Table 1:

Status of HER3-targeting agents in preclinical and clinical trials.

Drug type	Drug name	Mechanism of Action	Developer	Highest clinical trial phase	Indication (cancer type)	Key trial numbers	References
Antibodies	Patritumab (U3-1287)	HER3 mAb	Daiichi Sankyo	Phase III	NSCLC, breast, head & neck	NCT02134015 NCT02134015 NCT01211483	(104,120)
	Seribantumab (MM-121)	HER3 mAb	Merrimack Pharmaceuticals / Elevation Oncology	Phase II	NSCLC, breast, ovarian, advanced	NCT00994123 NCT01209195 NCT01451632 NCT04383210	(156)
	Lumretuzumab (RO5479599, RG7116)	HER3 mAb	Genentech/Roche	Phase Ib/II	NSCLC, breast solid tumors	NCT01918254 NCT02204345 NCT01482377	(157)
	Elgemtumab (LJM716)	HER3 mAb	Morphosys/Novartis	Phase I/II	Breast, gastric, head & neck, solid	NCT02143622 NCT01602406 NCT02167854	(158)
	GSK2849330	HER3 mAb	GlaxoSmithKline	Phase I	Solid tumors	NCT01966445	(159)
	CDX-3379 (KTN3379)	HER3 mAb	Celldex Therapeutics	Phase II	Head & neck, advanced tumors	NCT02473731 NCT02014909	(160)
	AV-203	HER3 mAb	Aveo Oncology	Phase I	Solid tumors	NCT01603979	(161)
	ISU104	HER3 mAb	ISU Abxis	Phase I	Solid tumors	NCT03552406
	REGN1400	HER3 mAb	Regeneron Pharmaceuticals	Phase I	Metastatic cancers	NCT01727869	(162)
	TK-A3, TK-A4	HER3 mAb	Takis Biotech	Preclinical			(163)
	MP-EV20	HER3 mAb	Mediapharma	Preclinical			(164)
	1A5-3D4	HER3 mAb		Preclinical			(165)
	9F7-F11, 16D3-C1	HER3 mAb	GamaMabs Pharma	Preclinical			(131)
	NG33	HER3 mAb		Preclinical			(150)
	A5, F4	HER3 mAb		Preclinical			(150)
	HMBD-001 (10D1F)	HER3 mAb	Hummingbird Bioscience	Preclinical			(166)
	huHER3-8	HER3 mAb		Preclinical			(167)
ADCs	U3-1402	HER3-ADC	Daiichi Sankyo	Phase II	Breast, NSCLC, colorectal	NCT04479436 NCT03260491 NCT02980341	(123,168)
	EV20/MMAF, EV20-Sap	HER3-ADC	Mediapharma	Preclinical			(128,129)
	HER3-ADC 9F7-F11	HER3-ADC		Preclinical			(169)
Bi-specific antibodies	Zenocutuzumab (MCLA-128)	HER2/HER3 bispecific	Merus	Phase I/II	Solid tumors	NCT02912949	(170)
	Sym013	EGFR/HER2/ HER3 mAb mixture	Symphogen	Phase I/II	Advanced epithelial malignancies	NCT02906670
	Duligotuzumab (MEHD7954A)	EGFR/HER3 bispecific	Genentech/Roche	Phase II	Head & neck, advanced tumors	NCT01911598 NCT01986166	(137)
	Istiratumab (MM-141)	HER3/IGF1R bispecific	Merrimack Pharmaceuticals	Phase II	Advanced solid, colorectal, Pancreatic, head & neck	NCT01733004 NCT02538627 NCT02399137	(171)
	SI-B001	EGFR/HER3 bispecific	Biokin Pharma	Phase I	Locally advanced or metastatic epithelial tumors	NCT04603287	(172)
	MM-111	HER2/HER3 bispecific	Merrimack Pharmaceuticals	Phase I	HER2 / heregulin positive, breast	NCT01097460 NCT00911898 NCT01304784	(108)
	scDb Fc (scDb hu225x3-43-Fc)	EGFR/HER3 bispecific		Preclinical			(109)
Antisense oligonucleotide	EZN-3920	HER3 mRNA antagonist	Enzon Pharmaceuticals	Preclinical			(152)
micro-RNAs	miR-450b-3p	Inhibits HER3 expression		Preclinical			(173)
	miR-205	Inhibits HER3 expression		Preclinical			(174)

ADC, antibody drug conjugate; EGFR, epidermal growth factor receptor; HER, human epidermal growth factor receptor; IGF1R, insulin-like growth factor receptor; mAb, monoclonal antibody; miR, micro-RNA; NSCLC, non-small cell lung cancer.