盐酸曲拉西利(Trilaciclib Dihydrochloride) - 药物靶点：CDK4 x CDK6_在研适应症：广泛期小细胞肺癌，化疗引起的骨髓抑制，三阴性乳腺癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Trilaciclib、Trilaciclib hydrochloride、G1T 28

+ [4]

靶点

CDK4 x CDK6

作用机制

CDK4抑制剂(细胞周期蛋白依赖性激酶4抑制剂)、CDK6抑制剂(细胞周期蛋白依赖性激酶6抑制剂)

治疗领域

肿瘤血液及淋巴系统疾病呼吸系统疾病+ [1]

在研适应症

广泛期小细胞肺癌化疗引起的骨髓抑制三阴性乳腺癌+ [3]

非在研适应症

化疗引起的发热性中性粒细胞减少症结直肠癌转移性结直肠癌+ [4]

原研机构

G1 Therapeutics, Inc.

在研机构

G1 Therapeutics, Inc.

江苏先声药业有限公司

先聲藥業集團有限公司

+ [1]

非在研机构-

最高研发阶段批准上市

首次获批日期

美国 (2021-02-12),

化疗引起的骨髓抑制

最高研发阶段(中国)批准上市

特殊审评突破性疗法 (美国)、快速通道 (美国)、优先审评 (中国)、附条件批准 (中国)

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结构/序列

分子式C24H32Cl2N8O

InChIKeyBRCYOXKEDFAUSA-UHFFFAOYSA-N

CAS号1977495-97-8

关联

51

项与盐酸曲拉西利相关的临床试验

ChiCTR2400094918

/ Suspended临床2期IIT

A prospective, single-arm, phase II clinical study of recombinant human endostatin in combination with trilaciclib, paclitaxel, carboplatin, and anti-PD-(L)1 as first-line treatment for advanced (stage IIIB-IV) squamous non-small cell lung cancer

开始日期2024-12-31

申办/合作机构

上海市胸科医院

NCT06714266

/ Not yet recruiting临床2期IIT

A Prospective, Single-arm, Phase II Clinical Trial to Evaluate the Efficacy and Safety of Trilaciclib in Preventing Hematopoietic Suppression in Patients with Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma Receiving Either Single Chemotherapy or Chemotherapy Combined with Immunotherapy/targeted Therapy.

This prospective, single-arm, exploratory, phase II study was designed to evaluate the efficacy and safety of Trilaciclib in reducing chemotherapy-induced neutropenia in patients with recurrent or metastatic head and neck squamous cell carcinoma. Eligible subjects screened by the inclusion and exclusion criteria will receive chemotherapy alone or combined with immune/targeted therapy and Trilaciclib for 4-6 cycles of continuous treatment. If the efficacy is not progressive after 4-6 cycles of treatment, the investigators can combine with Trilaciclib during immune and/or targeted maintenance therapy according to the specific conditions of the subjects until disease progression or intolerance. The efficacy of Trilaciclib will be evaluated by the incidence of grade ≥3 neutropenia during chemotherapy as the primary endpoint.
After the progression of treatment, if the subjects were treated with chemotherapy for subsequent treatment and were considered to be able to use Trilaciclib according to the evaluation of the investigator, the use of treaclib could be considered until the subjects had disease progression again or were intolerant to treatment.

开始日期2024-12-15

申办/合作机构

山东省肿瘤医院

ChiCTR2400093139

/ SuspendedN/AIIT

A real-world study on the efficacy and safety of Trilaciclib in bone marrow protection before chemotherapy for advanced solid tumors

开始日期2024-11-30

申办/合作机构-

100 项与盐酸曲拉西利相关的临床结果

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100 项与盐酸曲拉西利相关的转化医学

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100 项与盐酸曲拉西利相关的专利（医药）

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91

项与盐酸曲拉西利相关的文献（医药）

2025-01-23·JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Potent and Selective CDK4/6 Inhibitors for the Treatment of Chemotherapy-Induced Myelosuppression

Article

作者: Shi, Wei ; Li, You ; Hu, Xiaolong ; Xiong, Fei ; Ye, Wencai ; Wang, Lu ; Wang, Rong ; Mi, Yahui ; Qian, Jianqiang ; Pan, Mingshi ; Zhang, Xiaoqi ; Jia, Zhaotong ; Wang, Hao

Chemotherapy-induced myelosuppression (CIM) significantly impairs hematopoiesis. Trilaciclib (TC), originally developed for oncology application, is the only FDA-approved CDK4/6 inhibitor for CIM, which effectively protects bone marrow cells by inhibiting their proliferation. In this study, a series of TC derivatives were designed and synthesized as CDK4/6 inhibitors (CDK4/6i) for alleviating CIM. Among these, 42 displayed potent CDK4/6 inhibitory activity (IC₅₀ = 11 nM), lower cytotoxicity (CC₅₀ > 100 μM) and showed high selectivity among 86 kinases. Additionally, 42 possessed strong bone marrow penetration, favorable pharmacokinetic properties, excellent safety profiles, and superior efficacy in mitigating myelosuppression caused by 5-fluorouracil (5-FU) in vivo. In conclusion, as the first oral small-molecule CDK4/6 inhibitor optimized specifically for myelosuppression treatment, 42 expands the therapeutic applications of CDK4/6i, optimizes the mode of administration, and offers significant translational value and clinical potential.

2025-01-03·JNCI Cancer Spectrum

Trilaciclib prior to FOLFOXIRI/bevacizumab for patients with untreated metastatic colorectal cancer: phase 3 PRESERVE 1 trial

Article

作者: Wang, Wayne ; Bondarenko, Igor ; Danielewicz, Iwona ; Adeleye, Jennifer ; Zhang, Yanqiao ; Beelen, Andrew ; Hubbard, Joleen ; García-Alfonso, Pilar ; Chen, Emerson Y ; Liu, Tianshu ; Jones, Robert ; Aapro, Matti ; Wang, Jufeng ; Lenz, Heinz-Josef ; Ghidini, Michele ; Horváth, Zsolt

Abstract:

Background:

In metastatic colorectal cancer (mCRC), improvements in survival from combining leucovorin/fluorouracil/oxaliplatin/irinotecan (FOLFOXIRI) with bevacizumab have come at the risk of increased rates of high-grade toxicities. Trilaciclib is indicated to decrease the incidence of chemotherapy-induced myelosuppression in patients receiving standard-of-care chemotherapy for extensive-stage small cell lung cancer.

Methods:

Patients with untreated mCRC were randomly assigned 1:1 to trilaciclib (n = 164) or placebo (n = 162) prior to FOLFOXIRI/bevacizumab for up to 12 cycles (induction), followed by trilaciclib or placebo prior to fluorouracil/leucovorin/bevacizumab (maintenance). Co-primary endpoints were duration of severe (grade 4) neutropenia (DSN) in cycles 1-4 and occurrence of severe neutropenia (SN) during induction. Secondary endpoints included antitumor efficacy, survival, and safety.

Results:

The study met its co-primary endpoints. Administering trilaciclib prior to FOLFOXIRI/bevacizumab resulted in significant reductions in DSN in cycles 1-4 vs placebo (mean, 0.1 vs 1.3 days; P < .001) and occurrence of SN during induction (1.3% vs 19.7%; adjusted relative risk [96% CI] = 0.07 [0.0 to 0.3]; P < .001). Grade 3/4 adverse events, including neutropenia, diarrhea, and leukopenia, were less frequent with trilaciclib vs placebo (64.8% vs 73.1%). Trilaciclib was associated with fewer chemotherapy dose reductions and delays and with reduced administration of supportive therapies, compared with placebo. Objective response rate (41.6% vs 57.1%; P = .009) and median progression-free survival (10.3 vs 13.1 months; P < .001) were significantly lower with trilaciclib vs placebo.

Conclusions:

Administering trilaciclib prior to FOLFOXIRI/bevacizumab protected the neutrophil lineage from the effects of chemotherapy-induced myelosuppression. However, antitumor efficacy endpoints favored placebo.

Trial registration:

ClinicalTrials.gov: NCT04607668.

2024-11-01·Journal of Thoracic Disease

Myeloprotection effects of trilaciclib in Chinese patients with extensive stage small cell lung cancer (ES-SCLC) receiving chemotherapy—a real-world study

Article

作者: Liu, Lirong ; Chen, Yongxing ; Yang, Chen ; Meng, Chong ; Chen, Tao ; Liu, Kai

Background:

Trilaciclib, an intravenous short acting cyclin-dependent kinase 4/6 inhibitor, has been approved for the prevention of chemotherapy-induced myelosuppression (CIM) in patients with extensive stage small cell lung cancer (ES-SCLC) receiving platinum/etoposide (EP) or topotecan (TPT)-based therapy in United States (US) since February 2021. Trilaciclib use received the priority review and approval in a real-world setting in China. This study thus aimed to collect real-world data and evaluate the protective effect of trilaciclib on CIM in Chinese patients with ES-SCLC.

Methods:

This single-arm, noninterventional real world study invited all patients with ES-SCLC who received trilaciclib with the platinum and etoposide ± anti-programmed cell death ligand-1 [anti-PD-(L)1] antibodies (EP group) or trilaciclib with TPT (TPT group) in Boao, Hainan China to participate in the study. The primary endpoint was the incidence of the severe (grade four) neutropenia (SN), and the secondary endpoints included other myeloprotection effects, safety and anti-tumor activity.

Results:

Between August 2021 and December 2022, a total of 30 patients who received trilaciclib with chemotherapy consented to participate in this real-world study. Among the enrolled patients, 26 patients were treated with EP regimen, of these, 18 patients were combined with anti-PD-(L)1 antibodies, and 4 patients were treated with TPT. The incidence of SN was 6.7%, with one patient each in EP group and TPT group. The incidence of grade three hematological toxicities was 30% (9/30), with 19.2% (5/26) in the EP group, and 100% (4/4) in the TPT group. The incidence of grade four hematological toxicities was 5/30 (16.7%), with 3/26 (11.5%) and 2/4 (50%) in EP and TPT group, respectively. Overall, the incidence of those who received intravenous or oral antibiotics was 6/30 (20%), with 4/26 (15.4%) in the EP group, and 2/4 (50%) in the TPT group. No ≥ grade three adverse events, serious adverse events (SAEs), and adverse events of special interest associated with trilaciclib were reported.

Conclusions:

Trilaciclib decreased the incidence of CIM in Chinese patients when administered prior to an EP-containing regimen [combined with or without PD-(L)1] or TPT for ES-SCLC. The effect of myeloprotection, anti-tumor and safety were all consistent with the studies conducted globally and data from the Chinese Phase three placebo-controlled study (TRACES).

351

项与盐酸曲拉西利相关的新闻（医药）

2025-02-06

·CPHI制药在线

阿贝西利片将迎国内首仿，这一火爆赛道还是入局好时机吗？

关注并星标CPHI制药在线近期，国家药品监督管理局药品审评中心（CDE）官网显示，齐鲁制药提交的阿贝西利片的4类仿制上市申请已获得受理。阿贝西利是一款CDK4/6抑制剂，由礼来原研。而在CDK4/6抑制剂仿制药领域，齐鲁制药还获批上市了哌柏西利胶囊，成为国内市场上的首仿。随着仿制药的陆续上市，CDK4/6抑制剂赛道必将迎来一场混战。 CDK4/6抑制剂的作用机制 CDK（Cyclin-dependent Kinase）全称为“细胞周期蛋白依赖性激酶”，是丝氨酸/苏氨酸蛋白激酶家族成员，在细胞周期调节中起着至关重要的作用。CDK4/6即细胞周期蛋白依赖性激酶4和6，二者生化特性、结构和功能相似。CDK4和CDK6被D型细胞周期蛋白（Cyclins D）激活后，将磷酸化视网膜母细胞瘤蛋白（pRb），导致其灭活，进而诱导细胞从G1期到S期，导致癌细胞无序增殖扩散。CDK4/6抑制剂通过抑制CDK4/6的活性，阻断细胞从G1期到S期的进程，从而抑制肿瘤细胞增殖。卷成红海的CDK4/6抑制剂，还值得入局吗？ CDK自发现以来，一直被视为破坏癌细胞分裂和增殖的关键靶点，尤其在乳腺癌领域。多年来，药企对CDK4/6抑制剂的研发热情高涨，该赛道竞争十分激烈。 2015年，由辉瑞研发的哌柏西利（Palbociclib）获FDA批准上市，用于激素受体阳性（HR+）/人表皮生长因子受体2阴性（HER2-）的局部晚期或转移性乳腺癌的治疗，这是全球首款获批上市的CDK4/6抑制剂，分为片剂和胶囊两种剂型。目前，哌柏西利已成为HR+/HER2-乳腺癌患者的一线疗法，并获全球超90个国家批准，用于HR+/HER2-乳腺癌的一线、二线治疗。2018年-2022年，哌柏西利业绩营收均在40-50亿美元左右。随着2023年1月，哌柏西利的化合物专利到期，迎来更为激烈的市场竞争。2020年12月，齐鲁制药的哌柏西利胶囊获批上市，是国内首仿。2022年，豪森、山香药业的哌柏西利胶囊也先后获批上市。 2024年6月，石药集团子公司欧意药业的哌柏西利片获批上市，是国内该款药物的首仿产品。正大天晴的哌柏西利片剂仿制药申请正在接受药监局审查。齐鲁也曾于2022年4月提交过哌柏西利片的3类注册申请。哌柏西利的竞争，一目了然。第二款获批上市的是诺华/大冢的瑞波西利（ribociclib），该药于2017年3月获FDA批准上市，与芳香酶抑制剂联合使用作为内分泌的初始疗、绝经后女性激素局部晚期或转移性乳腺癌的一线治疗。后续瑞波西利又被FDA批准用于治疗HR +/HER2-晚期或转移性女性乳腺癌患者，成为首款联合AI治疗绝经前、围绝经、绝经后女性患者的CDK4/6抑制剂。 2017年9月，礼来的阿贝西利（Abemaciclib）获FDA批准上市，用于治疗某些类型的HR+/HER2-晚期或转移性乳腺癌，并在后续获批用于治疗淋巴结阳性，高复发风险且Ki-67≥20%的HR+/HER2-早期乳腺癌患者的辅助治疗，成为全球首款获批此适应症的CDK4/6抑制剂。自从阿贝西利拿下早期乳腺癌适应症后，市场格局彻底改变。据礼来2023年财报显示，阿贝西利的全球销售额为38.63亿美元，同比上涨56%。不过阿贝西利的核心专利将于2029年到期，已有众多药企对其仿制药虎视眈眈。后续上市的CDK4/6抑制剂还有G1 Therapeutics的曲拉西利（Trilaciclib）和恒瑞医药的达尔西利。其中，曲拉西利获批适应症为骨髓抑制的治疗，是全球首个全系骨髓保护创新药物。恒瑞的达尔西利于2021年获NMPA批准上市，适应症为联合氟维司群用于HR+/HER2-的经内分泌治疗后进展的复发或转移性乳腺癌的治疗。后续适应症扩大至联合芳香化酶抑制剂治疗HR+/HER2-局部晚期或转移性乳腺癌患者。除已上市药物外，据公开资料，目前国内至少有8款CDK4/6抑制剂的临床阶段推至III期，而且适应症主要集中在HR+乳腺癌，涉及的药企包括正大天晴、贝达药业、复星医药、轩竹生物、先声药业等。另外还有至少9款CDK4/6抑制剂处于临床Ⅱ期阶段，涉及的药企包括豪森药业等。而且除了创新药以外，国内CDK4/6抑制剂仿制药竞争也相当激烈。那么，国内药企此时入局CDK4/6抑制剂赛道还是好时机吗？答案是肯定的。主要基于两方面原因，一方面，目前CDK4/6抑制剂市场仍以辉瑞、诺华、礼来三家产品为主流，仅2023年，三家销售总额就接近100亿美元，国内药企还有弯道超车的机会。另一方面，乳腺癌已成为全球第一大癌症，从市场空间看，CDK4/6抑制剂的主要适应症——HR+/HER2-，是乳腺癌的主要亚型，占所有病例的近70%，市场空间巨大。据Nature Reviews Drug Discovery预计，到2029年，CDK4/6抑制剂预计将贡献200亿美元，占乳腺癌药物销售市场份额的42%。这一数字足以让任何药企为之动容。不过光鲜背后也有隐忧，CDK4/6抑制剂也会存在患者耐药或副作用等问题，同时吸引了全球药企投身其中寻求新的突破口。如何突破内卷？在耐药性问题方面，PIK3CA/AKT1/PTEN的改变在乳腺癌中经常发生，影响到多达50%的HR+晚期乳腺癌患者。在这一背景下，AKT抑制剂Truqap（capivasertib）应运而生。 AKT（磷酸激酶B），是PAM信号通路中的关键分子，PAM是细胞内重要的传导通路之一，发挥着抑制细胞凋亡，促进细胞增殖的作用，与人类肿瘤的发生、发展密切相关。 Truqap是一款AKT1/2/3高效选择性抑制剂。2023年11月，Truqap获FDA批准上市，用于治疗HR+/HER2-局部晚期或转移性乳腺癌患者，这些患者在接受内分泌基础方案治疗过程中或之后疾病复发或进展。国内目前有8款AKT抑制剂进入临床阶段，涉及药企包括南京正大天晴、海昶生物、来凯医药、恒瑞医药等。在副作用方面，目前困扰CDK4/6抑制剂的一个问题就在于毒性问题。最常见的不良反应是中性粒细胞减少和骨髓抑制，尤其是哌柏西利和瑞波西利出现比例最高，3-4级中性粒细胞减少的比例为60%-66%。为了降低副作用，CDK家族成员CDK2成为目前研究热点之一。同时，CDK2抑制剂还可能克服CDK4/6抑制剂耐药难题。研究表明，在CDK4被抑制后，CDK2会接管其作用并促进癌细胞增殖。这些癌细胞不仅会继续生长，还可能对之前的CDK抑制剂治疗产生耐药。这表明CDK2可能是CDK4/6耐药机制之一。根据公开资料，目前围绕CDK2靶点，全球已有几十款在研新药，大部分处于临床前阶段。其中，辉瑞的PF-07104091片、阿斯利康的AZD8421等CDK2抑制剂处于I/II期临床研究阶段。国内百济神州与昂胜医药达成合作，引进后者一款在研CDK2抑制剂ETX-197，已于2024年8月在国内获批临床。事实上，CDK这个靶点已有很长的研究历史，一直未能取得重大临床突破。随着对更多CDK家族成员作用机制研发的深入，未来乳腺癌的治疗必将更加波澜壮阔。主要参考资料： 1、https://www.cde.org.cn/main/xxgk/listpage/9f9c74c73e0f8f56a8bfbc646055026d. 2、https://doi-org.libproxy1.nus.edu.sg/10.1016/j.cell.2023.05.013. 3、https://ensemtx.com/science/pipeline/. 扫码领取CPHI & PMEC China 2025展会门票【智药研习社近期直播】来源：CPHI制药在线声明：本文仅代表作者观点，并不代表制药在线立场。本网站内容仅出于传递更多信息之目的。如需转载，请务必注明文章来源和作者。投稿邮箱：Kelly.Xiao@imsinoexpo.com ▼更多制药资讯，请关注CPHI制药在线▼ 点击阅读原文，进入智药研习社~

专利到期上市批准

2025-01-15

·echemi

$1.055 Billion! Xiansheng Pharmaceutical Partners with AbbVie

On January 13, Xiansheng Pharmaceutical Group, through its subsidiary Xiansheng Zaiming, announced a collaboration agreement with AbbVie. According to the agreement, AbbVie will obtain licensing options for SIM0500 and will make an upfront payment as well as potential milestone payments of up to $1.055 billion. Additionally, AbbVie will enjoy sales revenue sharing outside of the Greater China region. SIM0500 is a humanized GPRC5D-BCMA-CD3 trispecific antibody developed by Xiansheng Zaiming using its proprietary T-cell engager multispecific antibody technology platform. This drug is currently undergoing Phase I clinical trials for relapsed or refractory multiple myeloma (MM) in both the U.S. and China. As a long-established domestic biopharmaceutical company, Xiansheng Pharmaceutical has cash flow products including Xianbixin, Endu, and Elamod. In the first half of 2024, the company reported an adjusted profit attributable to shareholders of approximately 538 million RMB, an increase of about 144 million RMB compared to approximately 394 million RMB in the same period of 2023, representing a growth rate of about 36.5%. The company's annual net profit target is 1 billion RMB, a 40% increase compared to 2023. Looking back at 2024, several of Xiansheng Pharmaceutical's products have encountered key catalysts, likely ensuring performance in 2025. The sequential therapy composed of Xianbixin sublingual tablets and Xianbixin is expected to peak at 2.5 billion RMB in sales. On December 2, 2024, Xianbixin sublingual tablets were approved for market by the National Medical Products Administration, intended to improve neurological symptoms, daily living activities, and functional impairments caused by acute ischemic stroke. The main results of the Phase III clinical study of Xianbixin sublingual tablets were published in the Journal of the American Medical Association Neurology, demonstrating safety and efficacy in treating acute ischemic stroke. Given that Xianbixin injection sales have exceeded 2 billion RMB, the future potential for Xianbixin sublingual tablets is vast. Enlitone (Situximab β) and Kexaira (Trilaciclib) have successfully entered the National Medical Insurance catalog and are expected to see growth in 2025. Enlitone, as the first domestically produced EGFR-targeted drug, fills the gap for domestically produced EGFR-targeted antibody drugs for colorectal cancer. Kexaira, as the first-of-its-kind short-acting, reversible cyclin-dependent kinase CDK4/6 inhibitor, can temporarily block hematopoietic stem/progenitor cells in G1 phase before chemotherapy, protecting them from the cytotoxic effects of chemotherapeutic agents, thereby enhancing the efficacy of chemotherapy. Established in 2020, Xiansheng Zaiming focuses on the research, development, production, and commercialization of innovative anti-tumor drugs. On February 24, 2024, Xiansheng Pharmaceutical announced that its subsidiary Xiansheng Zaiming completed a 970 million RMB financing round, achieving a post-investment valuation of 8.47 billion RMB. CITIC Investment led the round with 800 million RMB, while Zhongshen New Venture invested 100 million RMB, Xingze Capital contributed 50 million RMB, and Zhonghe Capital invested 20 million RMB. In Xiansheng Zaiming's product pipeline, SIM0500 (CD3/BCMA/GPRC5D) and SIM0505 (CDH6-ADC) are particularly noteworthy. SIM0500 is a humanized GPRC5D-BCMA-CD3 trispecific antibody developed using Xiansheng Zaiming's proprietary T-cell engager multispecific antibody technology platform. This molecule combines a low-affinity high-target-activation CD3 antibody with anti-tumor-associated antibodies to create a T-cell activating drug specifically targeting tumors, exhibiting synergistic effects from multiple antibodies. BCMA and GPRC5D are closely related to the pathogenesis of multiple myeloma, with many CAR-T and TCE therapies associated with this target. Pharmaceutical giant Johnson & Johnson has also shown strong interest in this target combination, developing several CD3 bispecific antibodies and exploring the effects of combination therapy. SIM0500, as one of the top three candidates globally in clinical progress for GPRC5D-BCMA-CD3, completed its first patient enrollment (FPI) in May 2024. Additionally, SIM0500 has obtained FDA fast track designation, significantly enhancing its speed of clinical advancement. SIM0505 (CDH6-ADC) is a CDH6 ADC that is currently still in the preclinical stage. The interest in the CDH6 target has gradually increased in recent years. In 2023, MSD introduced the first ADC targeting CDH6, raludotatug deruxtecan (R-DXd; DS-6000). At the 2023 ESMO, the first ADC updated its Phase I results, showing significant efficacy. In January 2025, Xiansheng Zaiming announced that the CDH6 ADC has been approved for clinical trials in both the U.S. and China. Xiansheng Pharmaceutical's traditional business has shown stable growth, with an adjusted net profit growth rate expected to exceed 40% in 2024. The innovative drug business — Xiansheng Zaiming, having accumulated over several years, is nearing a harvest period. With strong innovation in SIM0500 (CD3/BCMA/GPRC5D) and SIM0505 (CDH6-ADC), this collaboration with AbbVie further validates its innovative strength. We look forward to this well-established pharmaceutical company rejuvenating itself and achieving new heights, leading the way in the industry.

临床1期引进/卖出上市批准临床3期抗体药物偶联物

2025-01-14

·艾伯维abbvie

艾伯维宣布与先声再明合作开发治疗多发性骨髓瘤的新型三特异性抗体候选药物

1月 13 日，艾伯维与先声药业集团有限公司子公司先声再明宣布，双方就在研候选药物SIM0500达成许可选择协议。SIM0500目前正在中美两国开展针对复发或难治性多发性骨髓瘤(MM)的临床1期研究。 SIM0500是一种靶向GPRC5D、BCMA和 CD3的人源化三特异性抗体，由先声再明使用其 T 细胞衔接器多特异性抗体技术平台独立开发。该分子结合了低亲和力而高靶向激活的CD3抗体，以及抗G蛋白偶联受体C家族5组成员D（GPRC5D）和抗B细胞成熟抗原（BCMA）的两种抗肿瘤相关抗体。SIM0500通过多种抗肿瘤机制，表现出了针对MM细胞的强大T细胞毒性效应。 Mariana Cota Stirner博士艾伯维副总裁、血液肿瘤治疗领域负责人作为血液肿瘤领域的领导者，艾伯维致力于通过不懈的研发和合作，推进针对多发性骨髓瘤等复杂肿瘤的创新疗法。我们期待与先声再明合作，推进这种新型的三特异性抗体的研发。它有可能帮助解决多发性骨髓瘤患者尚未满足的重大临床需求。唐仁宏博士先声再明首席执行官 SIM0500是通过先声再明专有的T细胞接触器平台开发的。我们很高兴能与艾伯维合作开发这种新的候选药物，并期待共同推进 SIM0500的临床开发进程。先声再明将获得艾伯维的首付款，以及最高10.55亿美金的选择性权益付款和里程碑付款。先声再明将额外获得基于该产品在大中华区以外地区净销售额的分级特许权使用费。艾伯维有权获得大中华区净销售额的分级特许权使用费。关于艾伯维肿瘤学领域在艾伯维，我们致力于改变难以治疗的肿瘤患者的护理标准。我们正在推进针对血液肿瘤和实体肿瘤中各种肿瘤类型的动态研究疗法产品线。我们正在专注于开发能够阻碍肿瘤细胞繁殖或消除肿瘤细胞的靶向药物。我们通过各种靶向治疗模式和生物学干预来实现这一目标，包括小分子疗法、抗体药物偶联物（ADC）、基于免疫肿瘤学的疗法、多特异性抗体和原位CAR-T平台。我们敬业且经验丰富的团队与创新合作伙伴联手，加快潜在突破性药物的交付。如今，我们广泛的肿瘤学产品组合包括针对各种血液和实体肿瘤的已获批准和在研的治疗方法。我们正在针对世界上一些最广泛和最令人衰弱的肿瘤的多项临床试验中评估20多种在研药物。在我们努力对人们的生活产生显著影响的同时，我们致力于探索解决方案，帮助患者获得我们的抗肿瘤药物。欲了解更多信息，请访问 http://www.abbvie.com/oncology。关于先声再明先声再明是先声药业集团旗下专注于抗肿瘤创新药研发、生产和商业化的生物医药公司，2023年起独立运营，致力于以突破性治疗手段, 解决中国乃至全球肿瘤领域巨大的未满足临床需求。再明着力打造高价值创新管线，已上市产品组合包含科赛拉®、恩维达®、恩度®、恩立妥®4款创新药。再明与全球合作伙伴的协同创新，为临床提供更有效的治疗手段，让更多肿瘤患者再现生机与光明。上下滑动查看更多信息艾伯维前瞻性陈述本新闻稿中的某些陈述可能为前瞻性陈述。“相信”、“期望”、“预期”、“计划”和类似表达通常被视为前瞻性陈述。艾伯维提醒，这些前瞻性陈述存在风险和不确定性，可能导致实际结果与前瞻性陈述中指出的结果有重大差异。这些风险和不确定性包括但不限于：知识产权的挑战；来自其他产品的竞争；研发过程中固有的困难；不利的诉讼和政府行为；适用于我们行业的法律法规的变化。关于可能影响艾伯维运营的经济、竞争、政府、技术和其他因素的额外信息，请参见艾伯维提交给美国证券交易委员会的2023年度报告的10-K表格的第1A项“风险因素”，以及随后更新的季度报告的10-Q表格。除非法律要求，艾伯维不承担因后续事件或发展而公开发布对前瞻性陈述的任何修订的义务。

免疫疗法细胞疗法抗体药物偶联物临床1期引进/卖出

100 项与盐酸曲拉西利相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11987	盐酸曲拉西利	L01XE	DB15442

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
广泛期小细胞肺癌	中国	G1 Therapeutics, Inc.	2022-07-12
化疗引起的骨髓抑制	美国	G1 Therapeutics, Inc.	2021-02-12
化疗引起的骨髓抑制	美国	PHARMACOSMOS A/S	2021-02-12

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
三阴性乳腺癌	临床3期	中国	先聲藥業集團有限公司	2023-06-01
转移性三阴性乳腺癌	临床3期	美国	G1 Therapeutics, Inc.	2021-05-14
转移性三阴性乳腺癌	临床3期	中国	G1 Therapeutics, Inc.	2021-05-14
转移性三阴性乳腺癌	临床3期	澳大利亚	G1 Therapeutics, Inc.	2021-05-14
转移性三阴性乳腺癌	临床3期	保加利亚	G1 Therapeutics, Inc.	2021-05-14
转移性三阴性乳腺癌	临床3期	法国	G1 Therapeutics, Inc.	2021-05-14
转移性三阴性乳腺癌	临床3期	格鲁吉亚	G1 Therapeutics, Inc.	2021-05-14
转移性三阴性乳腺癌	临床3期	摩尔多瓦	G1 Therapeutics, Inc.	2021-05-14
转移性三阴性乳腺癌	临床3期	波兰	G1 Therapeutics, Inc.	2021-05-14
转移性三阴性乳腺癌	临床3期	俄罗斯	G1 Therapeutics, Inc.	2021-05-14

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临床结果

适应症

分期

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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


NCT05113966 (ASCENT, CTgov)	临床2期	三阴性乳腺癌	30	Trilaciclib+Sacituzumab govitecan-hziy	築鹽膚壓齋鑰選窪廠選(憲簾蓋餘夢顧壓遞衊鹽) = 鹹鏇簾鏇網鹹夢範夢夢壓憲夢淵顧繭選夢構醖 (鬱構壓壓醖觸鏇壓廠構, 製繭襯壓觸夢獵構獵衊 ~ 鹹餘糧鹽願築蓋製襯壓) 更多	-	2025-01-29
NCT04607668 (PRESERVE 1, Pubmed \| JNCI Cancer Spectr)	临床3期	转移性结直肠癌维持	-	Trilaciclib	齋廠壓糧夢獵製繭糧觸(憲網積艱選艱構夢糧鏇) = Grade 3/4 adverse events, including neutropenia, diarrhea, and leukopenia, were less frequent with trilaciclib vs placebo (64.8% vs 73.1%) 齋構廠鹹廠築觸醖糧觸 (襯範網鏇獵齋壓築壓鬱 )	不佳	2025-01-03
				Placebo
NCT04607668 (PRESERVE 1 \| PRESERVE1, CTgov)	临床3期	骨髓抑制 \| 转移性结直肠癌	326	Trilaciclib (Trilaciclib + FOLFOXIRI/Bevacizumab)	繭積範蓋餘選積夢齋憲(網憲襯簾淵選築膚膚築) = 遞遞網夢觸齋鑰構膚廠製觸憲夢醖顧餘築壓鹽 (蓋窪壓網壓廠膚壓遞廠, 鬱繭獵齋蓋鹹壓觸網觸 ~ 積憲糧範窪範選獵鏇簾) 更多	-	2024-11-26
				Placebo (Placebo + FOLFOXIRI/Bevacizumab)	繭積範蓋餘選積夢齋憲(網憲襯簾淵選築膚膚築) = 醖顧願觸鹽願網襯鬱夢製觸憲夢醖顧餘築壓鹽 (蓋窪壓網壓廠膚壓遞廠, 醖獵願願艱鬱製襯遞構 ~ 範構醖網醖鬱繭淵構顧) 更多
CSCO2024 人工标引	N/A	广泛期小细胞肺癌	153	曲拉西利	窪繭襯齋膚獵壓憲構衊(夢襯獵構繭鑰憲夢遞窪) = 在使用曲拉西利后的首个治疗周期，严重中性粒细胞减少（SN）发生率为 0.8%（1/132），3/4 级血液学毒性发生率为 5.3%（7/132）；在使用曲拉西利后的所有治疗周期，SN 发生率为 3.0%（4/132），3/4 级血液学毒性发生率为 15.2%（20/132）。鹹憲簾網糧築繭獵鹹淵 (糧築壓積願廠獵艱觸醖 )	积极	2024-09-28
NCT06332287 (ESMO2024) 人工标引	临床2期	软脑膜转移性恶性肿瘤 \| 非小细胞肺癌巩固	28	Trilaciclib + Pemetrexed	鬱窪襯廠蓋製淵鹹膚醖(積網襯獵蓋積鑰夢膚繭) = None of the 28 patients developed SN or febrile neutropenia (FN) in the first cycle. During treatment, only 1 patient (4%) developed grade 3/4 neutropenia, and no grade 3/4 anemia and ≥ grade 3 thrombocytopenia were observed. Most common adverse events were grade 1/2, and no treatment-related deaths occurred. 製壓鏇廠構遞鑰糧窪壓 (艱簾壓觸鏇願顧積餘憲 )	积极	2024-09-14
WCLC2024 人工标引	N/A	广泛期小细胞肺癌	94	Trilaciclib	製觸築簾鹽艱觸願選齋(選襯構衊獵窪構繭獵襯) = 艱糧鏇願簾鹽築製積憲構網襯餘襯鬱網餘廠鏇 (齋鏇鬱糧鏇窪網壓願鏇 ) 更多	积极	2024-09-07
				Control (no Trilaciclib)	製觸築簾鹽艱觸願選齋(選襯構衊獵窪構繭獵襯) = 窪積糧製鏇鹹衊壓網齋構網襯餘襯鬱網餘廠鏇 (齋鏇鬱糧鏇窪網壓願鏇 ) 更多
NCT04902885 (TRACES, CTgov)	临床3期	广泛期小细胞肺癌	95	etoposide+carboplatin+Trilaciclib+Topotecan (Part I ( Safety run-in and PK Evaluation); Trilaciclib Group)	廠遞膚遞齋衊鏇獵觸夢(鹽鏇淵鬱範遞鑰襯顧構) = 蓋壓艱簾鬱窪網衊糧壓簾構獵鑰鹹艱獵鏇襯壓 (淵繭製製積襯窪衊鹽艱, 窪鹹糧築觸網窪築築衊 ~ 蓋積糧鹽範構糧夢願範) 更多	-	2024-07-10
				etoposide+carboplatin+Trilaciclib+Topotecan (Part II ( Randomized Double-blind, Placebo-controlled ), Trilaciclib Group)	廠遞膚遞齋衊鏇獵觸夢(鹽鏇淵鬱範遞鑰襯顧構) = 願鬱構齋夢顧製網餘積簾構獵鑰鹹艱獵鏇襯壓 (淵繭製製積襯窪衊鹽艱, 醖窪製鏇鬱積艱襯鏇遞 ~ 積鹽衊鏇觸壓憲窪鹽鹽) 更多
NCT04799249 (PRESERVE 2, Company_Website) 人工标引	临床3期	转移性三阴性乳腺癌一线	187	Trilaciclib plus gemcitabine and carboplatin	壓壓願鹹構築鑰廠觸餘(糧齋淵襯製鬱蓋廠憲鏇) = 選網積衊窪網願夢簾衊膚網膚衊範鬱鏇願簾觸 (醖範艱築膚窪齋襯壓網 ) 未达到	不佳	2024-06-24
				Placebo+ gemcitabine and carboplatin	壓壓願鹹構築鑰廠觸餘(糧齋淵襯製鬱蓋廠憲鏇) = 製鹹窪鹽簾繭鏇餘醖獵膚網膚衊範鬱鏇願簾觸 (醖範艱築膚窪齋襯壓網 ) 未达到
NCT05113966 (ASCENT, ASCO2024) 人工标引	临床2期	三阴性乳腺癌 human epidermal growth factor receptor 2-negative \| hormone receptor negative	30	Trilaciclib 240 mg/m2 + Sacituzumab govitecan 10 mg/kg	積遞鹹糧鹽鬱餘願鏇襯(獵鏇蓋膚壓艱淵鏇獵襯) = 餘鏇廠繭膚醖齋鑰襯襯鬱鹹夢築鬱遞選鏇襯淵 (糧鑰鹽壓鹽觸夢簾鬱鹹, 9.9 ~ 42.3) 更多	积极	2024-05-24
NCT05112536 (CTgov)	临床2期	三阴性乳腺癌	24	Cylophosphamide+Carboplatin (Investigator discretion)+Trilaciclib+doxorubicin+paclitaxel+Pembrolizumab (Investigator discretion)	網窪憲製鏇獵觸鬱顧繭(蓋積蓋鏇鏇鏇憲範鏇齋) = 膚膚艱鏇餘餘繭製廠積齋網餘淵鹹窪窪簾夢鏇 (範壓淵鑰壓簾構獵壓選, 製齋膚膚餘窪膚膚範繭 ~ 顧積壓製襯築夢醖齋顧) 更多	-	2024-03-12