Table 2.
Strategies targeting glycosylation in clinical trials
| Approach | Target | Drug candidate | Cancers | Phase | Identifier |
|---|---|---|---|---|---|
| Inhibitors of glycosylation | Galectin-1 | OTX008 | solid tumors | I | NCT01724320 |
| Galectin-3 | GB1211, GCS-100 | metastatic melanoma, head and neck squamous cell carcinoma, non-small cell lung cancer, diffuse large B-cell lymphoma, chronic lymphocytic leukemia | I/II | ||
| Galectin-1 and -3 | GR-MD-02, GM-CT-01 | melanoma, non-small cell lung cancer, squamous cell carcinoma of the head and neck, colorectal cancer, cancer of the bile duct, gallbladder cancer | I/II | ||
| Selectins | GMl-1271 | acute myeloid leukemia, multiple myeloma | I/II/III | ||
| Fucosylation | SGN-2FF | non-small cell lung cancer, renal cell carcinoma, breast neoplasms, urinary bladder neoplasm | I | NCT02952989 | |
| Glycan-based antibodies | Gangliosides (e.g., GD2, GD3, GM2, GM3 and fucosyl- GM1) | hu3F8, ch14.18, hu14.18- IL2, PF-06688992, KW- 2871, BMS-986012 | neuroblastoma, lung cancer, osteosarcoma, melanoma, brain and central nervous system tumors, ovarian cancer, retinoblastoma, sarcoma, small intestine cancer, melanomas, other solid tumors | I/II/III | |
| Globo H | OBI-888, OBI-999 | solid tumors | I/II | NCT03573544, NCT04084366 | |
| Truncated O-glycan (e.g., Tn, and STn) | PankoMab-GEX™ | ovarian epithelial cancer, fallopian tube cancer, primary peritoneal cancer, breast cancer | I/II/III | ||
| Lewis antigens (e.g., LeA, and LeY) |
MVT-5873 hu3S193 |
pancreatic cancer, ovarian cancer, small cell lung cancer | I/II | ||
| MUC-1 |
TAB004, SAR566658, MUC1 + CD3 BsAb |
breast cancer | I/II | ||
| Glycan-based vaccines | Glycolipids (e.g., GD2, GD3, GM2, GM3, and α-galactose containing) |
bivalent vaccine, GM2-KLH vaccine, BEC2 Vaccine, BCG vaccine |
sarcoma, neuroblastoma, small cell lung cancer, breast cancer, fallopian tubes, ovarian cancer, peritoneal cancer, metastatic melanoma | I/II/III | |
| Globo H | OBI-822 | breast cancer | II/III | NCT03562637 | |
| Truncated O-glycan (e.g., T, Tn and STn) |
MAG-Tn3 + AS15, THERATOPE STn-KLH vaccine |
ovarian cancer, peritoneal cancer, breast cancer, prostate cancer | I/III | ||
| Lewis antigens |
sialyl Lewis A-KLH + QS21 |
breast cancer | Not Applicable | NCT00470574 | |
| Polysialic acid | Polysialic acid-KLH + QS21 | small cell lung cancer | II | NCT00004249 | |
| MUC-1 | YB-01 | breast cancer, other solid tumors | I/II | ||
| Polyvalent vaccines |
(Bivalent vaccine+ OPT-821), (Trivalent vaccine- KLH conjugated + OPT-821), (Globo-H-GM2-STn-TF-Tn-KLH-QS21), (GD2L, GD3L, Globo H, fucosyl- GM1, and N- propionylated polysialic acid -KLH + OPT-821) |
neuroblastoma, sarcoma, ovarian cancer, breast cancer, small cell lung cancer | I/II | ||
| CAR-T cells against aberrant glycosylation | Gangliosides (e.g., GD2) |
GD2Bi-aATC, 4SCAR-GD2, 1RG-CART, GD2-CART01, GINAKIT |
neuroblastoma, sarcoma | I/II | |
| Lewis antigen (e.g., LeY) | LeY-CAR-T | lung cancer, fallopian tube cancer, other solid tumors | I/II | NCT03198052, NCT03851146 | |
| MUC-1/MUC1-Tn |
MUC-1 CART huMNC2-CAR44 |
intrahepatic cholangiocarcinoma, breast cancer, lung cancer, ovarian cancer, fallopian tube cancer, multiple myeloma, pancreatic ductal adenocarcinoma | I/II |
MUC-1 mucin 1, CAR chimeric antigen receptor, STn sialyl-Tn