Table 1.

Anti-HER2 ADCs approved for use or in clinical development (in clinical trials).

ADC	Antibody	Payload	Linker	DAR	Status	Clinical Trials and References
T-DM1	Trastuzumab	DM1	Non-cleavable	3.5	Approved
T-DXd	Trastuzumab	Deruxtecan	Cleavable	6–8	Approved
SYD985	Trastuzumab	Duocarmycin (seco-DUBA)	Cleavable (valine-citruline)	2.8		NCT03262935, phase III NCT04602117, phase I/Ib NCT02277717, phase I NCT04205630, phase II NCT04235101, phase I
ARX788	Modified trastuzumab	MMAF	Non-cleavable (Amberstatin, AS269)	1.9	CT	NCT05018676, phase II NCT05018702, phase II NCT048299604, phase II NCT04983121, phase II NCT05041972, phase II NCT03255070, phase I NCT02512237, phase I
RC48-ADC	Ig anti-Her2	MMAE	Cleavable (valine-citruline)	4	CT	NCT03052634, phase I/II NCT04400695, phase III NCT03500380, phase II/III NCT04311034, phase I/II NCT04714190, phase III NCT03556345, phase II NTC05016973, phase II NCT04879329, phase II NCT04264936, phase I/II NCT03809013, phase II NCT03507166, phase II NCT04073602, phase II NCT04965519, phase II NCT04329429, phase II NCT04280341, phase I NCT02881138, phase I NCT02881190, phase I
ALT-P7	Trastuzumab variant	MMAE	Cysteine -containing peptide	UD	CT	NCT03281824, phase I
MRG002	IgG anti-HER2	MMAE	Cleavable (valine-citruline)	3.8	CT	CTR20181778, phase I NCT04924699, phase II NCT04941339, phase I NCT04839510, phase II NCT04837508, phase II NCT04742153, phase II NCT04492488, phase I/II
A166	Trastuzumab	MMAF	Cleavable (valine-citruline)	UD	CT	NCT03602079, phase I/II
PF06804103	IgG1 antiHER2	Auristatin 0101	Cleavable (Maleimidocaproyl-valine-citruline)	4	CT	NCT03284723, phase I
MEDI4276	Trastuzumab scFV	MMETA	Protease cleavable	4	CT	NCT02576548, phase I/II
BDC1001	Trastuzumab biosimilar	TLR 7/8 agonist	Non-cleavable	UD	CT	NCT04278144, phase I/II
SBT6050	IgG anti-HER2	TLR8 agonist			CT	NCT05091528, phase I/II NCT04460456, phase I
FS-1502	Trastuzumab	MMAF	Beta-glucuronide	2	CT	NCT03944499, phase I
ZW49	Biparatopic antiHER2 IgG	Auristatin	Cleavable	UD	CT	NCT03821233, phase I
BAT8001	IgG1 antiHER2	Batansine	Non-cleavable	UD	CT	NCT04189211, phase I NCT04151329, phase I/II NCT04185649, phase III
DHES0815A	IgG antiHER2	PBD-MA	Non-cleavable	2	CT	NCT03451162, phase I
GQ1001	Trastuzumab	DM1	UD Intelligent ligase dependent conjugation	UD	CT	NCT04450732, phase I
DP303c	IgG antiHER2	UD			CT	NCT04146610, phase I NCT04828616, phase II NCT04826107, phase II
BB-1701	IgG antiHER2	UD			CT	NCT04257110, phase I
SHR-A1811	IgG antiHER2	UD			CT	NCT04446260, phase I NCT04818333, phase I/II NCT04513223 phase I
B003-101	IgG antiHER2	UD			CT	NCT03953833, phase I

Abbreviations: DAR = drug to antibody ratio; CT = clinical trial; UD = undisclosed; MMAE = monomethyl auristatin E; and MMAF = monomethyl auristatin F.