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Table 1 HER2-based immunotherapy in clinic

From: Recombinant immunotoxins development for HER2-based targeted cancer therapies

Therapeutics Features Status Tumor type Refs.
Antibody
 Trastuzumab ECD IV of HER2 binding humanized monoclonal antibody FDA approved HER2-positive breast cancer [34]
 Pertuzumab ECD II of HER2 binding humanized monoclonal antibody FDA approved HER2-positive breast cancer [38]
 Margetuximab Increased binding to activating Fcγ receptor IIIA (CD16A) and decreased binding to inhibitory Fcγ receptor IIB (CD32B) FDA approved HER2-positive BC, gastric cancers and gastro-esophageal junction cancer [41]
 BTRC4017A T-cell dependent (CD3) bispecific antibody Phase I (NCT03448042) HER2-positive solid tumors [42]
 PRS-343 T-cell dependent (CD137) bispecific antibody Phase I (NCT03330561, NCT03650348) HER2-positive solid tumors [43]
 GBR-1302 T-cell dependent (CD3) bispecific antibody Phase I (NCT02829372) Breast cancer [44]
 ZW25 Bispecific antibody against two distinct HER2 epitopes Phase I (NCT02892123)
Phase II (NCT04513665)
Breast cancer, endometrial cancer, carcinosarcoma [45]
Antibody–drug conjugate
 Trastuzumab– emtansine Trastuzumab antibody linked to anti-mitotic agent, mertansine FDA approved HER2-positive metastatic breast cancer [46]
 ARX788 HER2 targeting mAb linked to the AS269 (a highly potent tubulin inhibitor) Phase I (NCT02512237) HER2-positive metastatic breast cancer [47]
 DS8201a Trastuzumab–deruxtecan (DNA topoisomerase I inhibitor) Phase I (NCT04042701) Advanced/metastatic NSCLC [48]
 MEDI4276 Bispecific antibody targeting two different HER2 epitopes, conjugated with MMETA (a potent tubulysin-based microtubule inhibitor) Phase I/II (NCT02576548) HER2 positive breast cancer [49]
 MM302 Pegylated liposomal doxorubicin formulation, with anti-HER2 antibody fragments coupled to its surface. Phase I (NCT01304797) HER2-positive breast cancer [50]
 PF-06804103 Anti-HER2 monoclonal antibody conjugated with the cytotoxic agent Aur0101 Phase I (NCT03284723) HER2 positive breast cancer and gastric cancer [51]
 SYD985 Trastuzumab–duocarmazine Phase I (NCT02277717)
Phase II (NCT04205630)
Phase III (NCT03262935)
Metastatic breast cancer [52]
 XMT-1522 Anti HER2 IgG1 conjugated with the tubulin inhibitor AF-HPA Phase I (NCT02952729) Advanced breast cancer, gastric cancer and NSCLC [53]
Tyrosine kinase inhibitor
 Lapatinib HER1 and HER2 tyrosine kinases inhibitor FDA approved Metastatic breast cancer [54]
 Neratinib HER1, HER2, and HER4 tyrosine kinases inhibitor FDA approved Early-stage HER2-positive breast cancer [55]
 Afatinib ErbB family tyrosine kinases inhibitor FDA approved Metastatic NSCLC [56]
 Ibrutinib ErbB family tyrosine kinases inhibitor FDA approved CLL, MCL, DLBCL, MM, FL and WM [57]
 Pyrotinib HER1, HER2, and HER4 tyrosine kinases inhibitor Phase I (NCT01937689) Breast cancer [58]
  1. CLL chronic lymphocytic leukemia, FL follicular lymphoma, MCL mantle cell lymphoma, DLBCL diffuse large B cell lymphoma, MM multiple myeloma, NSCLC non-small cell lung cancer, WM waldenstrom’s macroglobulinemia