Biomarkers and overall survival in patients with advanced hepatocellular carcinoma treated with TGF-βRI inhibitor galunisertib

PLoS One. 2020 Mar 25;15(3):e0222259. doi: 10.1371/journal.pone.0222259. eCollection 2020.

Abstract

Background: Transforming growth factor beta (TGF-β) signalling is involved in the development of hepatocellular carcinoma (HCC). We followed changes in biomarkers during treatment of patients with HCC with the TGF-βRI/ALK5 inhibitor galunisertib.

Methods: This phase 2 study (NCT01246986) enrolled second-line patients with advanced HCC into one of two cohorts of baseline serum alpha-fetoprotein (AFP): Part A (AFP ≥1.5x ULN) or Part B (AFP <1.5x ULN). Baseline and postbaseline levels of AFP, TGF-β1, E-cadherin, selected miRNAs, and other plasma proteins were monitored.

Results: The study enrolled 149 patients (Part A, 109; Part B, 40). Median OS was 7.3 months in Part A and 16.8 months in Part B. Baseline AFP, TGF-β1, E-cadherin, and an additional 16 plasma proteins (such as M-CSF, IL-6, ErbB3, ANG-2, neuropilin-1, MIP-3 alpha, KIM-1, uPA, IL-8, TIMP-1, ICAM-1, Apo A-1, CA-125, osteopontin, tetranectin, and IGFBP-1) were found to correlate with OS. In addition, a range of miRs were found to be associated with OS. In AFP responders (21% of patients in Part A with decrease of >20% from baseline) versus non-responders, median OS was 21.5 months versus 6.8 months (p = 0.0015). In TGF-β1 responders (51% of all patients) versus non-responders, median OS was 11.2 months versus 5.3 months (p = 0.0036).

Conclusions: Consistent with previous findings, both baseline levels and changes from baseline of circulating AFP and TGF-β1 function as prognostic indicators of survival. Future trials are needed to confirm and extend these results.

Publication types

  • Clinical Trial, Phase II
  • Multicenter Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Antigens, CD / blood
  • Biomarkers, Tumor / blood
  • Cadherins / blood
  • Carcinoma, Hepatocellular / blood
  • Carcinoma, Hepatocellular / drug therapy*
  • Carcinoma, Hepatocellular / mortality*
  • Cohort Studies
  • Female
  • Humans
  • Liver Neoplasms / blood
  • Liver Neoplasms / drug therapy*
  • Liver Neoplasms / mortality*
  • Male
  • MicroRNAs / blood
  • Middle Aged
  • Prognosis
  • Pyrazoles / pharmacology*
  • Pyrazoles / therapeutic use*
  • Quinolines / pharmacology*
  • Quinolines / therapeutic use*
  • Receptor, Transforming Growth Factor-beta Type I / antagonists & inhibitors*
  • Survival Rate
  • Transforming Growth Factor beta1 / analysis
  • Treatment Outcome
  • alpha-Fetoproteins / analysis

Substances

  • AFP protein, human
  • Antigens, CD
  • Biomarkers, Tumor
  • CDH1 protein, human
  • Cadherins
  • MicroRNAs
  • Pyrazoles
  • Quinolines
  • TGFB1 protein, human
  • Transforming Growth Factor beta1
  • alpha-Fetoproteins
  • LY-2157299
  • Receptor, Transforming Growth Factor-beta Type I
  • TGFBR1 protein, human

Associated data

  • ClinicalTrials.gov/NCT01246986

Grants and funding

This study was funded by Eli Lilly and Company, Indianapolis, IN, USA (www.lilly.com). Employees of Eli Lilly and Company designed the study, analyzed the data, were authors on the manuscript, and approved the manuscript for publication.