Exploration of Targeted Anti-tumor Therapy

Table 1. 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

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

Declarations

Author contributions

PT and SM wrote the first draft of the manuscript. All authors contributed to manuscript revision, read and approved the submitted version.

Conflicts of interest

GC received honoraria for speaker, consultancy or advisory rule from Roche, Pfizer, Novartis, Seattle Genetics, Lilly, Ellipses Pharma, Foundation Medicine and Samsung. The other authors declare no conflict of interest to disclose.

Ethical approval

Not applicable.

Consent to participate

Not applicable.

Consent to publication

Not applicable.

Availability of data and materials

Not applicable.

Funding

No funding was provided for this work.

Copyright

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