Novel CAD-ALK gene rearrangement is drugable by entrectinib in colorectal cancer

Br J Cancer. 2015 Dec 22;113(12):1730-4. doi: 10.1038/bjc.2015.401. Epub 2015 Dec 3.

Abstract

Background: Activated anaplastic lymphoma kinase (ALK) gene fusions are recurrent events in a small fraction of colorectal cancers (CRCs), although these events have not yet been exploited as in other malignancies.

Methods: We detected ALK protein expression by immunohistochemistry and gene rearrangements by fluorescence in situ hybridisation in the ALKA-372-001 phase I study of the pan-Trk, ROS1, and ALK inhibitor entrectinib. One out of 487 CRCs showed ALK positivity with a peculiar pattern that prompted further characterisation by targeted sequencing using anchored multiplex PCR.

Results: A novel ALK fusion with the carbamoyl-phosphate synthetase 2, aspartate transcarbamylase, and dihydroorotase (CAD) gene (CAD-ALK fusion gene) was identified. It resulted from inversion within chromosome 2 and the fusion of exons 1-35 of CAD with exons 20-29 of ALK. After failure of previous standard therapies, treatment of this patient with the ALK inhibitor entrectinib resulted in a durable objective tumour response.

Conclusions: We describe the novel CAD-ALK rearrangement as an oncogene and provide the first evidence of its drugability as a new molecular target in CRC.

Publication types

  • Case Reports
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anaplastic Lymphoma Kinase
  • Antineoplastic Agents / therapeutic use*
  • Aspartate Carbamoyltransferase / genetics*
  • Benzamides / therapeutic use*
  • Carbamoyl-Phosphate Synthase (Glutamine-Hydrolyzing) / genetics*
  • Colorectal Neoplasms / drug therapy*
  • Colorectal Neoplasms / genetics
  • Colorectal Neoplasms / pathology
  • Dihydroorotase / genetics*
  • Female
  • Gene Rearrangement*
  • Humans
  • Indazoles / therapeutic use*
  • Middle Aged
  • Receptor Protein-Tyrosine Kinases / genetics*

Substances

  • Antineoplastic Agents
  • Benzamides
  • CAD trifunctional enzyme
  • Indazoles
  • Aspartate Carbamoyltransferase
  • ALK protein, human
  • Anaplastic Lymphoma Kinase
  • Receptor Protein-Tyrosine Kinases
  • Dihydroorotase
  • Carbamoyl-Phosphate Synthase (Glutamine-Hydrolyzing)
  • entrectinib