antibody-drug conjugate

Datopotamab deruxtecan (DS-1062) is a trophoblast cell surface antigen 2 (TROP2)-targeted antibody-drug conjugate (ADC) with antitumor activity. Datopotamab deruxtecan induces significant antibody-dependent cellular cytotoxicity in the presence of peripheral blood lymphocytes and inhibits tumor growth in xenograft models.

Labetuzumab govitecan is an anti-CEACAM5 SN-38 antibody-drug conjugate for therapy of refractory or relapsing metastatic colorectal cancer.

Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that combines the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of DM1, a microtubule-inhibitory derivative of maytansine, and is utilized in the investigation of advanced breast cancer[1][2].

Glembatumumab vedotin (CDX-011) is an antibody-drug conjugate with potent anticancer effects, utilized in the study of triple negative breast cancer (TNBC).

Indusatumab (5F9 Monoclonal antibody) is an anti-human GUCY2C (Guanylate cyclase 2C) monoclonal antibody utilized for synthesizing antibody-drug conjugates.

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].

Mipasetamab, an IgG1κ antibody, targets AXL, a tyrosine kinase receptor and TAM Receptor. It plays a crucial role in synthesizing ADCT-601 (Mipasetamab uzoptirine), an AXL-targeted antibody-drug conjugate (ADC), known for its anti-tumor activity [1].

Zilovertamab vedotin (VLS-101) is a novel antibody-drug conjugate composed of the humanized monoclonal antibody zilovertamab linked to the anti-microtubule cytotoxin monomethyl auristatin E (MMAE). Upon binding to ROR1 on tumor cells, it is rapidly internalized and directed to lysosomes for cleavage, releasing MMAE and inducing apoptosis in targeted cells. Zilovertamab vedotin has potential applications in cancer research [1].

Lorvotuzumab (Anti-NCAM1 CD56 Reference Antibody (lorvotuzumab)) is a humanized monoclonal antibody that binds to CD56 (NCAM1) and can be used to synthesize the antibody-drug conjugate Lorvotuzumab mertansine.

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].

Tisotumab vedotin is an antibody-drug conjugate (ADC) that targets tissue factor (TF), combining a fully human monoclonal antibody against TF (TF-011) with the cytotoxic agent Monomethyl Auristatin E (MMAE), and exhibits potent antitumor activity in advanced or metastatic solid tumors [1].

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.

Vobramitamab, a humanized B7-H3 monoclonal antibody (mAb), is conjugated to the prodrug seco-DUBA through a cleavable linker, creating the antibody-drug conjugate (ADC) known as MGC018 [1].

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 (MORAb-202) is a highly cytotoxic antibody-drug conjugate (ADC) targeting human folate receptor alpha (FRA). This ADC comprises the humanized Farletuzumab antibody linked to Mal-PEG2-Val-Cit-PAB-eribulin through reduced interchain disulfide bonds, with an agent-to-antibody ratio of 4.0, demonstrating potent antitumor activity against FRA-positive cells in vitro.

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].

Becotatug (JMT-101) is an IgG1 antibody targeting EGFR, which can be conjugated to Afatinib and Osimertinib, serving as a synthetic antibody-drug conjugate (ADC) [1].

Mecbotamab vedotin (BA3011) is a humanized IgG1-κ antibody engineered to target the AXL receptor tyrosine kinase (AXL). Serving as a conditionally active biologic (CAB), mecbotamab is conjugated to monomethyl auristatin E (MMAE) through a cleavable linker, creating an antibody-drug conjugate (ADC) for therapeutic use [1] [2].

Sofituzumab vedotin (DMUC5754A) is an antibody-drug conjugate (ADC) comprising an anti-MUC16 antibody linked to monomethyl auristatin E (MMAE) via a protease-cleavable linker, utilized for cancer research [1].

Izeltabart (IMGC-936) is a Maytansinoid-based Antibody-Drug Conjugate (ADC) that specifically targets ADAM9. It consists of a high-affinity humanized antibody conjugated site-specifically to DM21-C, a linker-payload that combines a microtubule-disrupting Maytansinoid with a stable tripeptide linker, maintaining a drug-to-antibody ratio of approximately 2.0. Izeltabart demonstrates cytotoxicity against ADAM9-expressing human tumor cell lines and possesses significant antitumor efficacy in xenograft tumor models [1].

Depatuxizumab MMAE is an antibody-drug conjugate (ADC) comprising the anti-EGFR monoclonal antibody depatuxizumab linked to the cytotoxic agent monomethyl auristatin E (MMAE). This ADC effectively suppresses the growth of xenograft models harboring both mutant EGFRvIII and wild-type EGFR [1].

Sirtratumab vedotin (ASG15-ME) is an antibody-drug conjugate (ADC) that links a SLITRK6-specific human gamma 2 antibody (Igγ2) to the microtubule disruption agent monomethyl auristatin E (MMAE) through a protease-cleavable linker [1].