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. Author manuscript; available in PMC: 2023 Jun 1.
Published in final edited form as: Clin Exp Metastasis. 2022 Jan 12;39(3):391–406. doi: 10.1007/s10585-022-10146-x

Table 3.

CD44 as a Therapeutic Target

Therapies Targeted isoform Cancers studied Mode of action References
Monoclonal antibodies
Chimeric mAb U36 (cmAb U36) CD44v6 Head and neck squamous cell carcinoma Radiolabeled cmAbU36 showed anti-tumor effect by binding and internalization in tumor cells. [125, 126]
Humanized mAb BIWA 4 (bivatuzumab) CD44v6 Head and neck squamous cell carcinoma Radiolabeled bivatuzumab showed anti-tumor effect by binding and internalization in tumor cells. [126]
Bivatuzumab mertansine CD44v6 Head and neck squamous cell carcinoma

  • Prodrug mertansine covalently conjugated to bivatuzumab.

  • Mertansine inhibits tubulin polymerization, thereby disrupting microtubule assembly

 [141]
RG7356 Pan-CD44 Phase I trial in several solid malignancies

  • Recombinant anti-CD44 immunoglobulin G1 humanized monoclonal antibody

  • Selectively binds near the HA-binding region of the extracellular domain of all CD44 isoforms.

  • Demonstrated growth inhibition of several CD44-expressing tumor xenografts.

  • Phagocytosis of CD44− positive cancer cells,

 [127]
RO5429083 Pan-CD44 Phase I trial in several solid malignancies

  • Immunomodulating and antineoplastic activity.

  • Binds to the constant region of the extracellular domain of CD44 and prevents the activation of various CD44-mediated signal transduction pathways

 [142]
mAbs IM7 Pan-CD44 Breast cancer cells Blocks CD44-HA interaction. Induces CD44 shedding from the cell surface. [128]
LA-chitosan-IM7 Pan-CD44 Ovarian cancer Blocks CD44-HA interaction and CD44-mediated proliferation. Effective in treating cancers in vitro and in vivo while reducing the toxicity of mAbs IM7. [143]
KM201 Pan-CD44 Human vascular endothelial cells Blocks CD44-HA interaction [129]
Natural compound
Silibinin CD44v7-10 Prostate cancer Blocks CD44-HA interaction [130]
Silibinin Cd44v6 Colon cancer Attenuates stemness of colon cancer stem cells [144]
Aptamers
DNA aptamer CD44v10 Breast cancer Inhibits breast cancer cell migration [132]
RNA aptamers Pan-CD44 Breast Cancer Targets CD44-positive cells, including cancer stem cells, for detection, sorting, enrichment, and drug delivery purposes. [133]