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 deruxtecan (T-DXd) is an antibody-drug conjugate functioning as a HER2-targeted topoisomerase I inhibitor, with targeting capability and antitumor activity, employed in research on HER2-positive breast cancer and gastric cancer.

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.

Timigutuzumab 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 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-MMAE-DXd is an ADC composed of an antibody targeting HER2, combined with Monomethyl auristatin E (MMAE) and deruxtecan (DXd), and is used in the research of breast cancer.

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.

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 = 650 nM). It inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome, displaying low-nM to sub-nM IC50s. Thailanstatin A, as a payload for ADCs, is conjugated to the lysines on trastuzumab, yielding linker-less ADC.

m-PEG4-Br is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADC) for Trastuzumab, positioned distally from the monomethyl auristatin E (MMAE) payload to produce an ADC with modified hydrophilicity, antigen binding, and in vitro potency[1].

Maleimido-tri(ethylene glycol)-propionic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs) for the preparation of neolymphostin-based ADC precursors, specifically for site-specific cysteine mutant trastuzumab-A114C conjugation[1].

LacNAc-VC-PAB-MMAE is a component of an antibody-drug conjugate (ADC). It is assembled onto the N-glycosylation site of Trastuzumab through WT Endo-S2.

SNX631 is a potent and highly selective CDK8/19 mediator kinase inhibitor with an IC₅₀ of 10.3 nM in NF-κB-dependent cellular assays. Its activity is 6–10 times higher than that of Senexin B in all assays except DiscoverX active site-dependent competitive binding experiments. SNX631 exerts synergistic effects with lapatinib and trastuzumab in multiple HER2-positive breast cancer cell lines, reversing and preventing resistance to HER2-targeted therapy. The combination of trastuzumab (a HER2 monoclonal antibody) and SNX631 inhibits the phosphorylation of STAT1 and STAT3 at the S727 site and upregulates the expression of the tumor suppressor BTG2 in HER2-positive breast cancer cells. SNX631 partially inhibits the growth of lapatinib-sensitive and -resistant HER2-positive breast cancer xenografts, and its antitumor effect is significantly enhanced when combined with lapatinib, effectively overcoming lapatinib resistance.

IYPTNGYTR acetate, a deamidation-sensitive peptide derived from Trastuzumab, is a suitable tool for monitoring the metabolism of Trastuzumab in vivo [1].

FTISADTSK acetate is a stable endogenous signature peptide sourced from Trastuzumab, which can be monitored using selected reaction monitoring (SRM)[1].

IYPTNGYTR, a deamidation-sensitive peptide, is a deamidation derivative of Trastuzumab. This compound, IYPTNGYTR, can be utilized for monitoring Trastuzumab metabolism in vivo.

FTISADTSK is an endogenous stable signature peptide derived from Trastuzumab, accurately assessed using selected reaction monitoring (SRM).

Anticancer agent 81 (Compound 37b3) induces tumor cell cycle arrest and apoptosis, and serves as a payload for conjugation with Trastuzumab, forming the antibody-drug conjugate (ADC) T-PBA, which retains Trastuzumab's targeting and internalization properties [1].

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).

(Aminooxy)acetamide-Val-Cit-PAB-MMAE (MMAE 5) serves as an intermediate for synthesizing drug-linker conjugates in antibody-drug conjugates (ADCs). The compound is initially conjugated to a polyamide via oxime bond formation, forming an MMAE polyamide conjugate, which is then attached to Trastuzumab to create the ADC [1].

STING agonist-18 is a STING agonist that can be used as a functional module for constructing antibody–drug conjugates (ADCs), for example by conjugation with Trastuzumab, and is applied in studies of cancer immunotherapy.

Rezetecán serves as a precursor for synthesizing Trastuzumab rezetecan, an antineoplastic agent [1].