antibody-drug conjugates (adcs)

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).

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.

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.

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.

DEDN6526A (RG-7636) is a humanized ADC compound targeting endothelin B receptor (ETBR), which can be used to study melanoma.

PF-06647263 (anti-EFNA4-ADC) is an ADC compound targeting EFNA4, with anti-tumor activity, composed of an anti-EFNA4 antibody conjugated with calicheamicin, inducing significant tumor regression in TNBC xenografts.

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.

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].

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].

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].

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].

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].

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).

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

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

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].

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].

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].

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

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