Abstract
PURPOSE There is no effective therapy for patients with distant metastasis of medullary thyroid carcinoma (MTC). Activating mutations in the RET proto-oncogene cause hereditary MTC, which provides a strong therapeutic rationale for targeting RET kinase activity. This open-label, phase II study assessed the efficacy of vandetanib, a selective oral inhibitor of RET, vascular endothelial growth factor receptor, and epidermal growth factor receptor signaling, in patients with advanced hereditary MTC. METHODS Patients with unresectable locally advanced or metastatic hereditary MTC received initial treatment with once-daily oral vandetanib 300 mg. The dose was adjusted additionally in some patients on the basis of observed toxicity until disease progression or any other withdrawal criterion was met. The primary assessment was objective tumor response (by RECIST [Response Evaluation Criteria in Solid Tumors]). Results Thirty patients received initial treatment with vandetanib 300 mg/d. On the basis of investigator assessments, 20% of patients (ie, six of 30 patients) experienced a confirmed partial response (median duration of response at data cutoff, 10.2 months). An additional 53% of patients (ie, 16 of 30 patients) experienced stable disease at >/= 24 weeks, which yielded a disease control rate of 73% (ie, 22 of 30 patients). In 24 patients, serum calcitonin levels showed a 50% or greater decrease from baseline that was maintained for at least 4 weeks; 16 patients showed a similar reduction in serum carcinoembryonic antigen levels. The most common adverse events were diarrhea (70%), rash (67%), fatigue (63%), and nausea (63%). CONCLUSION In this study, vandetanib demonstrated durable objective partial responses and disease control with a manageable adverse event profile. These results demonstrate that vandetanib may provide an effective therapeutic option in patients with advanced hereditary MTC, a rare disease for which there has been no effective therapy.
MeSH Terms
Administration, Oral
Adult
Aged
Antineoplastic Agents/administration & dosage,adverse effects
Biomarkers, Tumor/blood
Calcitonin/blood
Carcinoembryonic Antigen/blood
Carcinoma, Medullary/drug therapy,genetics,metabolism,mortality,secondary
Disease-Free Survival
Drug Administration Schedule
Female
France
Genetic Predisposition to Disease
Germ-Line Mutation
Humans
Kaplan-Meier Estimate
Male
Middle Aged
Pedigree
Piperidines/administration & dosage,adverse effects
Protein Kinase Inhibitors/administration & dosage,adverse effects
Proto-Oncogene Mas
Proto-Oncogene Proteins c-ret/antagonists & inhibitors,genetics
Quinazolines/administration & dosage,adverse effects
Risk Factors
Thyroid Neoplasms/drug therapy,genetics,metabolism,mortality,pathology
Time Factors
Treatment Outcome
United States
Young Adult
Chemicals
Antineoplastic Agents
Biomarkers, Tumor
Carcinoembryonic Antigen
MAS1 protein, human
Piperidines
Protein Kinase Inhibitors
Proto-Oncogene Mas
Quinazolines
Calcitonin
Proto-Oncogene Proteins c-ret
RET protein, human
N-(4-bromo-2-fluorophenyl)-6-methoxy-7-((1-methylpiperidin-4-yl)methoxy)quinazolin-4-amine
Authors & Affiliations
10 authors, click to expand affiliations / ORCID
Wells Samuel A
Dept of Surgery, Washington University School of Medicine, Box 8109, 660 S Euclid Ave, St Louis, MO 63110, USA. wellss@wudosis.wustl.edu
Gosnell Jessica E
Gagel Robert F
Moley Jeffrey
Pfister David
Sosa Julie A
Skinner Michael
Krebs Annetta
Vasselli James
Schlumberger Martin
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