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. 2021 Dec 24;11:785111. doi: 10.3389/fonc.2021.785111

Table 2.

Drug clinical trials with HIF-1α inhibitors.

Agent Disease/cases Combined with other agent(s) Outcome Ref.

  • 2ME2

  • Prostate cancer/21

  • none

  • PFS-6 mo:5.35%

  • Ovarian cancer/18

  • none

  • ORR:0; SD:38.89%

  • Renal cell cancer/12

  • Arm A: +sunitinib malate

  • SD:57%

  • Arm B: +none

  • SD:60%

  • Tanespimycin

  • Renal cell cancer/20

  • none

  • CR or PR:0; SD:70%

  • Prostate cancer/15

  • none

  • PSA PFS:1.8 mo

  • Vorinostat

  • Renal cell cancer/33

  • bevacizumab

  • OR:18%; PFS-6 mo:48%; PFS:5.7 mo; OS: 13.9 mo

  • Melanoma/32

  • none

  • PR:6%; SD:50%

  • EZN-2968

  • Refractory advanced solid tumour/10

  • none

  • Decreased HIF-1α at mRNA level:5;

  • Decreased HIF-1α at protein level:3

  • Hepatocellular cancer/9

  • none

  • Decreased HIF-1α at mRNA level in patients had SD and PR

  • SD:11.1%

  • PR:11.1%

  • EZN-2208

  • Colorectal cancer/211

  • Arm A: +none

  • No radiographic response were observed

  • Arm B: +cetuximab

  • OR:8%; PFS: 4.9 mo; OS:9.8 months; PFS-6 mo:37%

  • Arm C: irinotecan+cetuximab

  • OR:5%; PFS: 3.7 mo; OS:9.1 months; PFS-6 mo:29%

  • CRXL101

  • Renal cell cancer/111

  • Arm A: bevacizumab

  • PFS: 3.7 mo

  • Arm B: other agents

  • PFS: 3.9 mo

  • Ovarian cancer/63

  • Arm A: none

  • ORR: 11%; PFS: 4.5 mo

  • Arm B: +bevacizumab

  • ORR: 18%; PFS: 6.5 mo

PFS, progression-free survival; mo, months; PFS-6 mo, progression-free survival at 6 months; ORR, overall response rate; CR, complete response; PR, partial response.