| Compound |
Class |
Targets |
Clinical Status |
References |
| |
|
|
|
|
| H90
(anti-CD44) |
Mouse IgG1 mAb |
Acute myeloid leukemia (AML) SCs |
Preclinical, xenograft mice |
[70] |
| P245
(anti-CD44) |
Mouse IgG1 mAb |
Breast CSCs |
Preclinical, xenograft mice |
[77] |
| H4C4
(anti-CD44) |
Mouse IgG1 mAb |
Pancreatic CSCs |
Preclinical, xenograft mice |
[83] |
| GV5
(anti-variant 8-epitope of CD44R1) |
Human recombinant IgG1 mAb |
Uterine cervix and larynx CSCs |
Preclinical, xenograft mice |
[84] |
| RO5429083
(anti-CD44; targets a glycosylated, conformation-dependent epitope of CD44) |
Humanized recombinant IgG1 mAb |
Head and neck squamous cell carcinoma |
Preclinical, xenograft mice |
[86] |
| |
|
Patients with metastatic and/or locally advanced, CD44-expressing malignant solid tumors |
Phase I clinical study |
[88] |
| |
|
Patients with AML |
Phase I clinical study; RO5429083
alone or in combination with cytarabine |
[89] |
| B6H12.2
(anti-CD47, blocking) |
Mouse IgG1mAb |
AML SCs,
bladder CSCs,
glioblastoma CSCs,
colon CSCs |
Preclinical, xenograft mice |
[100]
[101]
[102] |
| |
|
Ovarian, breast, colon, bladder, prostate, hepatocellular, lung, kidney and gastric carcinomas, head and neck squamous cell carcinoma, sarcomas and glioblastomas |
Preclinical, xenograft mice |
[100] |
| |
|
Non-Hodgkin lymphoma,
acute lymphoblastic leukemia, multiple myeloma |
Preclinical,
xenograft mice |
[97]
[103]
[104]
[105] |
| B6H12
(anti-CD47, blocking) |
Humanized IgG1 mAb |
Aggressive metastatic leiomyosarcoma |
Preclinical, xenograft mice |
[107] |
| 7G3 (anti-CD123)
|
Mouse IgG2a mAb |
AML SCs |
Preclinical, xenograft mice |
[111] |
| CSL360
(anti-CD123) |
Humanized recombinant chimeric IgG1 mAb |
Patients with relapsed, refractory or high risk AML |
Phase I clinical study |
[113] |
| CSL362
(anti-CD123) |
Humanized recombinant chimeric IgG1 mAb |
Patients with AML in remission |
Phase I clinical study |
[114] |
| Fusion of anti-CD123 scFv and anti-CD3 scFv |
BiTE;
human recombinant bispecific mAb construct, |
AML blasts and AML SCs |
Preclinical,
in vitro |
[115] |
| Fusion of anti-CD123 scFv, anti-CD33 scFv and anti-CD16 scFv |
Human recombinant trispecific mAb construct |
Primary AML cells |
Preclinical,
in vitro |
[116] |
| 111In-NLS-7G3
(anti-CD123 7G3 modified with 13-mer peptides harboring the nuclear translocation sequence of SV-40 large T-antigen, and labelled with 111Indium) |
Mouse IgG2a mAb, labelled with nuclear translocation sequence of SV-40 large T-antigen, and 111Indium |
Primary AML cells |
Preclinical, xenograft mice |
[117] |
MT110
(Solitomab)
(anti-EpCAM/
anti-CD3) |
BiTE;
human recombinant single-chain bispecific bifunctional mAb construct |
Breast CSCs,
liver CSCs,
colon CSCs,
pancreatic CSCs
|
Preclinical,
xenograft mice.
Phase I clinical study,
advanced solid tumors |
[128]
[129]
[130]
[131]
[132] |
Catumaxomab
(Removab)
(anti-EpCAM/
anti-CD3/Fcγ) |
Triomab; recombinant chimeric two half antibody, each with one light and one heavy chain from mouse IgG2a and rat IgG2b isotypes. Bispecific, trifunctional mAb construct |
CSCs in malignant ascites from metastatic human ovarian, gastric and pancreatic cancer.
Patients with non-small cell lung cancer, and epithelial cancers |
Phase I-III clinical studies,
malignant pleural effusions, malignant ascites,
peritoneal carcinomatosis. Non-small cell lung cancer, ovarian, gastric and epithelial cancer, intraperitoneal administration.
Phase I clinical studies,
lung cancer,
epithelial cancers, intravenous administration |
[139]
[140]
[141]
[142]
[144]
[145] |
AVE1642
(anti-IGF-IR) |
Humanized recombinant IgG1 mAb, derived from mouse anti-IGF-IR IgG1mAb EM164 |
Myeloma cell lines
colon CSCs.
Patients with relapsed multiple myeloma and advanced solid tumors |
Preclinical,
in vitro,
xenograft mice.
Phase I clinical study, relapsed multiple myeloma, advanced solid tumors
|
[159]
[157]
[153]
[154] |
Figitumumab
(CP-751,871)
(anti-IGF-IR) |
Humanized recombinant IgG2 mAb |
Colon CSCs.
Patients with non-small cell lung cancer and other solid tumors |
Preclinical,
in vitro,
xenograft mice.
Phase I-III clinical study, patients with non-small cell lung cancer and other solid tumors |
[159]
[161]
[159]
[158]
[150]
[162] |
Demcizumab
(OMP-12M18)
(anti-Dll4) |
Humanized recombinant IgG mAb |
Colon CSCs,
breast CSCs,
colon cancer cells with KRAS mutations,
pancreatic CSCs,
melanoma CSCs,
triple-negative breast cancer cells |
Preclinical,
xenograft mice.
Phase I clinical study, single-agent, patients with solid tumors.
Phase I clinical studies, combination with cytostatic drugs, in patients with colorectal cancer, pancreatic cancer and non-small cell lung cancer |
[57]
[58]
[59]
[60]
[169]
[170]
[171]
[172-175]
|
OMP-18R5
(anti-Frizzled 1, 2, 5, 7, 8) |
Humanized recombinant IgG2 mAb |
Pancreatic CSCs,
breast CSCs,
colon cancer cells,
breast cancer cells,
lung cancer cells,
pancreatic cancer cells
Patients with solid tumors |
Preclinical,
xenograft mice.
Phase I clinical study in patients with solid tumors |
[61]
[62]
[63]
[182] |
