trastuzumab

Trastuzumab is a humanized monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has been clinically used to treat HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer.

Trastuzumab duocarmazine ((vic)-Trastuzumab duocarmazine) is an ADC targeting HER2, cleaved by histone B within tumor cells for selective targeting, exhibiting antitumor activity and applicable in cancer research, particularly for uterine and ovarian sarcomas [1].

Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody–drug conjugate that combines the HER2-targeted antitumor specificity of trastuzumab with the potent cytotoxic activity of the microtubule inhibitor DM1, Trastuzumab emtansine enables selective intracellular delivery of the cytotoxic payload to HER2-expressing cells and supporting translational and mechanistic research in advanced breast cancer models.

Trastuzumab beta (ABP 980), a biosimilar to Trastuzumab, is a monoclonal antibody (McAb) that targets the human epidermal growth factor receptor 2 (HER2). It is utilized in the research of HER2-positive metastatic breast cancer, early breast cancer (EBC), and metastatic gastric cancer [1].

Trastuzumab MMAE is an antibody-drug conjugate (ADC) that combines a HER2-targeted antibody with Monomethyl auristatin E (MMAE), utilized in breast cancer research.

Trastuzumab rezetecan (SHR-A1811) is an antibody-drug conjugate (ADC) targeting HER2. It is composed of a humanized anti-HER2 antibody, a cleavable linker MC-Gly-Gly-Phe-Gly, and an effective payload of the topoisomerase I inhibitor Rezetecán. Trastuzumab rezetecan is utilized in the research of HER2-positive breast cancer.

Trastuzumab envedotin (DP303c) is an antibody-drug conjugate (ADC) targeting the human epidermal growth factor receptor 2 (HER2). It consists of the anti-HER2 antibody DP001 linked to the microtubule polymerization inhibitor MonomethylauristatinE (MMAE) through a cleavable linker. This compound is utilized in research involving HER2-positive solid tumors such as breast cancer, colorectal cancer, and gastric cancer.

Timigutuzumab (GEXMab73) is a glyco-optimized monoclonal antibody targeting the human epidermal growth factor receptor 2 (ErbB2/HER2). Through glyco-engineering (typically afucosylation), the antibody's Fc region exhibits enhanced binding affinity for the FcγRIIIa receptors on immune effector cells, such as natural killer (NK) cells. This optimization significantly boosts Antibody-Dependent Cell-mediated Cytotoxicity (ADCC), enabling potent tumor cell lysis even in cases with low HER2 expression levels. Timigutuzumab is designed to overcome resistance to conventional anti-HER2 therapies and provide an improved therapeutic option for solid tumors.

Trastuzumab deruxtecan (T-DXd) is an antibody-active molecule conjugate (ADC) with anticancer and antitumor activity, which is composed of a monoclonal antibody targeting human epidermal growth factor receptor 2 (HER2) coupled to a topoisomerase I inhibitor (DXd). Trastuzumab deruxtecan has an improved effect on the treatment of HER2-positive breast cancer and gastric cancer.

Anbenitamab (KN-026) is a novel Fc-fused bispecific antibody targeting the human epidermal growth factor receptor 2 (HER2). It simultaneously binds to two non-overlapping extracellular domain epitopes of HER2 (domain IV, targeted by trastuzumab, and domain II, targeted by pertuzumab). This biparatopic binding mode induces superior receptor clustering and rapid degradation, leading to potent inhibition of downstream signaling pathways such as MAPK and PI3K. Anbenitamab demonstrates significant anti-tumor activity in HER2-positive or low-expressing breast, gastric, and gastroesophageal junction cancers, and effectively mediates antibody-dependent cellular cytotoxicity (ADCC).

MAB802 (MRG002 antibody) is a recombinant humanized anti-HER2 monoclonal antibody. It shares the same amino acid sequence as Trastuzumab but is highly fucosylated. The antibody-dependent cell-mediated cytotoxicity (ADCC) activity of MAB802 is comparatively lower. MAB802 is employed as the antibody component in the antibody-drug conjugate Trastuzumab vedotin (MRG002).

HLX-22 is a humanized monoclonal antibody targeting HER2. When used in combination with trastuzumab, HLX-22 can induce apoptosis in HER2-overexpressing breast and gastric cancer cells. It also exhibits potent antitumor activity against advanced solid tumors.

BI-1607 is a humanized monoclonal antibody targeting CD32b/FcγRIIB. It acts as an antagonist, capable of blocking the inhibitory effects of FcγRIIB on immune effector cells. When used in combination with Trastuzumab, BI-1607 can significantly suppress HER2-positive solid tumors, including advanced gastric cancer (GC).