详细介绍

Trastuzumab (Synonyms: 曲妥珠-单抗; Anti-Human HER2, Humanized Antibody)

Trastuzumab 是一种人源化 IgG1 单克隆抗体，其以高亲和力与 HER2 选择性结合。Trastuzumab 可用于 HER2 阳性转移性乳腺癌和 HER2 阳性胃癌的研究。

生物活性

Trastuzumab is a humanized IgG1 monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has the potential for HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer research.

IC₅₀ & Target^[1]

HER2

体外研究(In Vitro)

Treatment of HER2-overexpressing breast cancer cell lines with Trastuzumab results in induction of p27KIP1 and the Rb-related protein, p130, which in turn significantly reduces the number of cells undergoing S-phase. A number of other phenotypic changes are observed in vitro as a consequence of Trastuzumab binding to HER2-overexpressing cells. Interaction of Trastuzumab with the human immune system via its human immunoglobulin G1 Fc domain may potentiate its antitumor activities. in vitro studies demonstrate that Trastuzumab is very effective in mediating antibody-dependent cell-mediated cytotoxicity against HER2-overexpressing tumor targets^[1]. Trastuzumab consists of two antigen-specific sites that bind to the juxtamembrane portion of the extracellular domain of the HER2 receptor and that prevent the activation of its intracellular tyrosine kinase. Trastuzumab recruits immune effector cells that are responsible for antibody-dependent cytotoxicity^[2]. The presence of Trastuzumab IgG significantly increases killing of all breast cancer cell lines. The ADCC activity of PBMCs evoked by Trastuzumab is equally strong against Trastuzumab-sensitive (SKBR-3) or Trastuzumab-resistant (JIMT-1) breast cancer cells, with dose-dependent cell death reaching 50–60% killing at an effector/target ratio of 60:1^[3].

体内研究(In Vivo)

Trastuzumab treatment of mouse xenograft models results in marked suppression of tumor growth. When given in combination with standard cytotoxic chemotherapeutic agents, Trastuzumab treatment generally results in statistically superior antitumor efficacy compared with either agent given alone^[1]. Trastuzumab causes a significant growth inhibition of the outgrowth of macroscopic JIMT-1 xenograft tumors in both nude and SCID mice^[3].

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04158258	Hoffmann-La Roche\|Latin American Cooperative Oncology Group	Breast Cancer	February 21, 2020
NCT02774681	Northwestern University\|Pfizer\|National Cancer Institute (NCI)	Breast Carcinoma Metastatic in the Brain\|Estrogen Receptor Negative\|HER2+Neu Negative\|HER2+Neu Positive\|Progesterone Receptor Negative\|Recurrent Breast Carcinoma\|Stage IV Breast Cancer	August 31, 2016	Phase 2
NCT03493854	Hoffmann-La Roche	Early Breast Cancer	June 14, 2018	Phase 3

分子量：145531.50

Formula：C₆₄₇₀H₁₀₀₁₂N₁₇₂₆O₂₀₁₃S₄₂

CAS 号：180288-69-1

中文名称：曲妥珠-单抗；曲妥-单抗；群司珠-单抗

储存方式;Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Sliwkowski MX, et al. Nonclinical studies addressing the mechanism of action of trastuzumab. Semin Oncol. 1999 Aug;26(4 Suppl 12):60-70.
[2]. Hudis CA, et al. Trastuzumab--mechanism of action and use in clinical practice. N Engl J Med. 2007 Jul 5;357(1):39-51.
[3]. Barok M, et al. Trastuzumab causes antibody-dependent cellular cytotoxicity-mediated growth inhibition of submacroscopic JIMT-1 breast cancer xenografts despite intrinsic drug resistance. Mol Cancer Ther. 2007 Jul;6(7):2065-72.

注：产品仅用于科研

产品简介

详细介绍

Trastuzumab (Synonyms: 曲妥珠-单抗; Anti-Human HER2, Humanized Antibody)