Table 4 TGF-β-targeted therapies in cancer
From: TGF-β signaling in the tumor metabolic microenvironment and targeted therapies
Agent | Target | Treatment | Application | Experiment status | Clinical outcome | Clinical trial |
|---|---|---|---|---|---|---|
Small-molecule inhibitor | ||||||
Galunisertib | TGFβRI | Combination with durvalumab | Pancreatic cancer | I; Completed | Had acceptable tolerability and safety | NCT02734160 |
Combination with nivolumab | NSCLC and HCC | I/II; Completed | Some patients exhibited complete or partial remission | NCT02423343 | ||
LY3200882 | TGFβRI | Combination with pembrolizumab | Advanced cancer | Ib/II; Withdrawn | No results posted | NCT04158700 |
Combination with capecitabine | Colorectal cancer | I/II; Not yet recruiting | No results posted | NCT04031872 | ||
Vactosertib | TGFβRI | Monotherapy | Solid tumor | I; Completed | No results posted | NCT02160106 |
Combination with pembrolizumab | NSCLC | II; Recruiting | No results posted | NCT04515979 | ||
PF06952229 | TGFβRI | Monotherapy/Combination with enzalutamide | Solid tumor | I; Terminated | No results posted | NCT03685591 |
TEW-7197 | TGFβRI ALK5 | Monotherapy | Solid tumor | I; Completed | No results posted | NCT02160106 |
Combination with FOLFOX | Pancreatic cancer | I/II; Recruiting | No results posted | NCT03666832 | ||
Neutralizing antibody | ||||||
Fresolimumab | TGFβ1/2/3 | Monotherapy | MPM | II; Completed | 3 patients (out of 13) showed stable disease | NCT01112293 |
Combination with radiotherapy | BC | II; Completed | Suppressed tumor | NCT01401062 | ||
NIS793 | TGFβ1/2/3 | Combination with chemotherapy | PDAC | III; Recruiting | No results posted | NCT04935359 |
Combination with PDR001 | Advanced malignancies | I; Completed | No results posted | NCT02947165 | ||
SAR439459 | TGFβ1/2/3 | Monotherapy/Combination with cemiplimab | Solid tumor | I; Terminated | No results posted | NCT03192345 |
Monotherapy/Combination with novel agents in RRMM | Plasma cell myeloma | I/II; Recruiting | No results posted | NCT04643002 | ||
SRK181 | TGFβ1 | Monotherapy/Combination with anti-PD-(L)1 antibody | Solid tumor | I; Recruiting | No results posted | NCT04291079 |
ABBV151 | GARP-TGFβ1 | Monotherapy/Combination with ABBV-181 | Solid tumor | I; Recruiting | No results posted | NCT03821935 |
LY3022859 | TGFβRII | Monotherapy | Solid tumor | I; Completed | The maximum tolerated dose was not determined | NCT01646203 |
Luspatercept | TGFβ1/2/3 | Monotherapy | MDS | II; Completed | Was well tolerated and effective | NCT02268383 |
Monotherapy | MDS | III; Completed | Reduced the severity of anemia | NCT02631070 | ||
AVID200 | TGFβ1/3 | Monotherapy | Solid tumor | I; Active, not recruiting | No results posted | NCT03834662 |
M7824 | TGFβ1/2/3 and PD-L1 | Monotherapy | NSCLC | III | No significant improvement of OS | NCT03631706 |
Monotherapy | metastatic BTC | II/III | No results posted | NCT04066491 | ||
Combination with chemotherapy | NSCLC | I/II; Completed | No results posted | NCT03840915 | ||
Monotherapy | BC | I; Completed | No results posted | NCT03524170 | ||
Antisense oligonucleotide | ||||||
AP12009 | TGFβ2 mRNA | Monotherapy | Pancreatic cancer, melanoma and CRC | I; Completed | No results posted | NCT00844064 |
Monotherapy | GBM | II; Completed | No results posted | NCT00431561 | ||
Vaccine | ||||||
Lucanix | TGFβ2 | Monotherapy | NSCLC | II; Completed | No results posted | NCT01058785 |
Monotherapy | NSCLC | III; Completed | No results posted | NCT00676507 | ||
Vigil ™ | TGFβ1/2 | Combination with pembrolizumab | Advanced melanoma | I; Completed | No results posted | NCT02574533 |
Monotherapy/Combination with temozolomide and irinotecan | Ewing's Sarcoma | II; Completed | Reduce disease burden | NCT02511132 | ||
Integrin inhibitor | ||||||
Cilengitide | Integrins αvβ3 and αvβ5 | Monotherapy | Prostate cancer | II; Completed | Had good tolerance but no detectable clinical activity | NCT00121238 |
Monotherapy | HNSCC | I/II; Completed | No significant effect | NCT00705016 | ||
SF1126 | Integrin-targeted PI3 kinase | Monotherapy | Solid tumor | I; Completed | No results posted | NCT00907205 |
Monotherapy | HNSCC | II; Terminated | No data available | NCT02644122 | ||
IMGN388 | Integrin αv | Monotherapy | Solid tumor | I; Completed | No results posted | NCT00721669 |
Abergrin | Integrin αvβ3 | Monotherapy | MM | I; Completed | No results posted | NCT00111696 |
Volociximab | Integrin α5β1 | Combination with gemcitabine | Pancreatic cancer | II; Completed | No results posted | NCT00401570 |