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]
Table 1: Antibodies and antibody constructs that target human CSCs.