Combination of CDK4/6 and mTOR Inhibitors Suppressed Doxorubicin-resistant Osteosarcoma in a Patient-derived Orthotopic Xenograft Mouse Model: A Translatable Strategy for Recalcitrant Disease

Anticancer Res. 2021 Jul;41(7):3287-3292. doi: 10.21873/anticanres.15115.

Abstract

Background: Osteosarcoma is the most frequent malignant bone neoplasm. The efficacy of combination therapy of a cyclin-dependent kinase 4/6 (CDK4/6) inhibitor and a mammalian-target-of-rapamycin (mTOR) inhibitor was previously reported in several cancer types. In the present study, we evaluated the efficacy of a combination of palbociclib (CDK 4/6 inhibitor) and everolimus (mTOR inhibitor) on an osteosarcoma patient-derived orthotopic xenograft (PDOX) mouse model.

Materials and methods: osteosarcoma PDOX mouse models were randomized into five treatment groups of seven mice each: Group 1, untreated control; group 2, doxorubicin treatment; group 3, palbociclib treatment; group 4, everolimus treatment; group 5, palbociclib-everolimus combination treatment. Treatment duration was 2 weeks.

Results: The palbociclib-everolimus combination reduced the tumor-volume ratio in the osteosarcoma PDOX mouse model compared with the control and doxorubicin (p=0.018). Everolimus alone also inhibited osteosarcoma PDOX growth compared to the control (p=0.04), but less than the combination. Palbociclib alone and doxorubicin were ineffective. There were no significant body-weight losses in any group. Only the palbociclib-everolimus combination induced extensive tumor necrosis observed histopathologically.

Conclusion: The present study demonstrated that the combination of CDK4/6 and mTOR inhibitors can be a translatable approach for doxorubicin-resistant osteosarcoma in the clinic.

Keywords: CDK4/6 inhibitor; Osteosarcoma; PDOX; cell cycle; everolimus; mTOR inhibitor; palbociclib; patient-derived orthotopic xenograft.

MeSH terms

  • Adolescent
  • Animals
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology*
  • Bone Neoplasms / drug therapy*
  • Bone Neoplasms / metabolism
  • Cyclin-Dependent Kinase 4 / antagonists & inhibitors*
  • Cyclin-Dependent Kinase 6 / antagonists & inhibitors*
  • Disease Models, Animal
  • Doxorubicin / pharmacology
  • Drug Resistance, Neoplasm / drug effects*
  • Everolimus / pharmacology
  • Female
  • Humans
  • Mice
  • Mice, Nude
  • Osteosarcoma / drug therapy*
  • Osteosarcoma / metabolism
  • Piperazines / pharmacology
  • Protein Kinase Inhibitors / pharmacology
  • Pyridines / pharmacology
  • TOR Serine-Threonine Kinases / antagonists & inhibitors*
  • Tumor Burden / drug effects
  • Xenograft Model Antitumor Assays

Substances

  • Piperazines
  • Protein Kinase Inhibitors
  • Pyridines
  • Doxorubicin
  • Everolimus
  • MTOR protein, human
  • TOR Serine-Threonine Kinases
  • CDK4 protein, human
  • CDK6 protein, human
  • Cyclin-Dependent Kinase 4
  • Cyclin-Dependent Kinase 6
  • palbociclib