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Table 2 Examples of drugs used in HER2 breast cancer treatment

From: Targeting protein quality control pathways in breast cancer

Drug name Notes Developmental stage References
Trastuzumab (Herceptin) Monoclonal antibody against HER2 FDA approved [355,356,357,358,359,360]
Ado trastuzumab emtansine (T-DM1) Bifunctional antibody-drug (trastuzumab linked to ematansine, DM1). Binds HER2 and inhibits microtubule assembly/disassembly FDA approved [361,362,363,364]
Eetumaxomab Monoclonal antibody with CD3 and HER2 recognition sites Clinical trial [365, 366]
Pertuzumab (Perjeta) Recombinant humanized antibody against domain II of HER2 FDA approved [284, 367, 368]
MM-111 Antibody against HER2-HER3 dimers Clinical trial [369, 370]
Lapatinib (Tykerb) Irreversible tyrosine kinase inhibitor in luminal B cancers FDA approved [371, 372]
Afatinib Irreversible pan-HER tyrosine kinase inhibitor Clinical trial [373,374,375]
Canertinib Irreversible tyrosine kinase inhibitor Clinical trial [19, 376, 377]
Neratinib Irreversible pan-HER tyrosine kinase inhibitor, effective against EGFR, HER2, and HER4 Clinical trial [378,379,380,381]
Gefitinib EGFR tyrosine kinase inhibitor Clinical trial [382, 383]
Erlotinib hydrochloride (Erlotinib) Reversibly binds to the intracellular catalytic domain of EGFR; used also in TBNC cancers Clinical trial [383,384,385]
Sapitinib Tyrosine kinase inhibitor effective in luminal B resistant cells Clinical trial [380, 386]
Sorafenib Blocks the enzyme RAF kinase, inhibiting cancer cell proliferation and autophagy induction Clinical trial [63,388,, 387389]
Sildenafil citrate Selectively inhibits cyclic guanosine monophosphate (cGMP)-specific type 5 phosphodiesterase Clinical trial [63]
MM-121 Human monoclonal antibody against HER3 Clinical trial [267,391,, 390392]
MM-302 Doxorubicin encapsulated within liposomes, and conjugated to a monoclonal antibody against HER2. Inhibits HER2 and topoisomerase II Clinical trial [393, 394]
ARRAY-380 Reversible selective HER2 inhibitor Clinical trial [395]
TAK-285 HER2-EGFR tyrosine kinase inhibitor HER2-positive breast cancer cells [396,397,398,399]
Everolimus (Afinitor) Inhibitor of mTORC1 used both in luminal A and in HER2-positive tumors FDA approved [277,278,279, 283]
Temsiroliums Inhibitor of mTORC1 used in luminal A, TNBC, and HER2-positive tumors Clinical trial [331]
GDC-0941 PI3K inhibitor Clinical trial [400, 401]
SAR245408 PI3K inhibitor Clinical trial [402, 403]
17-AAG Hsp90 inhibitor Clinical trial [404,405,406]
Retaspinmycin (IPI-504) Hsp90 inhibitor Clinical trial [406,407,408]
Genetespib Hsp90 inhibitor used in metastatic HER2 breast cancers Clinical trial [409,410,411,412]
Pazopanib inhibitor of VEGFRs able to inhibit Hsp90 ATPase activity Clinical trial [63, 413, 414]
SNX-2112 Hsp90 inhibitor, effective in HER2 and luminal B breast cancers Clinical trial [83, 280, 415]
Geldanamycin Hsp90 inhibitor HER2-positive breast cancer cells [20,115,, 109, 114116]
KIN001-51 HER3 binder, impairs dimerization HER2-positive breast cancer cells [416, 417]
TX1-85-1 Induces HER3 degradation by covalent binding to a residue in the receptor HER2-positive breast cancer cells [100, 383]
TX2-121-1 Derivate of TX1-85-1 linked to adamantane group. Induces HER3 degradation HER2-positive breast cancer cells [100, 383]
Patritumab (AMG 888) Monoclonal antibody directed against the ligand-binding pocket of HER3 Clinical trial [418]
MEHD7945A Monoclonal antibody directed against EGFR and HER3 Clinical trial [419, 420]
Pilaralisib Pan-class I PI3K inhibitor HER2-positive breast cancer cells [224, 421]
liposomal paclitaxel Inhibits tubulin assembly/disassembly FDA approved [224, 421, 422]
hydroxychloroquine Autophagy inhibitor, suppresses lysosomal acidification Clinical trial [167, 225]
Eeyarestatins p97 inhibitor HER2-positive breast cancer cells [81, 85]
NMS-873 p97 inhibitor HER2-positive breast cancer cells [81]
HA15 Inhibitor of BiP ATPase activity HER2-positive breast cancer cells [173]