Clinical Trial Stage

ADC name

Antibody/Linker

Cytotoxic drugs

Cancer types

Antigen targeted

Phase I

ASG-22ME

Hu IgG1/valine-citrulline (V.C)

MMAE

Urothelial and other malignant solid tumors

Nectin-4

SAR566658

Hz IgG1/DS6 disulfide

Maytansinoid

Malignant neoplasm, triplenegative breast cancer

CA6

BAY 94-9343

H IgG1/disulfide, HuIgG1/SPDB

Maytansinoid, (DM4)

Mesothelin-positive solid tumors

Mesothelin

IMGN388

IgG1/disulfide

Maytansinoid

Solid tumors

Integrin αv

BIIB015

IgG1/disulfide

Maytansinoid

Anti-Cripto, refractory solid tumors

Cripto-1

SGN-75

Anti D70/dipeptide

Auristatin

Renal cell carcinoma

CD70

AGS-22M6E

Anti-Nectin fully human IgG/dipeptide

Auristatin

Malignant solid tumors

Nectin4

IMGN529

K7153A humanized IgG1/ thioether

Maytansinoid

B cell malignancies

CD37

AMG595

Anti-EGFRvIII fully human IgG1/thioether

Maytansinoid

Glioblastoma

EGFRvIII

RG7593/DCDT2980S

Hz IgG1/valine-citrulline

MMAE

NHL

CD22

SAR566658

Hu IgG1/SPDB

Maytansine (DM4)

Solid tumors

CA6

Labestuzumab-SN-38

HzIgG1/phenylalanine-lysine

SN38

Colorectal cancer

CD66e/CEACAM5

AGS-16C3F

Hu IgG2/maleimidocaproyl

MMAF

Renal cell carcinoma

ENPP3

SGN-CD33A

Hz

PDB dimer

AML

CD33

SGN-CD19A

Hz IgG1/maleimidocaproyl

MMAF

B cell lymphoma

CD19

SGN-LIV1A

Hz IgG1/V.C

MMAE

Metastatic breast cancer

LIV-1

RG7596

Hz IgG1/V.C

MMAE

NHL

CD79b

ASG-5ME

Hu IgG2/V.C

MMAE

Pancreatic, gastric, an prostate cancers

SLC44A4

BAY 79-4620

Hu IgG1/V.C

MMAE

Advanced solid tumors

CA-IX

AGS-67E

Hu IgG2/V.C

MMAE

Lymphoid malignancies, leukemia

CD37

AMG-172

Hu IgG1/MCC

Maytansine (DM1)

Clear cell renal cell carcinoma, renal cell adenocarcinoma and carcinoma

CD27L

AGS15E

Hu IgG2/[cleavable]

MMAE

Metastatic urothelial cancer

SLITRK6

GSK2857916

Hz IgG1/maleimidocaproyl

MMAF

Multiple myeloma

BCMA

IMGN289

Humanized Anti-EGFR Antibody, J2898A/SMCC

Maytansine (DM1)

EGFR-positive solid tumors

EGFR

AMG 595

Hu anti-EGFRvIII specific IgG1 antibody/SMCC

Maytansine DM1

Advanced malignant glioma,

anaplastic astrocytomas, glioblastoma multiforme

EGFRvIII

IMGN242 (huC242-DM4)

Humanized IgG1/huC242 disulfide

Maytansinoid

Solid tumors

CanAg

Phase I/II

Immunomedics (IMMU)-110 (hLL1-DOX)

Milatuzumab hydrazone

Doxorubicin

Multiple myeloma

CD74

Lorvotuzumab mertansine (IMGN901)

Humanized IgG1/huC242 disulfide

Maytansinoid

Multiple myeloma, solid tumors

CD56

IMMU-132

Hz IgG1/CL2A

CPT-11 SN38

Colorectal cancer, gastric

adenocarcinoma, esophageal cancer, hepatocellular carcinoma

TROP-2

Milatuzumab doxorubicin

Hz IgG1/hydrazone

Doxorubicin

Multiple myeloma

CD74

HuMax® -TF

Hu IgG1/V.C

MMAE

Solid tumors

Tissue factor

Phase II

SAR3419 (huB4-DM4)

huB4/humanized IgG1 disulfide, Hz IgG1/SPDB

DM4

B cell NHL

CD19

BT062

ChIgG4/SPDB, anti-CD138 chimeric IgG4 disulfide

DM4

Multiple myeloma

CD138, Syndecan1

Glembatumumab vedotin (CDX-011)

Hu IgG2/valine-citrullin, anti-CR011 dipeptide

MMAE

Breast cancer melanoma, squamous cell carcinoma of lung

gpNMB

Anti-PSMA ADC

Hu IgG1/V.C

MMAE

Prostate cancer

PSMA

MLN0264

Hu IgG1/V.C

MMAE

Gastrointestinal malignancies

Guanylyl cyclase C

Lorvotuzumab mertansine

Hz IgG1/SPP

DM1

Solid tumors

CD56

PSMA ADC

Anti-PSMA fully human IgG1/dipeptide

Auristatin

Metastatic, hormone-refractory prostate cancer

PSMA

Phase III

Inotuzumab ozogamicin (CMC 544)

Humanized IgG4/G5/44 hydrazone

Calicheamicin

B- cell lymphomas, NHL

CD22

FDA Approved

Gemtuzumab ozogamicin (mylotarg®), Now terminated

Hu IgG4/hydrazone

Calicheamicin

AML

CD33

Trastuzumab-emtansine (Kadcyla®)

HzIgG1 trastuzumab/thioether

DM1

Metastatic breast cancer

HER2

Brentuximab vedotin (Adcetris®)

Ch IgG1/V.C

MMAE

Hodgkin’s lymphoma

CD30

Terminated

LOP628

HzIgG1/(noncleavable)

Maytansine

AML/C-Kit-positive solid tumors

cKit