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.

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.

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.

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.

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.

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

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).

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

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).

Clivatuzumab MMAE is an ADC consisting of a humanized monoclonal antibody against MUC1 (mucin) and the anti-mitotic cytotoxin MMAE for pancreatic cancer.

Enapotamab vedotin is an investigational antibody-drug conjugate (ADC) specifically targeting the receptor tyrosine kinase AXL. it consists of a monoclonal antibody linked to the potent microtubule-disrupting agent monomethyl auristatin E (MMAE) and demonstrates significant inhibitory potential against high AXL-expressing non-small cell lung cancer (NSCLC), including tumors with resistance to EGFR inhibitors like Osimertinib.

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.

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.

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

Sigvotatug Vedotin is an antibody-drug conjugate (ADC) designed to selectively target integrin αvβ6-positive tumor cells through an engineered antibody with high specificity. Sigvotatug Vedotin employs a protease-cleavable linker that delivers the cytotoxic payload monomethyl auristatin E (MMAE), a microtubule inhibitor, directly into tumor cells. Upon internalization, MMAE disrupts microtubule organization, inhibits proper cell division, and ultimately results in tumor cell death, providing a targeted strategy in oncology research.

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.

Sacituzumab tirumotecan (SKB264) is an antibody-drug conjugate (ADC) targeting TROP2 (trophoblast cell surface antigen 2), capable of releasing the active payload KL610023 within TROP2-positive tumour cells. an effective topoisomerase I inhibitor that induces DNA damage and leads to cell cycle arrest and apoptosis, for use in non-small cell lung cancer (NSCLC) and triple-negative breast cancer (TNBC).

ORM-5029 is the first antibody-drug conjugate (ADC) targeting the human epidermal growth factor receptor 2 (HER2), combining the highly potent GSPT1 degrader SMol006 with Pertuzumab. It is applicable in cancer research.

REGN5093-M114 is a bispecific antibody-drug conjugate (ADC) that targets two epitopes of the MET receptor tyrosine kinase, effectively inhibiting NSCLC cell proliferation and demonstrating antitumor activity in mouse models. REGN5093-M114 is composed of the human monoclonal anti-MET antibody Davutamig and a tubulin-inhibiting linker-payload.

FZ-AD005 is a DLL3-targeted ADC composed of the novel anti-DLL3 antibody FZ-A038 and a valine-alanine (Val-Ala) dipeptide linker. This compound is used for research in small cell lung 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.

Anti-SLC34A2 (Lifastuzumab)-SPDB-DM4 is an antibody-drug conjugate (ADC) composed of the humanized anti-SLC34A2 (sodium-dependent phosphate transporter 2) antibody, Lifastuzumab, linked via SPDB to the tubulin inhibitor DM4. The toxic component and linker of this ADC is sulfo-SPDB-DM4. This compound can be utilized for cancer research.

PF-08046054 (SGN-PDL1V) is an antibody-drug conjugate (ADC) targeting PD-L1, created by linking an anti-PD-L1 antibody with the vedotin drug linker VcMMAE. This compound delivers MMAE intracellularly, exerting direct cytotoxic effects on PD-L1-expressing tumor cells. PF-08046054 is applicable for research in solid tumors.

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.