antibody-drug conjugates

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.

Disitamab vedotin (RC48) is an antibody-drug conjugate (ADC) and a HER2-targeted cytotoxic agent, consisting of an anti-HER2 monoclonal antibody conjugated to MMAE via a cleavable linker, used for the treatment of HER2-expressing solid tumors including gastric cancer, breast cancer, and urothelial carcinoma.

Datopotamab deruxtecan (DS-1062) is an antibody-drug conjugate (ADC) that targets tropomyosin 2 (TROP2) on the surface of trophoblast cells. Datopotamab deruxtecan exhibits antitumor activity by specifically binding to TROP2 and internalizing, releasing DXd to inhibit topoisomerase I (IC₅₀ = 0.31 μM), thereby inducing DNA damage and apoptosis. Datopotamab deruxtecan induces significant antibody-dependent cellular cytotoxicity in the presence of peripheral blood lymphocytes and inhibits tumor growth in xenograft models.

Brentuximab vedotin (SGN-35) is a CD30-targeting antibody-active molecule conjugate (ADC) that combines a CD30 monoclonal antibody with the microtubule disrupting agent monomethylauristatin E for the study of lymphoma.

Sacituzumab govitecan (IMMU-132) is a humanized ADC compound targeting Trop-2 with anticancer activity for the study of refractory, locally advanced or metastatic breast cancer and uroepithelial cancer.

Enfortumab vedotin-ejfv (Padcev) is an ADC compound targeting Nectin-4 with anti-tumor activity, used in the study of urothelial carcinoma.

Izeltabart Tapatansine (IMGC-936) is a CHO-expressing humanized next-generation medetonin-based ADC compound targeting ADAM9-expressing tumors, and exhibits cytotoxicity against ADAM9-positive human tumor cell lines for cancer research.

Labetuzumab govitecan is an antibody-drug conjugate (ADC) targeting CEACAM5, composed of the labetuzumab antibody, the payload SN-38, and a pH-sensitive linker. It can be used in research on malignant tumors such as colorectal 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.

Glembatumumab vedotin (CDX-011) is an antibody-drug conjugate (ADC) that targets cancer cells expressing transmembrane glycoprotein NMB (GPNMB). Glembatumumab vedotin has potent anticancer effects and can be used in the study of triple negative breast cancer (TNBC).

Loncastuximab tesirine, a human cluster of differentiation 19 (CD19)-directed antibody-drug conjugate (ADC), binds to CD19 on the cell membrane, facilitating rapid internalization and inducing cell apoptosis. This mechanism makes it a valuable asset in researching diffuse large B-cell lymphoma [1] [2].

Cantuzumab mertansine (SB-408075; huC242-DM1), an antibody-drug conjugate (ADC), comprises the potent maytansine derivative (DM1) linked to the humanized monoclonal antibody (huC242) targeting CanAg. Demonstrating cytotoxicity against colon cancer cells, this compound shows extensive antitumor effectiveness across various CanAg-positive human tumor xenografts [1] [2].

Cantuzumab ravtansine (IMGN242; huC242-DM4), an antibody-drug conjugate (ADC), comprises the humanized monoclonal antibody huC242 covalently bonded through a disulfide linkage to the cytotoxic agent DM4 (DM4), demonstrating extensive antitumor effectiveness across various CanAg-positive human tumor xenografts [1] [2].

Zilovertamab vedotin is a novel antibody-drug conjugate (ADC) constructed by conjugating the humanized monoclonal antibody zilovertamab with the anti-microtubule cytotoxic drug monomethyl vedotin. It binds to ROR1 on the surface of tumor cells, promotes rapid internalization and trafficking of the complex to lysosomes, followed by ADC cleavage and release of monomethyl vedotin, thereby inducing tumor cell apoptosis. It can be used in cancer-related research.

Polatuzumab vedotin, an antibody-drug conjugate, selectively targets CD79b with a humanized anti-CD79b IgG1 monoclonal antibody bound to monomethyl auristatin E (MMAE), a robust microtubule inhibitor. This compound shows promise for research into Large B-cell lymphomas (LBCL) [1].

Telisotuzumab vedotin (ABBV-399) is an ADC compound targeting c-Met with antitumor activity, used for research in recurrent squamous cell lung cancer.

Tisotumab vedotin is an antibody-drug conjugate (ADC) targeting tissue factor (TF), consisting of the fully human monoclonal antibody (TF-011) conjugated with monomethyl auristatin E (MMAE). It exhibits significant antitumor activity and is suitable for research on the treatment of advanced or metastatic solid tumors.

Belantamab mafodotin (GSK2857916) is an antibody-drug conjugate targeting B-cell maturation antigen (BCMA) that enhances immune cell infiltration and activation within tumors and delays tumor growth. It is used in studies of multiple myeloma.

Tusamitamab ravtansine (SAR-408701) is a DM4-linked anti-CEACAM5 antibody-drug conjugate (ADC) comprising a humanized monoclonal antibody targeting carcinoembryonic antigen-related cell adhesion molecule-5 (CEACAM5) conjugated to a cytotoxic maytansinoid, selectively engaging CEACAM5-positive tumor cells [1].

Farletuzumab ecteribulin is an antibody-drug conjugate (ADC) consisting of the humanized antibody farletuzumab, which targets the folate receptor alpha (FRA), with an antibody-to-drug ratio of 4.0. In vitro, farletuzumab ecteribulin exhibits cytotoxic and antitumor activity against FRA-positive cells.

Patritumab deruxtecan (HER3-DXd) is an antibody-drug coupling (ADC) targeting HER3 consisting of a fully humanized anti-HER3 IgG1 monoclonal antibody linked via a cleavable tetrapeptide linker to a topoisomerase I inhibitor payload (an ezetiocan derivative, DXd) for the study of non-small cell lung cancer (NSCLC).

Gemtuzumab ozogamicin is an antibody-drug conjugate (ADC) composed of a CD33-specific monoclonal antibody linked to a cytotoxic agent derived from Calicheamicin, utilized in the investigation of acute myeloid leukemia [1].

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].

Sofituzumab vedotin is an anti-MUC16 antibody-drug conjugate (ADC) containing MMAE and a protease-cleavable linker, which can be used in cancer research.