Antibody-Drug Conjugates (ADCs)

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.

Disitamab vedotin (RC-48) is a newly developed antibody-active molecule conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2), consisting of hertuzumab coupled to monomethyl auristatin E (MMAE) via a cleavable linker. Disitamab vedotin showed anti-tumor and anti-proliferative activities in gastric cancer cells with different HER-2 expression levels and inhibited the expression of HER-2 protein in gastric cancer cells.

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.

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

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.

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].

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].

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].

Belantamab mafodotin (GSK2857916) is a conjugate of a humanized, targeted monoclonal antibody directed against the B cell maturation antigen (BCMA) and the cytotoxic agent McMMAF, exhibiting anti-myeloma activity [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].

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].

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].

Telisotuzumab vedotin (ABBV-399), an antibody-drug conjugate (ADCs), targets c-Met and comprises the cytotoxic agent Monomethyl Auristatin E (MMAE), the Telisotuzumab antibody, and a cleavable mc-val-cit-PABC linker. This compound is utilized in cancer research [1].

Patritumab deruxtecan (HER3-DXd), an antibody-drug conjugate (ADC), comprises a fully human anti-HER3 IgG1 monoclonal antibody, Patritumab, linked to a topoisomerase I inhibitor payload through a tetrapeptide-based cleavable linker, demonstrating anticancer activity [1].

Cofetuzumab pelidotin (PF-06647020) is an antibody-drug conjugate (ADC) targeting PTK7, composed of the humanized anti-PTK7 monoclonal antibody (hu6M024, IgG1) linked to the auristatin-based microtubule inhibitor payload, auristatin-0101 (Aur0101), via a cleavable valine-citrulline (vc)-based linker. This compound exhibits a drug-to-antibody ratio (DAR) of 4 and selectively binds to cell-surface PTK7 with an EC50 of 1153 pM as determined by flow cytometry. Cofetuzumab pelidotin holds promise for the study of solid tumors [1] [2] [3].

Depatuxizumab mafodotin, an antibody-drug conjugate (ADC) targeting the epidermal growth factor receptor (EGFR), is utilized in cancer research [1].

Moxetumomab Pasudotox (CAT 8015) is an anti-CD22 immunotoxin comprising an anti-CD22 Fv and Pseudomonas exotoxin, targeting the CD22 cell surface receptor present on various malignant B-cells. This compound is applicable in researching hairy cell leukemia (HCL) [1] [2] [3].

Inotuzumab Ozogamicin is an antibody-conjugated active molecule (ADC) that targets CD22 and is conjugated to Ozogamicin, a cytotoxic antibiotic. Inotuzumab Ozogamicin is indicated for use in the study of acute lymphoblastic leukemia (ALL).

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].

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

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].

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].

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].

Sacituzumab govitecan (IMMU-132), an antibody-drug conjugate (ADC) targeting Trop-2, facilitates the delivery of SN-38. It demonstrates anticancer activity [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].

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.

Enfortumab vedotin-ejfv is an antibody-drug conjugate targeting Nectin-4, employed in the treatment of urothelial carcinoma [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].

Cetuximab sarotalocan (Cetuximab-IRDye-700DX) is a conjugate comprising Cetuximab, an anti-EGFR monoclonal antibody, and IRdye700DX, a near-infrared photosensitizing dye. It is utilized in the study of head and neck cancers [1] [2].