Skip to main content
. 2022 Mar 9;14(6):1392. doi: 10.3390/cancers14061392

Table 1.

Anti-CAIX monoclonal antibodies-based preclinical studies reporting antitumor responses.

Author Antibody Type Tumor Type Dosage Response
Surfus et al. (1996) [17] cG250 RCC and breast carcinoma cell lines cG250: 0.5 µg/mL,
IL2: 100 U/mL		 ADCC with PBMCs (effector to target rate 100:1) after 4 h
RCC—SK-RC-13: cG250 48%; cG250 + IL2 50%;
SK-RC-30: cG250 25%; cG250 + IL2 65%;
Breast cancer—BT-20: cG250 38%; cG250 + IL2 28%
Liu et al. (2002) [18] cG250 RCC and chronic myelogenous leukemia cG250: 1 µg/mL, IL2 10 IU/mL;
IFNγ, IFN-2a, IFN-2b 1000 IU/mL		 ADCC with PBMC (effector to target rate 25:1) after 2 days
RCC—SK-RC-52: cG250 + IL2 42%; cG250 + IFN-𝛾 33%; cG250 + IFN-𝛼-2a or cG250 + IFN-α-2b 25%;
SK-RC-09: cG250 + IL2 28%; cG250 + IFN-𝛾; cG250 + IFN-𝛼-2a, and cG250 + IFN-α-2b < 10%;
Leukemia—K562: cG250 + IL2 60%; cG250 + IFN-𝛾 30%; cG250 + IFN-𝛼-2a or cG250 + INF-α-2b 43%
Brouwers et al. (2004) [19] 131I-cG250, 90Y-SCN-Bz- DTPA-cG250, 177Lu-SCN-Bz-DTPA-cG250, or 186Re-MAG3 cG250 RCC 30 µg 131I-cG250,
30 µg 90Y-SCN-Bz-DTPA-cG250,
60 µg 177Lu-SCN-Bz-DTPA-cG250, or
35 µg 186Re-MAG3-cG250;
Variable doses of radioisotopes		 Best median survival (SK-RC-52 cells)
177Lu-SCN-Bz-DTPA cG250: 294 days;
90Y-SCN-Bz-DTPA cG250: 241 days;
186Re-MAG3-cG250: 211 days;
131I-cG250: 164 days;
Control groups < 150 days
Bauer et al. (2009) [20] cG250-TNF and cG250 RCC 100 µg of cG250 or cG250-TNF
300 ng every 3 days		 In vivo tumor size after 78 days (SK-RC-52 cells)
cG250-TNF + IFNγ: 60% decrease;
cG250-TNF: 50% decrease;
cG250 + IFNγ: no difference in tumor size
compared to negative control
Zatovicova et al. (2010) [21] VII/20 Colorectal carcinoma 100 μg twice a week In vivo tumor weight/volume reduction (HT-29 cells)
60%/73% treatment initiated
after 10 days of tumor implantation;
88%/93% treatment initiated
in the same day of tumor implantation
Oosterwijk-Wakka et al. (2011) [22] 125I-cG250 + sorafenib, sunitinib, or vandetanib RCC 125I-cG250 185 kBq/5 μg
35 mg/kg of sunitinib,
50 mg/kg of sorafenib,
50 mg/kg of vandetanib		 In vivo tumor volume (NU-12 cells) decrease for continuous treatment (14 days)
Vandetanib: 57%, sunitinib: 49%, and
sorafenib: 37%,
all compared to 125I-cG250 alone
Petrul et al. (2012) [23] BAY 79-4620 Colorectal cancer, gastric carcinoma, and NSCLC-PDX Variable In vivo tumor regression (3 doses of every 4 days)
Colorectal cancer (dose 10 mg/kg): HT-29: 100%, Colo205: 85%;
Gastric carcinoma (dose 60 mg/kg): NCI-N87: 87%, MKN-45: 90%, SNU-16: 75%;
NSCLC-PDX: complete regression in 2/5, partial regression in 3/5
Muselaers et al. (2014) [15] 111In-DOTA-mG250 and 177Lu-DOTA-mG250 RCC 13 MBq 177Lu-DOTA-mG250,
13 MBq nonspecific 177Lu-DOTA-MOPC21,
20 MBq 111In-DOTA-mG250		 Median survival (SK-RC-52 cells)
177Lu-DOTA-mG250: 139 days;
177Lu-DOTA-MOPC21: 49 days;
111In-DOTA-mG250: 53 days;
Control: 49–53 days
Zatovicova et al. (2014) [16] mG250 Colorectal carcinoma 100 µg/dose In vivo tumor weight/volume reduction (HT-29 cells)
Treatment initiated after 10 days
of tumor implantation: 55%/73%;
Treatment initiated at the same day
of tumor implantation: 90%/93%
Chang et al. (2015) [24] In vitro: G10, G36, G37, G39, and G119;
In vivo: only G37 and G119 were tested		 RCC ADCC in vitro: 5 µg/mL,
In vivo: 10 mg/kg		 ADCC in SK-RC-09 cells:
25:1 effector to target cells: 25% for G36 and G119; 15–20% for G10, G37, and G39;
50:1 effector to target cells: 45% for G10, G36, G37, and G119; 30% for G39
In vivo tumor weight (Day 29)/volume (Day 28)
reduction (SK-RC-59 CAIX+ cells):
85%/75% for G37, G119, mG37, and mG119
Oosterwijk-Wakka et al. (2015) [25] 111In-cG250 and Sunitinib RCC 0.4 MBq/5 µg 111In-cG250 three days after administration of 40–50 mg/kg of sunitinib
for 13 days		 In vivo tumor growth reduction 20 days after the beginning of the treatment with sunitinib
NU-12: 60%;
SK-RC-52: not statistically significant compared to control
Yamaguchi et al. (2015) [26] chKM4927 and chKM4927_N297D RCC 10 mg/kg i.p. twice a week for three weeks In vivo tumor volume (VMRC-RCW cells)
reduction after 32 days
chKM4927 and chKM4927_N297D:
60% compared to negative control
Lin et al. (2017) [27] Anti-CAIX functionalized liposomes with TPL Lung cancer cells 0.15 mg/kg once every 3–4 days for 8 times
via pulmonary
delivery		 Median survival time (A549 cells)
CAIX-TPL-Lips: 90 days (statistically significant compared to saline control);
Nontargeted TPL-lips: 71 days (not statistically significant compared to saline control);
Control group: 45 days
De Luca et al. (2019) [28] IL2-Anti-CAIX(XE114)-TNFmut and
IL2-Anti-CAIX(F8)-TNFmut		 Colon Carcinoma 30 µg i.v. four times every 24 h Tumor volume reduction (CT26-CAIX cells) after 18 days
IL2-F8-TNFmut: 58%;
mIL2-F8-mTNFmut: 72%;
IL2-XE114-TNFmut: 63%;
mIL2-XE114-mTNFmut: 50%

ADCC: antibody-dependent cell cytotoxicity, Bz: benzyl, DOTA: 1,4,7,10-tetraazacyclododecane-tetraacetic acid, DTPA: diethylenetriaminepentaacetic acid, I: iodine, IL2: interleukin-2, In: indium, IFN: interferon, Lu: lutetium, MAG3: mercaptoacetyltriglycine, MOPC21: unspecific control antibody, NSCLC-PDX: non-small cell lung cancer patient-derived xenograft, PBMCs: peripheral blood mononuclear cells, RCC: renal cell cancer, Re: rhenium, TNF: tumor necrosis factor, TNFmut: low potency mutated tumor necrosis factor, TPL: triptolide, Y: yttrium.