Table 2.

Breast cancer-targeting ADCs in clinical development

Target antigen	ADC designation	Application	Patient population	Development Stage	Main results	Representative clinical trials (ClinicalTrials.gov Identifier)*	Reference
HER2	MM-302	Combo	HER2+ mBC	Phase I, II, III	Manageable safety profile, evidence of antitumor activity	NCT02213744, NCT01304797	(Geretti et al., 2015; LoRusso et al., 2015a)
	SYD985	Mono	mBC	Phase I	Preclinical antitumor activity	NCT02277717	(Dokter et al., 2014; Elgersma et al., 2015; van der Lee et al., 2015)
	XMT-1522	N/A	mBC	Preclinical	Preclinical antitumor activity	N/A	(Bergstrom et al., 2015)
gpNMB	CDX-011	Mono	gpNMB+ mBC	Phase I, II	Acceptable safety profile, evidence of antitumor activity	NCT01997333, NCT01156753, NCT00704158	(Bendell et al., 2014a; Vaklavas and Forero, 2014; Yardley et al., 2015)
Trop-2	IMMU-132	Mono	mBC	Phase I, II	Acceptable safety profile, evidence of antitumor activity	NCT01631552	(Goldenberg et al., 2015; Sharkey et al., 2015; Starodub et al., 2015)
Mesothelin (MSLN)	BMS-986148	Mono	Advanced solid tumor	Phase I, II	Preclinical antitumor activity	NCT02341625	(Gupta et al., 2014; Lamberts et al., 2015; Scales et al., 2014)
	BAY94-9343	Mono	Advanced solid tumor	Phase I	Preclinical antitumor activity	NCT01439152, NCT02485119
CA6	SAR566658	Mono	CA6+ breast cancers	Phase I	Favorable safety profile, evidence of antitumor activity	NCT01156870	(Boni et al., 2014)
Ephrin-A4 (EFNA4)	PF-06647263	Mono	Advanced solid tumor	Phase I	Preclinical antitumor activity	NCT02078752	(Damelin et al., 2015)
LIV-1 (SLC39A6)	SGN-LIV1A	Mono	LIV-1-Positive mBC	Phase I	Preclinical antitumor activity	NCT01969643	(Sussman et al., 2014)
Ly6E	DLYE5953A	Mono	Advanced solid tumor	Phase I	Preclinical antitumor activity	NCT02092792	(Asundi et al., 2015)
c-RET	Y078-DM1/DM4	N/A	HER2+ and basal breast cancer	Preclinical	Preclinical antitumor activity	N/A	(Nguyen et al., 2015)
B7-H4	Anti-B7-H4 ADC	N/A	B7-H4+ breast cancer	Preclinical	Preclinical antitumor activity	N/A	(Leong et al., 2015)
CD138	BT-062	N/A	mBC	Preclinical	Preclinical antitumor activity	N/A	(Ibrahim et al., 2013; Rapraeger, 2013)

^*Phase III, II and I trials are highlighted in red, blue and black respectively