Activity of selected, novel anti-HER2 compounds under development

Compound Sponsor Phase BC patients treated ORR in study arm Median PFS in study arm NCT.gov
Monoclonal antibodies
Margetuximab (+ chemotherapy) [43] MacroGenics III 536 25% 5.8 months NCT02492711
Antibody drug conjugates
Trastuzumab deruxtecan [47] Daiichi Sankyo II 184 60.9% 16.4 months NCT03248492
Trastuzumab duocarmazine [49] Byondis B.V. I 48 33% 7.6 months NCT02277717
PF-06804103 [50] Pfizer I 10 66% NA NCT03284723
ARX788 [51] Ambrx, Inc. I 45 31% NA NCT03255070
RC48-ADC [52] RemeGen I 70 31% 5.8 months NCT03052634
A166 [53] Klus Pharma Inc. I 24 26% NA NCT03602079
bsAbs
Zanidatamab (ZW25) [54] Zymeworks Inc. I 13 46% NA NCT02892123
PRS-343 [55] Pieris Pharma, Inc. I 16 12% NA NCT03330561
Zenocutuzumab (MCLA-128) (+ trastuzumab & vinorelbine) [56] Merus N.V. II 28 19% NA NCT03321981
TKIs
Tucatinib (+ trastuzumab & capecitabine) [57] Seagen Inc. II R 612 40% 7.8 months NCT02614794
Neratinib (+ capecitabine) [42] Puma Biotech. Inc. III R 621 33% 5.6 months NCT01808573
Poziotinib (+ capecitabine) [58] Spectrum Pharma Inc. II 106 25% 4 months NCT02659514
Pyrotinib (+ capecitabine) [59] Jiangsu HengRui Med. Co. II 267 67% 12.5 months NCT03080805

R: randomized; NA: not applicable; PRS: progesterone receptors