Drug Database
TR

trastuzumab (Saituo / TQB211 / TQ B211)

✓ Approved

Sino Biopharmaceutical Co., Ltd · ERBB2 · 单克隆抗体

什么是 trastuzumab?

trastuzumab 是一种单克隆抗体,由Sino Biopharmaceutical Co., Ltd研发。该药已获批,用于治疗相关适应症,给药途径:Injectable (Others)、Intravenous (IV)。

药物档案

商品名Saituo, TQB211, TQ B211
公司Sino Biopharmaceutical Co., Ltd
药物类别单克隆抗体, 抗体
分子靶点ERBB2
给药途径Injectable (Others), Intravenous (IV)
状态Approved

作用机制

分子靶点

trastuzumab 作用于 1 个分子靶点:

ERBB2erb-b2 receptor tyrosine kinase 2 (NEU, CD340)
需要更深入的分析?Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

trastuzumab 针对 3 个适应症,涉及 1 个治疗领域。

治疗领域疾病/病症分期
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Breast cancer✓ Approved
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Gastric cancer✓ Approved
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Oesophageal carcinomaPreclinical

相关研究文献

PubMedAntibodies (Basel, Switzerland)2026-10-26

Complement in HER2-Positive Breast Cancer: A Conditionally Protective Mechanism Under Attack.

Petkova Dobromira D, Kuleva Ivaila I, Stoyanova Zhasmin Z, Ilcheva Boryana B et al.

The therapeutic efficacy of anti-HER2 monoclonal antibodies in breast cancer has traditionally been attributed to direct inhibition of signaling and antibody-dependent cellular cytotoxicity (ADCC). Recent evidence, however, has established complement activation through the classical pathway as a possible adjunct mechanism underlying the synergistic activity of the trastuzumab and pertuzumab combination. This synergy is mediated by complement-dependent cytotoxicity (CDC) and complement-dependent cellular phagocytosis (CDCP), and is lost upon C1q deletion in preclinical models. Tumor cells evade complement-mediated killing through overexpression of membrane-bound complement regulatory proteins (mCRPs), particularly CD55 and CD59, which correlate with shorter disease-free survival in patients treated with trastuzumab. C1q itself plays a dual, context-dependent role: it acts as a complement-independent tumor suppressor in HER2-positive breast cancer while promoting tumor progression in most other malignancies. Emerging therapeutic strategies, including biparatopic antibodies such as zanidatamab, complement-redirecting immunoconjugates, and mCRP-targeting approaches, aim to overcome complement resistance and enhance antitumor immunity. On this basis, we propose that HER2-positive breast cancer represents a conditionally complement-protective tumor, in which the balance between antibody-directed complement activation and mCRP-mediated evasion determines treatment outcome. This review evaluates the current evidence linking complement to anti-HER2 therapy and highlights future directions for successful treatment.

PMID 42930033
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PubMedMolecular cancer therapeutics2026-10-26

Preclinical modeling of trastuzumab deruxtecan in a mouse model of brain metastatic triple-negative breast cancer identifies two contributors to efficacy.

Khan Imran I, Kumar Dinesh D, Difilippantonio Simone S, Robinson Christina C et al.

Trastuzumab deruxtecan (T-DXd) has demonstrated clinical efficacy in advanced HER2-low to -ultralow breast cancer. We employed a mouse model of triple-negative breast cancer in the difficult-to-treat brain metastasis setting to determine T-DXd efficacy and investigate mechanism(s). T-DXd (10 and 3 mg/kg) was compared to an identical ADC except HER2-nonbinding (control) in a hematogenous model of HER2-ultralow brain-tropic triple-negative breast cancer, MDA-MB-231-BR7 (231-BR). The roles of HER2 and the neonatal Fc receptor (FcRn) were determined by CRISPR-Cas9 deletion and shRNA knockdown, respectively. 231-BR cells exhibited HER2 0+ staining, with occasional membrane expression. T-DXd at 10 mg/kg reduced 231-BR brain metastases by 49% (P=0.002), while a dose reduction showed a 30% (ns) metastasis reduction, each compared to the control-ADC. HER2-specific and -nonspecific ADC uptake into metastases was accompanied by a 23-47% tumor cell Ki-67 decline, and 5-fold increase in tumor apoptosis. A HER2 CRISPR-Cas9 knockout 231-BR formed multiple brain metastases but was insensitive to T-DXd in vivo. 231-BR tumor cells expressed FcRn, potentially enabling nonspecific ADC uptake. Analysis of human tumors showed TNBC tumors expressed FcRn mRNA. T-DXd failed to inhibit brain metastases in two 231-BR FcRn knockdown clones compared to a 231-BR clone transduced with a scrambled shRNA where T-DXd inhibited brain metastases (67% reduction, P=0.01). Despite ultralow HER2 expression, the HER2 binding capacity of T-DXd is a significant contributor to its efficacy. Breast cancers variably express FcRn, suggesting that nonspecific tumor cell uptake of T-DXd via FcRn is also a potential mechanism of T-DXd action.

PMID 42929047
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PubMedCurrent oncology (Toronto, Ont.)2026-10-26

A New Era of Treatment Sequencing in Platinum-Resistant Ovarian Cancer: Integrating Immunotherapy, Antibody-Drug Conjugates, and Targeted Therapies.

Mabuchi Seiji S, Kusakabe Ai A, Takimoto Yumi Y

Platinum-resistant ovarian cancer (PROC) has historically been treated with sequential non-platinum chemotherapy, with bevacizumab added when appropriate. The therapeutic landscape has expanded with positive randomized phase III data for pembrolizumab plus weekly paclitaxel with or without bevacizumab (KEYNOTE-B96), mirvetuximab soravtansine (MIRV) in FRα-high disease (MIRASOL), and relacorilant plus nab-paclitaxel (ROSELLA). Trastuzumab deruxtecan (T-DXd) has also shown substantial activity in previously treated HER2-expressing ovarian cancer, although its ovarian cohort was small, nonrandomized, and not restricted to PROC. These trials enrolled different populations and do not establish a cross-trial efficacy hierarchy. We therefore review the development of immunotherapy leading to KEYNOTE-B96, compare newer strategies with established PROC treatments, distinguish phase III evidence from regulatory approval and routine availability, and propose an evidence-informed framework for treatment selection and sequencing. The framework prioritizes current treatment opportunity while accounting for biomarker eligibility, prior treatment, residual toxicity, treatment and financial burden, patient priorities, and the feasibility of later-line therapy.

PMID 42930189
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PubMedBiotech (Basel (Switzerland))2026-10-26

Pharmaceutical Residues in Human Urine from Patients Under Antiretroviral Regimens and Self-Reported Healthy Individuals Before and After Three Months' Storage: Implication for Agricultural Reuse in Pretoria, South Africa.

Lizbelt Mugivhisa Liziwe ML, Faith Baloyi Khanyi BK, Oladeji Oluwaseun Mary OM, Olatunji Olatunde Stephen OS et al.

Background/Objectives: Pharmaceutical residues in human urine have raised serious concerns about the safe reuse of urine in agriculture. The current study investigates and compares the concentrations of pharmaceuticals in urine samples collected from male patients undergoing active antiretroviral regimens and self-reported "healthy individuals" at a government hospital in Pretoria, South Africa, and determines how the residues changed during three months of ambient storage, which is the usual recommendation before use in agriculture. Methods: The urine samples were collected in a plastic bottle to prevent fecal contamination, and 15 targeted compounds were analyzed using solid-phase extraction and liquid chromatography-mass spectrometry. The linearity ranged from 0.9910 to 0.9999, 75.5% to 99.1% for recovery, and intra-day and inter-day precision were below 6%. The urine from each group was collected into one pooled sample and then analyzed both pre- and post-storage. Results: Thirteen pharmaceuticals were detected in urine from patients on regular medication before storage; in "healthy individuals", detections rose from eight to twelve after storage. Concentrations in the composite samples after storage were higher for some of the compounds but lower for others, including caffeine, nevirapine, prednisolone and 17α-ethinylestradiol. Metformin was highest overall at 1186.25 µg/L and remained at 806.68 µg/L after storage. The highest concentration for all the pharmaceuticals was reported for metformin, with a value of 1186.25 µg/L, occurring in the group of patients on a regular regimen. There could be a possibility that the rise can be attributed to the hydrolysis of conjugated metabolites during storage; however, no analysis of conjugates was carried out. Conclusions: This study shows the need for appropriate treatment of human urine prior to its reuse as fertilizer and echoes the importance of further research into human exposure pathways and effective pharmaceutical removal strategies.

PMID 42930069
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PubMedBiosensors2026-10-26

Porous Transducers and Hybrid Recognition for Bulky Nitrosamine Impurities: Toward 3D-MXene-Aptamer Detection of Tricyclic NDSRIs.

Shah Tirath T, Patel Ankur A, Shah Jignesh J, Shah Darshil D

Pharmaceutical quality control faces an emerging problem with Tricyclic nitrosamine drug substance-related impurities (NDSRIs), for example, N-nitroso clozapine. The impurities preserve the compl ete structure of their parent active pharmaceutical ingredients, which consist of bulky lipophilic molecules with restricted conformational flexibility. The retention of bulky lipophilic structures from the parent active pharmaceutical ingredients in these impurities results in their complete overlap with other substances, which causes matrix ion suppression and weak ionization and unstable mass-spectrometric responses. The LC-MS/MS method functions as the official standard but its workflow requires excessive solvent use and produces complicated equipment systems, which prevent its use for routine ultra-trace monitoring. This narrative review analyzes hybrid electrochemical sensing technology to determine if it can solve the current problem by using tricyclic NDSRIs steric complexity as a functional benefit for detection purposes. The research combines data from nitrosamine detection with studies on porous 3D-printed electrodes, MXene electrochemistry, molecularly imprinted polymers, aptamer engineering and the computational systematic evolution of ligands by exponential enrichment (SELEX), molecularly imprinted polymer (MIP) and signal-off aptasensing. This review presents that planar electrodes create an unfavorable structure for bulky tricyclic analytes because they lead to surface obstruction and increased resistance during charge transfer. This review demonstrates that gyroid and TPMS-type porous scaffolds with a Ti3C2Tx MXene coating offer superior internal surface area, enhanced diffusion channels and accelerated electron movement. The dual MIP-aptamer system enables selective recognition by using MIP to perform shape-based target capture and specimen protection and aptamer to recognize specific molecular targets. The design process for aptamers includes E/Z nitrosamine isomer modeling, docking and molecular dynamics, and AI-based sequence selection methods, which form the core approach to targeting N-nitroso clozapine (N-CZN)-like proteins. This research outlines a new technique, which uses steric hindrance to block redox-probe entry, thus generating an electrical signal through current reduction. This review presents a fundamental operational model which supports the development of eco-friendly portable electrochemical devices to detect tricyclic NDSRIs with maximum sensitivity.

PMID 42930082
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PubMedJournal of chemical information and modeling2026-10-26

Bridging the Markush Gap in Optical Chemical Structure Recognition via a CLIP-Derived Visual Backbone and Synthetic Data Generation.

Huang Qixing Q, Chang Haohua H, Mao Liyun L, Shen Zihao Z et al.

The rapidly growing chemical literature contains invaluable information for pharmaceutical research and molecular biology, yet manual extraction on a large scale is increasingly impractical. Optical chemical structure recognition (OCSR), which converts molecular depictions into machine-readable representations, provides a key route toward automated chemical information extraction. However, existing OCSR methods remain limited in recognizing Markush structures, which are widely used in chemical documents, particularly pharmaceutical patents, because of their structural complexity and the scarcity of annotated data. Here, we introduce CLIP-OCSR, an encoder-decoder framework that integrates a domain-adaptively pretrained CLIP-RN50 vision encoder with a transformer decoder for chemical structure recognition, with a focus on Markush representations. To address data scarcity, we developed a synthetic data generation strategy that produces diverse Markush images paired with pseudo-SMILES representations encoding substituent, frequency, and position variations. Benchmarking demonstrates that CLIP-OCSR achieves competitive performance on standard OCSR benchmarks and shows strong capability in recognizing Markush structures involving substituents and frequency variations. For structures with position variations, CLIP-OCSR generates pseudo-SMILES predictions that retain the corresponding positional information, enabling the downstream enumeration of possible positional isomers. Beyond image-only OCSR, we extend CLIP-OCSR toward multimodal Markush structure extraction by integrating graphical recognition with LLM-based textual variable-definition extraction, enabling downstream structure instantiation. Overall, this work advances automated recognition of complex chemical structures and provides a framework for the structured extraction of Markush information from chemical documents.

PMID 42929585
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