Table S1. Clinical trials involving chemical immunoconjugates
Conjugate
Clinical
trial
identifier
NCT01100502
NCT00848926
NCT01352520
NCT00866047
NCT00430846
NCT00947856
NCT01026415
NCT01060904
NCT01309789
NCT01026233
NCT01100502
NCT00704158
NCT00412828
NCT01156753
Drug
Target
Stage
Cancer
Effects
monometil
auristatin
E
(MMAE)
CD30
I, II, III
Relapsed or Refractory HL,
Relapsed or Refractory ALCL,
Relapsed or Refractory NHL,
Mycosis Fungoides,
Extensive
Lymphomatoid
Papulosis (LyP)
1-4
monomethyl
auristatin
E
(MMAE)
GPNMB
I, II
4, 5
ASG-5ME
NCT01228760
NCT01166490
SLC44A4
(AGS-5)
I
BAY79-4620
NCT01028755
NCT01065623
Advanced Solid Tumors
Not
yet
available
NCT01015911
Carbonic
anhydrase IX
(CAIX)
CD70
I
SGN-75
I
NCT01114230
AGS-16
I
Relapsed or Refractory NHL,
Metastatic
Renal
Cell
Carcinoma
Advanced
Renal
Cell
Carcinoma
Not
yet
available
AGS-16M8F
Trastuzumab
emtansine
NCT00932373
NCT00679341
NCT00875979
NCT00928330
NCT00951665
NCT00829166
NCT01120561
NCT00943670
NCT00679211
NCT00509769
NCT00781612
NCT01120184
NCT00721669
monomethyl
auristatin
E
(MMAE)
monomethyl
auristatin
E
(MMAE)
monomethyl
auristatin
F
(MMAF)
monomethyl
auristatin
F
(MMAF)
maytansinoid
DM1
Locally Advanced or Metastatic
Breast Cancer,
Unresectable Stage III or Stage
IV Melanoma
Advanced Prostate Cancer,
Pancreatic Adenocarcinoma
HER2
I, II, III
Metastatic Breast Cancer
4, 6, 7
maytansinoid
DM4
maytansinoid
DM4
maytansinoid
DM4
Integrin
I
Solid Tumors
8
CD138
I, II
4
CD33
I
maytansinoid
DM4
CD19
I
SAR566658
NCT00539682
NCT00796731
NCT00549185
NCT01156870
Relapsed/Refractory Multiple
Myeloma
Recurrent Ovarian, Prostate,
Colorectal or Non-Small Cell
Lung Cancers
Refractory Epithelial Cancer
Relapsed/Refractory NHL
maytansinoid
DM4
CA6
I
Not
yet
available
BIIB015
NCT00674947
Cripto
I
AMG386
NCT00770536
NCT00861419
NCT00807859
NCT01204749
NCT00511459
NCT01253681
NCT01331941
NCT00752570
NCT01281254
maytansinoid
DM4
peptide-Fc
fusion protein
(peptibody)
Angiopoietin1
and
Angiopoietin2
I, II, III
CA6-expressing Cancers (many
breast, ovarian, cervical, lung
and pancreatic tumors)
Relapsed or Refractory Solid
Tumors
Advanced Recurrent Epithelial
Ovarian Cancer,
Advanced Solid Tumors,
HER2-positive
Locally
Recurrent or Metastatic Breast
Cancer,
Recurrent Primary Peritoneal or
Fallopian Tube Cancers,
Her2-Negative, Metastatic or
Brentuximab
vedotin (SGN35)
CDX-011
(CR011vcMMAE)
IMGN388
BT-062
EMD 273066
SAR3419
NCT01001442
NCT00723359
NCT00132522
NCT00016237
Not
yet
available
Not
yet
available
9
10
Not
yet
available
11-13
NCT00853372
NCT00583674
NCT00872014
NCT00102830
NCT00479817
NCT00467025
NCT01210222
NCT01249521
NCT01290263
NCT01042379
Locally
Recurrent
Breast
Cancer,
Metastatic
Colorectal
Carcinoma,
Metastatic
Clear
Cell
Carcinoma of the Kidney,
Metastatic
Gastric,
Gastroesophageal Junction, or
Distal
Esophageal
Adenocarcinoma,
Advanced
or
Inoperable
Hepatocellular Carcinoma,
Persistent/Recurrent Carcinoma
of the Endometrium,
Recurrent Glioblastoma
Small Cell Lung Cancer,
Relapsed
and
Relapsed
Refractory
CD56-Positive
Multiple Myeloma,
14, 15
NCT00065429
NCT00346255
NCT00346385
NCT01237678
NCT00991562
NCT00868608
NCT01055496
NCT00867087
NCT00724971
NCT01363297
NCT01232556
NCT00073749
NCT00717925
NCT00299494
NCT01134575
NCT01371630
mertasine
CD56
I, II
calicheamicin
CD22
I, II, III
Milatuzumabdoxorubicin
(hLL1-DOX )
NCT01101594
Doxorubicin
CD74
I, II
Multiple Myeloma
Not
yet
available
MDX-1203
NCT00944905
CD70
I
47 clinical trials
in
clinicaltrials.go
v
VEGF
I, II, III
Advanced/Recurrent Clear Cell
Renal Cell Carcinoma,
Relapsed/Refractory
B-Cell
NHL
Relapsed
or
Refractory
Advanced Solid Tumors,
Relapsed
or
Refractory
Advanced NHL,
Malignant
Glioma,
Gliosarcoma,
Glioblastoma
multiforme,
Advanced
Refractory,
Relapsed, or Untreated AML
Not
yet
available
Aflibercept
DNA
alkylating
cytotoxic
Drug A
VEGFR-1 and
VEGFR-2
Lorvotuzumab
mertansine
(BB10901/IMG
N901)
Inotuzumab
ozogamicin
(CMC-544)
NHL,
Relapsed/Refractory
Positive DLBCL
4, 16, 17
CD22-
18
AML = Acute Myeloid Leukaemia; ALCL = Anaplastic Large-Cell Lymphoma; DLBCL = Diffuse
Large B-Cell Lymphoma; HL = Hodgkin’s Lymphoma; NHL = Non-Hodgkin’s Lymphoma
References
1.
Deutsch YE, Tadmor T, Podack ER, et al. CD30: an important new target in hematologic
malignancies. Leuk Lymphoma 2011.
2.
Younes A, Bartlett NL, Leonard JP, et al. Brentuximab vedotin (SGN-35) for relapsed
CD30-positive lymphomas. N Engl J Med 2010;363:1812-21.
3.
Brentuximab vedotin. Drugs R D 2011;11:85-95.
4.
Beck A, Senter PD, Chari RJ. World Antibody Drug Conjugate Summit Europe: February
21-23, 2011; Frankfurt, Germany. MAbs 2011;3.
5.
Naumovski L, Junutula JR. Glembatumumab vedotin, a conjugate of an anti-glycoprotein
non-metastatic melanoma protein B mAb and monomethyl auristatin E for the treatment of
melanoma and breast cancer. Curr Opin Mol Ther 2010;12:248-57.
6.
Burris HA. Trastuzumab emtansine: a novel antibody-drug conjugate for HER2-positive
breast cancer. Expert Opin Biol Ther 2011;11:807-19.
7.
Niculescu-Duvaz I. Trastuzumab emtansine, an antibody-drug conjugate for the treatment of
HER2+ metastatic breast cancer. Curr Opin Mol Ther 2010;12:350-60.
8.
ImmunoGen. ImmunoGen, Inc. Announces Encouraging IMGN388 Clinical Data Reported
at ASCO. 2010. Available at: http://phx.corporate-ir.net/phoenix.zhtml?c=97573&p=irolnewsArticle&ID=1435268&highlight=.
9.
Ko YJ, Bubley GJ, Weber R, et al. Safety, pharmacokinetics, and biological
pharmacodynamics of the immunocytokine EMD 273066 (huKS-IL2): results of a phase I trial in
patients with prostate cancer. J Immunother 2004;27:232-9.
10.
Coiffier B, Ribrag V, Dupuis J, et al. Phase I/II study of the anti-CD19 maytansinoid
immunoconjugate SAR3419 administered weekly to patients with relapsed/refractory B-cell NonHodgkin's Lymphoma (NHL). Asco Annual Meeting. June 2011. abstract 8017.
11.
Mita AC, Takimoto CH, Mita M, et al. Phase 1 study of AMG 386, a selective angiopoietin
1/2-neutralizing peptibody, in combination with chemotherapy in adults with advanced solid
tumors. Clin Cancer Res 2010;16:3044-56.
12.
Herbst RS, Hong D, Chap L, et al. Safety, pharmacokinetics, and antitumor activity of AMG
386, a selective angiopoietin inhibitor, in adult patients with advanced solid tumors. J Clin Oncol
2009;27:3557-65.
13.
Amgen. Updated AMG 386 Data Demonstrate Promising Antitumor Activity in Patients
With Recurrent Ovarian Cancer. 2010. Available at:
http://wwwext.amgen.com/media/media_pr_detail.jsp?year=2010&releaseID=1480835.
14.
ImmunoGen. ImmunoGen, Inc. Announces Presentation of Encouraging Clinical Data for
Lorvotuzumab Mertansine at ESMO Annual Meeting. 2010.
15.
ImmunoGen. Lorvotuzumab mertansine. 2011. Available at:
http://www.immunogen.com/wt/page/IMGN901b.
16.
Advani A, Coiffier B, Czuczman MS, et al. Safety, pharmacokinetics, and preliminary
clinical activity of inotuzumab ozogamicin, a novel immunoconjugate for the treatment of B-cell
non-Hodgkin's lymphoma: results of a phase I study. J Clin Oncol 2010;28:2085-93.
17.
Ogura M, Tobinai K, Hatake K, et al. Phase I study of inotuzumab ozogamicin (CMC-544)
in Japanese patients with follicular lymphoma pretreated with rituximab-based therapy. Cancer Sci
2010;101:1840-5.
18.
Teng LS, Jin KT, He KF, et al. Clinical applications of VEGF-trap (aflibercept) in cancer
treatment. J Chin Med Assoc 2010;73:449-56.
Table S1: Details of the clinical trials involving chemical immunoconjugates (data gathered from US
clinicaltrials.gov, Clinical Trials register EU and available bibliography in sponsor an PubMed websites).