Phase 2 trial of afatinib, an ErbB family blocker, in solid tumors genetically screened for target activation

Cancer. 2013 Aug 15;119(16):3043-51. doi: 10.1002/cncr.28120. Epub 2013 Jun 14.

Abstract

Background: The efficacy of afatinib, an irreversible ErbB Family Blocker, was evaluated in patients who had 1 of 4 categories of solid tumors with epidermal growth factor receptor/human epidermal growth factor receptor 2 (EGFR/HER2) gene amplification or EGFR-activating mutations.

Methods: Patients with previously treated but ErbB inhibitor-naive esophagogastric, biliary tract, urothelial tract, or gynecologic cancers (lung cancers were excluded) harboring EGFR/HER2 gene amplification or high polysomy were identified by fluorescence in situ hybridization (FISH). Tumors were also screened for EGFR mutations. The primary endpoint was the objective response rate; secondary endpoints included the clinical benefit rate, pharmacokinetics, and safety.

Results: Of 385 prescreened patients, 38 had FISH-positive tumors (10 with EGFR amplification and 29 with HER2 amplification or high polysomy [1 tumor had EGFR/HER2 high polysomy]; none had EGFR-activating mutations), and 20 patients received treatment with afatinib 50 mg daily. The objective response rate was 5% (1 of 20 patients), and the best objective response included 1 complete response. Eight patients experienced stable disease. The most frequently reported adverse events were diarrhea, rash, and decreased appetite. The trial closed early because of slow recruitment.

Conclusions: Single-agent afatinib activity was limited, yet encouraging, in selected tumors that were screened prospectively for target activation. The implementation of a biomarker-driven approach using a low-frequency biomarker for patient selection across multiple tumor types can be challenging.

Keywords: EGFR; EGFR-activating mutations; ErbB Family Blocker; HER2; afatinib; epidermal growth factor receptor; gene amplification; human epidermal growth factor receptor 2; solid tumors.

Publication types

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

MeSH terms

  • Adult
  • Afatinib
  • Aged
  • Aged, 80 and over
  • ErbB Receptors / antagonists & inhibitors*
  • ErbB Receptors / genetics
  • ErbB Receptors / metabolism
  • Female
  • Gene Amplification
  • Humans
  • In Situ Hybridization, Fluorescence
  • Male
  • Middle Aged
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Neoplasms / genetics
  • Prospective Studies
  • Quinazolines / pharmacokinetics
  • Quinazolines / therapeutic use*
  • Receptor, ErbB-2 / genetics
  • Receptor, ErbB-2 / metabolism
  • Treatment Outcome

Substances

  • Quinazolines
  • Afatinib
  • ErbB Receptors
  • Receptor, ErbB-2