Table 1. Properties of ADC and dosing regimen in first-in-man studies.

Drug	Name	Company	Target	Indication	Isotype	linker	Linker class	Cytotoxin	DAR	Development phase	Ph 1 Doses (mg/kg)	Ph 1 Regimen	MTD (mg/kg)
Adcetris®	Brentuximab vedotin, SGN35	Seattle	CD30	HL and ALCL	IgG1	vc	cleavable, protease	MMAE	4	Approved	0.4 - 1.4	Q1W	1.8
		Genetics									1.2 - 2.7	Q3W
Kadcyla®	Trastuzumab emtansine, T-DM1	Genentech/	Her2	HER2+ breast cancer	IgG1	SMCC	stable	DM1	3.5	Approved	1.2 - 2.9	Q1W	2.4
		Roche									0.3 - 4.8	Q3W	3.6
Mylotarg®	Gemtuzumab ozogamicin	Pfizer	CD33	AML	IgG4	hydrazone	cleavable,	calicheamicin	2.5	Approved, withdrawn	0.006–0.22	Q2W	0.22
							acid labile					(2 doses)
CMC544	Inotuzumab ozogamicin	Pfizer	CD22	NHL - ALL	IgG4	hydrazone	cleavable,	calicheamicin	6	3	0.01–0.06	Q3W	-
							acid labile				0.044	Q4W	0.044
IMGN242, huC242-DM4	Cantuzumab ravtansine	ImmunoGen	CanAg	Gastric	IgG1	SPDB	cleavable, disulfide	DM4	ND	2, discontinued	0.44–7.3	Q3W	4.2
IMGN901	Lorvotuzumab mertansine	ImmunoGen	CD56	Small cell lung cancer	IgG1	SPP	cleavable, disulfide	DM1	3.5	2, discontinued	1–3.5	Q4W	2.8
												Day 1 and 8
BT062	Indatuximab ravtansine	Biotest	CD138	Multiple myeloma	IgG4	SPDB	cleavable, disulfide	DM4	3.5	2	-	Q1W	-
											0.25–4.9	Q3W	4.0
											-	Q4W	-
CDX-011	Glembatumumab vedotin	Celldex	GPNMB	Breast	IgG2	vc	cleavable, protease	MMAE	4	2	-	Q1W	1.88
											-	Q2/3W
											0.03 - 2.63	Q3W
DCDT2980S	Pinatuzumab vedotin	Genentech/	CD22	NHL and DLBCL	IgG1	MC-VC-PABC	cleavable, protease	MMAE	ND	2	0.1–3.2	Q3W	2.4
		Roche
PSMA-ADC	-	Progenics	PSMA	metCRPC	IgG1	vc	cleavable, protease	MMAE	4	2	0.4 - 2.8	Q3W	2.5
SAR3419	Coltuximab ravtansine	Sanofi	CD19	NHL	IgG1	SPDB	cleavable, disulfide	DM4	3.5	2	0.12–1.7	Q1W	1.4
											0.25–6.7	Q3W	4.0
DCDS4501A	Polatuzumab vedotin	Genentech /	CD79b	NHL and DLBCL	IgG1	MC-VC-PABC	cleavable, protease	MMAE	ND	2	0.1 - 2.4	Q3W	not reached
		Roche
AVE9633	-	Sanofi	CD33	AML	IgG1	SPDB	cleavable, disulfide	DM4	3.5	1, discontinued	0.37–6.4	Q1W	not reached
												Q3W
huC242-DM1	Cantuzumab mertansine	ImmunoGen	CanAg	Solid malignancies	IgG1	SPP	cleavable, disulfide	DM1	3.5	1, discontinued	0.54–7.3	Q3W	5.8
IMGN388	-	ImmunoGen	integrin	Solid malignancies	IgG1	SPDB	cleavable, disulfide	DM4	ND	1, discontinued	0.12–4.0	Q3W	not defined
MEDI547	-	MedImmune	EphA2	Solid tumors	IgG1	maleimido caproyl	stable	MMAF	4	1, discontinued	0.08	Q3W	not defined
MLN2704	-	Millennium	PSMA	Prostate	IgG1	thioester	cleavable, disulfide	DM1	3.5	1, discontinued	0.44–8.5	Q4W	not defined
ASG-5ME	-	Agensys (Astellas)	SLC44A4	Prostate, pancreatic, and gastric cancers	IgG2	vc	cleavable, protease	MMAE	3.7	1, discontinued	0.3 - 1.5	Q1W	1.2
											0.3 - 3	Q3W	2.4
SGN-75	Vorsetuzumab mafodotin	Seattle	CD70	RCC	IgG1	mc	stable	MMAF	ND	1, discontinued	0.3 - 4.5	Q1W	-
		Genetics									0.3 - 4.5	Q3W	3.0
IMGN853	-	ImmunoGen	FOLR1	Ovarian, solid tumors	ND	sulfo-SPDB	cleavable, disulfide	DM4	ND	1	0.15 - 7	Q3W	ongoing
MLN0264	-	Millennium	Guanylyl cyclase C	GI malignancies	ND	ND	cleavable, protease	MMAE	ND	1	0.3–1.8	Q3W	ongoing

ND: no data; HL: Hodgkin lymphoma; ALCL: Anaplastic large cell lymphoma; DLBCL: diffuse large B-cell lymphoma; AML: Acute myeloid leukemia ; NHL: Non-Hodgkin Lymphoma; metCRPC: metastatic castrate-resistant prostate cancer; RCC: Renal cell carcinoma ; q1w: every week; q2w: every 2 wk; q3w: every 3 wk