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. 2023 Apr 2;43(5):525–561. doi: 10.1002/cac2.12416

TABLE 2.

Existing anticancer signaling and immune checkpoint inhibitory molecules in clinical trials.

Treatment Drugs/regimen Condition or disease Target Clinical Trial No. Phase
Chemotherapy Leflunomide smoldering multiple myeloma Dihydroorotate dehydrogenase NCT05014646 Phase 2
Pemetrexed Non‐Small Cell Lung Cancer Glycinamide ribonucleotide formyltransferase NCT00102804 Phase 3
Metformin Hydrochloride HER2‐positive breast cancer MAP kinase, Akt, mTOR NCT03238495 Phase 2
AZD3965 Burkitt Lymphoma, Diffuse Large B Cell Lymphoma, Adult Solid Tumor Monocarboxylate transporter 1 NCT01791595 Phase 1
L‐asparaginase Pancreatic Adenocarcinoma Metastatic Asparagine synthetase NCT02195180 Phase 2
Methotrexate primary CNS lymphoma Dihydrofolate reductase NCT04609046 Phase 1
5‐Fluorouracil Metastatic Pancreatic Cancer Thymidylate synthase NCT02620800 Phase 1
Hydroxyurea Leukemia Ribonucleotide reductase NCT05005182 Phase 2
6‐Mercaptopurine Acute Lymphoblastic Leukemia Phosphoribosyl pyrophosphate amidotransferase NCT01503632 Phase 3
Enasidenib/AG‐221 Hematologic Neoplasms Isocitrate dehydrogenase 2 NCT01915498 Phase 1/2
CB‐839 Non‐Small Cell Lung Cancer Glutaminase NCT04250545 Phase 1
Immunotherapy Pembrolizumab Colorectal cancer PD‐1 NCT02563002 Phase 3
Nivolumab Melanoma PD‐1/PD‐L1 NCT01721772 Phase 3
Cemiplimab NSCLC PD‐1/PD‐L1 NCT03088540 Phase 3
Nivolumab, Ipilimumab combined with chemotherapy NSCLC PD‐L1 NCT03215706 Phase 3
TSR‐022+Nivolumab combined with chemotherapy Advanced solid tumors TIM‐3/PD‐1 NCT02817633 Phase 1
Atezolizumab + Carboplatin + Etoposide SCLC PD‐L1 NCT02763579 Phase 3
Varlilumab and nivolumab Recurrent glioblastoma Anti‐CD27 and anti‐PD‐1 NCT02335918 Phase 1/2
Atezolizumab combination Nab‐Paclitaxel Breast cancer PD‐L1 NCT02425891 Phase 3
Pembrolizumab and vorinostat combined with temozolomide New diagnosis GBM PD‐L1 NCT03426891 Phase 1
Pembrolizumab and Bevacizumab Recurrent glioblastoma PD‐1 and VEGF NCT02337491 Phase 2
Tremelimumab and durvalumab in combination or alone Malignant Glioma, Recurrent Glioblastoma CTLA4 and PDL1 NCT02794883 Phase 2
Nivolumab and ipilimumab Mesothelioma PD‐L1 NCT02899299 Phase 3
Atezolizumab + Bevacizumab Hepatocellular Carcinoma PD‐L1 NCT03434379 Phase 3
ICT‐121 DC vaccine Recurrent gliomas Dendritic cell Vaccine NCT02049489 Phase 1
MBG453 Hematologic malignancy TIM‐3 NCT03066648 Phase 1
LY3321367 Advanced solid tumors TIM‐3 NCT03099109 Phase 1
TTF(Optune), Nivolumab Plus/Minus Ipilimumab Recurrent glioblastoma PD‐1/PD‐L1 NCT03430791 Phase 2
Atezolizumab combination with Cobimetinib + Vemurafenib Melanoma PD‐L1/BRAF kinase NCT02908672 Phase 3
Nivolumab Recurrent or progressive IDH‐mutant gliomas PD‐1/PD‐L1 NCT03557359 Phase 2
IMP321 (anti‐LAG‐3) + Pembrolizumab Melanoma LAG‐3/PD‐1 NCT02676869 Phase 1
IMP321 (anti‐LAG‐3) + Paclitaxel Breast cancer LAG‐3/PD‐1 NCT02614833 Phase 2
BMS‐986016 + Nivolumab Melanoma LAG‐3/PD‐1 NCT05002569 Phase 3
Favezelimab/Pembrolizumab Colorectal cancer LAG‐3/PD‐1 NCT05064059 Phase 3