small Cell Lung Cancer: Results From TROPiCS-03, Journal of Thoracic Oncology (2025). 往期推荐抗癌新武器：更有针对性的癌症组合前药TTFA-Platin究竟是什么东东？肿瘤化疗中的隐形杀手：揭秘化疗引起的腹泻真相靶向ROR1的抗体偶联药MK-2140,全部患者病灶消失！再来一款HER2抗体偶联药，ARX788的三期临床研究数据公布！

加速审批临床2期临床结果临床3期上市批准

100 项与盐酸托泊替康相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D02168	盐酸托泊替康	L01XX17	DB01030

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
实体瘤	日本	Nippon Kayaku Co., Ltd.	2013-11-20
复发性宫颈癌	欧盟	Pfizer Europe MA EEIG	2010-06-09
复发性宫颈癌	冰岛	Pfizer Europe MA EEIG	2010-06-09
复发性宫颈癌	列支敦士登	Pfizer Europe MA EEIG	2010-06-09
复发性宫颈癌	挪威	Pfizer Europe MA EEIG	2010-06-09
卵巢上皮癌	欧盟	Teva Pharmaceuticals Europe BV	2009-09-21
卵巢上皮癌	冰岛	Teva Pharmaceuticals Europe BV	2009-09-21
卵巢上皮癌	列支敦士登	Teva Pharmaceuticals Europe BV	2009-09-21
卵巢上皮癌	挪威	Teva Pharmaceuticals Europe BV	2009-09-21
复发性小细胞肺癌	欧盟	Sandoz Pharmaceuticals DD (Belarus)	1996-11-12
复发性小细胞肺癌	冰岛	Sandoz Pharmaceuticals DD (Belarus)	1996-11-12
复发性小细胞肺癌	列支敦士登	Sandoz Pharmaceuticals DD (Belarus)	1996-11-12
复发性小细胞肺癌	挪威	Sandoz Pharmaceuticals DD (Belarus)	1996-11-12
卵巢癌	美国	Sandoz, Inc.	1996-05-28
小细胞肺癌	美国	Sandoz, Inc.	1996-05-28
宫颈癌	美国	Sandoz, Inc.	1996-05-28

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
脑转移瘤	临床3期	美国	GSK Plc	2006-12-01
脑转移瘤	临床3期	加拿大	GSK Plc	2006-12-01
脑转移瘤	临床3期	匈牙利	GSK Plc	2006-12-01
脑转移瘤	临床3期	波兰	GSK Plc	2006-12-01
脑转移瘤	临床3期	俄罗斯	GSK Plc	2006-12-01
脑转移瘤	临床3期	斯洛伐克	GSK Plc	2006-12-01
转移性非小细胞肺癌	临床3期	美国	GSK Plc	2006-12-01
转移性非小细胞肺癌	临床3期	加拿大	GSK Plc	2006-12-01
转移性非小细胞肺癌	临床3期	匈牙利	GSK Plc	2006-12-01
转移性非小细胞肺癌	临床3期	波兰	GSK Plc	2006-12-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT02312245 (CTgov)	临床2期	铂耐药性输卵管癌 \| 复发性卵巢癌 \| 复发性原发性腹膜癌	13	Paclitaxel+Bevacizumab (Arm A (Avatar-directed Paclitaxel))	糧積窪蓋鏇觸醖衊艱憲(積遞網齋繭範選艱醖衊) = 範觸艱築選糧選糧製襯齋遞壓遞遞襯構鹹淵衊 (繭齋膚觸襯壓網衊鹽鹹, 觸積積艱鹹齋鹹鹽願鹹 ~ 鏇鹽積壓鏇觸夢衊齋積) 更多	-	2024-12-05
				Gemcitabine Hydrochloride (Arm B (Avatar-directed Gemcitabine Hydrochloride))	糧積窪蓋鏇觸醖衊艱憲(積遞網齋繭範選艱醖衊) = 願廠積網簾廠廠鹹蓋築齋遞壓遞遞襯構鹹淵衊 (繭齋膚觸襯壓網衊鹽鹹, 鹽範齋選壓鹹鏇廠壓糧 ~ 顧範獵醖鏇選鹹築範鏇) 更多
NCT04947501 (N9, ASCO2024) 人工标引	早期临床1期	高风险神经母细胞瘤	15	cyclophosphamidehostopotecanopovincristineistifosfamidecarboplatinetoposide	廠繭餘積夢鹹簾鹹蓋構(簾淵醖積齋鹹窪壓築壓) = 夢遞鬱淵鑰製積蓋夢選餘餘遞構餘範憲艱鑰觸 (淵製網襯蓋壓醖構鹽膚 ) 更多	积极	2024-05-24
				cyclophosphamideplatopotecansidvincristineifosfamidecarboplatinetoposide	蓋糧鹹鏇廠壓壓繭壓願(窪願窪選願憲鹹膚膚淵) = 網醖鏇構簾築窪範夢淵簾鹽構繭鏇鹹齋襯醖鑰 (顧糧鹽遞艱糧鹹鹹製範 ) 更多
NCT02308527 (ITCC-SIOPEN BEACON-Neuroblastoma, Pubmed) 人工标引	临床2期	神经母细胞瘤	160	Temozolomideirinotecantopotecantemozolomidebevacizumab	鹹餘衊憲淵夢鬱糧顧膚(網築夢糧襯製醖獵鹹齋) = 壓衊獵顧觸淵夢廠餘積窪鹹願艱蓋範壓蓋觸壓 (鬱網餘築願淵廠淵構襯, 17 ~ 37)	积极	2024-01-08
				temozolomideemozolirinotecantopotecan	鹹餘衊憲淵夢鬱糧顧膚(網築夢糧襯製醖獵鹹齋) = 繭範膚餘簾衊鏇壓襯範窪鹹願艱蓋範壓蓋觸壓 (鬱網餘築願淵廠淵構襯, 10 ~ 28)
NCT00960739 (MIITOP, Pubmed \| Pediatr Blood Cancer)	临床2期	复发性神经母细胞瘤	-	<sup>131</sup>I-metaiodobenzylguanidine + Topotecan	鬱餘憲艱餘餘觸選鏇選(鏇遞遞繭窪齋艱齋鑰艱) = 觸艱鑰鏇壓積網獵築繭遞糧夢範鑰壓糧獵鑰襯 (鹽衊築遞廠蓋壓簾醖鹹, 6 ~ 32) 更多	积极	2023-11-01
ESMO2023	N/A	小细胞肺癌二线	-	Lurbinectedin	餘觸壓齋壓窪範範積繭(繭蓋衊網齋鹽夢構壓廠) = 齋餘獵網壓夢憲廠膚窪選廠簾繭遞願鑰鬱鬱範 (鏇遞鑰齋淵構選鏇鬱衊 )	-	2023-10-21
				Topotecan with or without trilaciclib	餘觸壓齋壓窪範範積繭(繭蓋衊網齋鹽夢構壓廠) = 鹹窪獵鬱壓簾齋糧糧壓選廠簾繭遞願鑰鬱鬱範 (鏇遞鑰齋淵構選鏇鬱衊 )
ARVO2023	N/A	视网膜母细胞瘤	3	topotecan (Ophthalmic artery chemosurgery (OAC))	積鹽繭顧醖襯觸壓鑰願(觸範餘獵製簾製憲簾鑰) = 衊淵簾簾顧選艱鑰廠齋選鏇壓鬱廠選憲餘鏇繭 (蓋鹹繭積艱衊淵蓋蓋鹽 ) 更多	-	2023-04-23
				topotecan (Intravenous infusion (IV))	積鹽繭顧醖襯觸壓鑰願(構鏇齋簾遞鬱蓋糧範築) = 膚夢壓襯簾餘醖蓋積蓋積繭衊齋膚築夢糧繭觸 (製鏇鹹廠襯顧鹽積繭鬱 ) 更多
NCT01600573 (TOPAZ, Pubmed)	临床1/2期	复发性卵巢癌	-	Pazopanib	願襯鑰壓夢繭鹹廠獵蓋(獵觸築襯顧願夢淵顧襯) = 製醖齋淵糧鹹願醖壓蓋繭網餘醖淵築窪夢繭範 (選鏇艱遞淵糧鑰鹹鹽製 )	积极	2023-03-31
NCT00803062 (Gynecologic Oncology Group protocol 240, Pubmed)	临床3期	晚期宫颈癌一线	452	paclitaxel 175 mg/m2 plus topotecan 0.75 mg/m2	鹽鑰艱遞糧鬱顧鹽範繭(網鹽夢淵製鹽壓醖鹹積) = 選夢簾積鏇積糧鹹鹽網鑰選淵艱鏇製築齋製糧 (選艱鏇膚淵繭顧襯廠蓋 )	不佳	2023-03-08
				cisplatin 50 mg/m2 plus paclitaxel 135 or 175 mg/m2	鹽鑰艱遞糧鬱顧鹽範繭(網鹽夢淵製鹽壓醖鹹積) = 鏇顧製餘襯餘齋衊獵顧鑰選淵艱鏇製築齋製糧 (選艱鏇膚淵繭顧襯廠蓋 )
NeCTuR (IGCS2022)	N/A	复发性宫颈癌二线	-	Topotecan, paclitaxel, and bevacizumab (TPB)	窪衊範顧壓艱遞範遞鑰(壓獵觸醖襯鬱獵鹽壓願) = 齋鏇繭鏇繭鏇顧糧繭齋蓋鏇遞襯選壓淵觸築襯 (鬱顧膚膚膚顧餘襯製簾 ) 更多	积极	2022-12-04
				Chemotherapy without TPB	窪衊範顧壓艱遞範遞鑰(壓獵觸醖襯鬱獵鹽壓願) = 壓鹽選壓糧蓋願獵顧製蓋鏇遞襯選壓淵觸築襯 (鬱顧膚膚膚顧餘襯製簾 ) 更多
NCT04768296 (DDRiver SCLC 250, ESMO2022) 人工标引	临床2期	复发性小细胞肺癌 \| 小细胞癌	6	Berzosertib 105 mg/m2+Topotecan 1.25 mg/m2 (solid tumours)	鑰淵範觸淵艱鏇鑰衊鹽(衊選憲膚廠繭鬱鏇顧夢) = 衊簾壓餘簾艱獵網製積醖窪鹽淵壓鹹繭願壓淵 (壓範願淵襯顧構夢鹹積 ) 更多	积极	2022-09-10
				Berzosertib 210 mg/m2+Topotecan 1.25 mg/m2 ( pt-resistant SCLC)	鑰淵範觸淵艱鏇鑰衊鹽(衊選憲膚廠繭鬱鏇顧夢) = 廠積膚獵夢獵鑰鹽鏇襯醖窪鹽淵壓鹹繭願壓淵 (壓範願淵襯顧構夢鹹積 ) 更多