Inhibition of DNA-PK with AZD7648 Sensitizes Tumor Cells to Radiotherapy and Induces Type I IFN-Dependent Durable Tumor Control

Clin Cancer Res. 2021 Aug 1;27(15):4353-4366. doi: 10.1158/1078-0432.CCR-20-3701. Epub 2021 May 19.

Abstract

Purpose: Combining radiotherapy (RT) with DNA damage response inhibitors may lead to increased tumor cell death through radiosensitization. DNA-dependent protein kinase (DNA-PK) plays an important role in DNA double-strand break repair via the nonhomologous end joining (NHEJ) pathway. We hypothesized that in addition to a radiosensitizing effect from the combination of RT with AZD7648, a potent and specific inhibitor of DNA-PK, combination therapy may also lead to modulation of an anticancer immune response.

Experimental design: AZD7648 and RT efficacy, as monotherapy and in combination, was investigated in fully immunocompetent mice in MC38, CT26, and B16-F10 models. Immunologic consequences were analyzed by gene expression and flow-cytometric analysis.

Results: AZD7648, when delivered in combination with RT, induced complete tumor regressions in a significant proportion of mice. The antitumor efficacy was dependent on the presence of CD8+ T cells but independent of NK cells. Analysis of the tumor microenvironment revealed a reduction in T-cell PD-1 expression, increased NK-cell granzyme B expression, and elevated type I IFN signaling in mice treated with the combination when compared with RT treatment alone. Blocking of the type I IFN receptor in vivo also demonstrated a critical role for type I IFN in tumor growth control following combined therapy. Finally, this combination was able to generate tumor antigen-specific immunologic memory capable of suppressing tumor growth following rechallenge.

Conclusions: Blocking the NHEJ DNA repair pathway with AZD7648 in combination with RT leads to durable immune-mediated tumor control.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor / radiation effects*
  • DNA-Activated Protein Kinase / antagonists & inhibitors*
  • Interferon Type I / drug effects*
  • Mice
  • Neoplasms / radiotherapy*
  • Protein Kinase Inhibitors / pharmacology*
  • Purines / pharmacology*
  • Pyrans / pharmacology*
  • Radiation-Sensitizing Agents / pharmacology*
  • Triazoles / pharmacology*

Substances

  • AZD7648
  • Interferon Type I
  • Protein Kinase Inhibitors
  • Purines
  • Pyrans
  • Radiation-Sensitizing Agents
  • Triazoles
  • DNA-Activated Protein Kinase