Efficacy and toxicity of vemurafenib and cobimetinib in relation to plasma concentrations, after administration via feeding tube in patients with BRAF-mutated thyroid cancer: a case series and review of literature

Cancer Chemother Pharmacol. 2022 Jul;90(1):97-104. doi: 10.1007/s00280-022-04437-z. Epub 2022 May 22.

Abstract

Introduction: The combination of vemurafenib, a proto-oncogene B-Raf inhibitor (BRAFi) and cobimetinib, an inhibitor of mitogen-activated protein kinase kinase (MEKi) has shown to improve survival in patients with BRAF V600-mutated melanoma. BRAF mutations are also frequently detected driver mutations in other tumor types, including thyroid carcinoma. Since thyroid carcinoma is not a labeled indication for BRAF/MEKi, a cohort for patients with BRAF V600-mutated thyroid carcinoma was opened within the Drug Rediscovery Protocol (DRUP), a national ongoing pan-cancer multi-drug trial, in which patients receive off-label treatment with approved drugs based on their molecular tumor profile.

Results: Here, we present two patients with BRAF-mutated thyroid carcinoma, who were successfully treated with vemurafenib/cobimetinib administered via a feeding tube. Plasma concentrations of vemurafenib and cobimetinib were determined. A partial response was observed in both patients, but they experienced significant toxicity.

Conclusion: Our cases show that vemurafenib/cobimetinib treatment is effective in BRAF V600-mutated thyroid carcinoma, also when administered via a feeding tube. Although serious side effects occurred in both patients, we hypothesize that this was not attributable to the administration route. Therefore, administration of vemurafenib/cobimetinib by feeding tube is feasible and effective.

Trial registration: Clinical trial identification: NCT02925234.

Keywords: Case series; Cobimetinib; Feeding tube; Plasma concentrations; Thyroid carcinoma; Vemurafenib.

Publication types

  • Case Reports
  • Review

MeSH terms

  • Antineoplastic Agents* / adverse effects
  • Antineoplastic Agents* / pharmacokinetics
  • Azetidines* / adverse effects
  • Azetidines* / pharmacokinetics
  • Humans
  • Piperidines* / adverse effects
  • Piperidines* / pharmacokinetics
  • Proto-Oncogene Proteins B-raf / genetics
  • Skin Neoplasms* / drug therapy
  • Skin Neoplasms* / genetics
  • Thyroid Neoplasms* / drug therapy
  • Thyroid Neoplasms* / genetics
  • Vemurafenib* / adverse effects
  • Vemurafenib* / pharmacokinetics

Substances

  • Antineoplastic Agents
  • Azetidines
  • Piperidines
  • Vemurafenib
  • BRAF protein, human
  • Proto-Oncogene Proteins B-raf
  • cobimetinib

Associated data

  • ClinicalTrials.gov/NCT02925234