antibody-drug conjugates (adcs)

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.

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].

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].

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].

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

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].

Indatuximab ravtansine (BT-062) is an antibody-drug conjugate (ADC) (Antibody-Drug Conjugates (ADCs)) that consists of a murine-human chimeric form based on B-B4, which specifically targets CD138, linked via a disulfide bond to the maytansinoid drug DM4. It exhibits antitumor activity.

M3554 is an innovative anti-GD2 ADC derived from the humanized ch14.18 anti-GD2 antibody, exhibiting antitumor properties. It demonstrates sub-nanomolar IC50 cytotoxicity against GD2-positive neuroblastoma cell line CHP134.

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.

ABBV-221 is an intravenously administered drug that modulates the activity of epidermal growth factor receptor (EGFR) and has potential antitumor activity.

Ifinatamab deruxtecan (DS-7300a) is an active chemical compound utilized in various biochemical research applications.

Maridebart cafraglutide, an antibody-peptide conjugate, serves as a GLP-1 receptor agonist and a GIP receptor antagonist. It effectively reduces body weight and enhances metabolic markers in male obese mice and cynomolgus monkeys, showing promise for obesity research.

Mecbotamab vedotin (BA301) is an inhibitory IgG1 antibody that targets human tyrosine kinase receptor AXL and the humanized murine monoclonal BA301 γ1 chain. It can be utilized in the preparation of immunoconjugates for research into cancers expressing the Axl type.

Aprutumab ixadotin (BAY 1187982) is the first antibody-drug conjugate (ADC) targeting FGFR2, and is also the inaugural ADC to employ an auristatin-based active payload.

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-CD22-NMS249 is an antibody-drug conjugate (ADC) that targets CD22, comprising the humanized anti-CD22 antibody Pinatuzumab, a cleavable linker (Mc-VC-PAB), and the effective payload of DNA topoisomerase II inhibitor PNU-159682. This compound is utilized in the study of non-Hodgkin lymphoma (NHL).

Rolinsatamabtalirine (ABBV 176) is an antibody-drug conjugate (ADC) that targets the Prolactin receptor (PRLR). It consists of the antibody Rolinsatamab, an enzymatically cleavable peptide linker, and the cytotoxic agent SGD-1882.

SHR-A1201 is an antibody-drug conjugate (ADC) targeting HER2. This compound is composed of a humanized anti-HER2 antibody, the linker SMCC, and the cytotoxic payload Mertansine, which is a microtubule inhibitor. SHR-A1201 is utilized in research for HER2-positive breast cancer.

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.

Epratuzumab Tesirine (ADCT-602) is a novel CD22-targeted antibody-drug conjugate (ADC). This compound comprises a pyrrolobenzodiazepine (PBD) dimer and the active payload SG3249.