Lenvatinib-induced thyroid abnormalities in unresectable hepatocellular carcinoma.

Lenvatinib has anti-tumor activity against advanced hepatocellular carcinoma (HCC). Hypothyroidism is also a frequent complication in patients treated with lenvatinib. However, studies on lenvatinib-induced thyroid toxicity and destructive thyroiditis are limited. Therefore, this study aimed to clarify the frequency and timing of thyroid abnormalities in lenvatinib for unresectable HCC. This retrospective study enrolled 50 patients with advanced HCC treated with lenvatinib. Patients were classified to have euthyroid, subclinical hypothyroidism, overt hypothyroidism, and thyrotoxicosis. The timing of thyroid dysfunction was assessed, and risk factors for incident hypothyroidism or thyrotoxicosis were evaluated using multivariate models. Subclinical hypothyroidism, overt hypothyroidism, and thyrotoxicosis occurred in 7 (14.0%), 26 (52.0%), and 5 (10.0%) patients, respectively. In the 33 patients with hypothyroidism, 27 (84.4%) developed the condition within 2 weeks of starting lenvatinib treatment. Of the 5 patients with thyrotoxicosis, 3 developed the condition within 8 weeks of starting lenvatinib administration. One patient developed thyrotoxicosis in only 1 week of the initiation of treatment. No correlation between the presence of antibodies and the incidence and severity of thyroid dysfunction due to the autoimmune mechanism was observed. The progression-free survival was significantly better in the hypothyroidism group. Lenvatinib treatment for unresectable HCC not only causes hypothyroidism, but also thyrotoxicosis. Moreover, these thyroid conditions develop within the early period of treatment at a higher prevalence. Patients with thyroid dysfunction had better prognosis. Based on these results, in patients administered with lenvatinib, there is need for careful assessment for the possibility of thyroid dysfunction from the onset of treatment.

[1]  Y. Hiasa,et al.  Destructive Thyroiditis Induced by Lenvatinib in Three Patients with Hepatocellular Carcinoma , 2018, Internal medicine.

[2]  J. Llovet,et al.  Molecular therapies and precision medicine for hepatocellular carcinoma , 2018, Nature Reviews Clinical Oncology.

[3]  M. Kudo,et al.  Lenvatinib versus sorafenib in first-line treatment of patients with unresectable hepatocellular carcinoma: a randomised phase 3 non-inferiority trial , 2018, The Lancet.

[4]  M. Kudo,et al.  Phase 2 study of lenvatinib in patients with advanced hepatocellular carcinoma , 2016, Journal of Gastroenterology.

[5]  David C. Smith,et al.  Cabozantinib in chemotherapy-pretreated metastatic castration-resistant prostate cancer: results of a phase II nonrandomized expansion study. , 2014, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[6]  Masao Iwata,et al.  Antitumor Activity of Lenvatinib (E7080): An Angiogenesis Inhibitor That Targets Multiple Receptor Tyrosine Kinases in Preclinical Human Thyroid Cancer Models , 2014, Journal of thyroid research.

[7]  Z. Dezső,et al.  Lenvatinib, an angiogenesis inhibitor targeting VEGFR/FGFR, shows broad antitumor activity in human tumor xenograft models associated with microvessel density and pericyte coverage , 2014, Vascular cell.

[8]  U. Schweizer,et al.  Endocrine side-effects of anti-cancer drugs: thyroid effects of tyrosine kinase inhibitors. , 2014, European journal of endocrinology.

[9]  I. Salti,et al.  Tyrosine Kinase Inhibitors Induced Thyroid Dysfunction: A Review of Its Incidence, Pathophysiology, Clinical Relevance, and Treatment , 2013, BioMed research international.

[10]  J. Reeves,et al.  Pazopanib versus sunitinib in metastatic renal-cell carcinoma. , 2013, The New England journal of medicine.

[11]  Hirotoshi Nakamura,et al.  Inappropriate elevation of serum thyrotropin levels in patients treated with axitinib. , 2013, Thyroid : official journal of the American Thyroid Association.

[12]  N. Gavara,et al.  Thyroid hormone increases fibroblast growth factor receptor expression and disrupts cell mechanics in the developing organ of corti , 2013, BMC Developmental Biology.

[13]  R. Motzer,et al.  Comparative effectiveness of axitinib versus sorafenib in advanced renal cell carcinoma (AXIS): a randomised phase 3 trial , 2011, The Lancet.

[14]  J. Bruix,et al.  Management of hepatocellular carcinoma: An update , 2011, Hepatology.

[15]  T. Visser,et al.  Sorafenib induced thyroiditis in two patients with hepatocellular carcinoma. , 2011, Thyroid : official journal of the American Thyroid Association.

[16]  Riccardo Lencioni,et al.  Modified RECIST (mRECIST) Assessment for Hepatocellular Carcinoma , 2010, Seminars in liver disease.

[17]  Xin Huang,et al.  Overall Survival and Updated Results for Sunitinib Compared With Interferon Alfa in Patients With Metastatic Renal Cell Carcinoma , 2009, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[18]  Y. Funahashi,et al.  Multi-Kinase Inhibitor E7080 Suppresses Lymph Node and Lung Metastases of Human Mammary Breast Tumor MDA-MB-231 via Inhibition of Vascular Endothelial Growth Factor-Receptor (VEGF-R) 2 and VEGF-R3 Kinase , 2008, Clinical Cancer Research.

[19]  Yuji Yamamoto,et al.  E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition , 2008, International journal of cancer.

[20]  J. Samarut,et al.  Thyroid hormones regulate fibroblast growth factor receptor signaling during chondrogenesis. , 2005, Endocrinology.

[21]  Wei Liu,et al.  Fibroblast growth factor receptors as molecular targets in thyroid carcinoma. , 2005, Endocrinology.

[22]  J. Samarut,et al.  Thyroid hormone activates fibroblast growth factor receptor-1 in bone. , 2002, Molecular endocrinology.

[23]  Shuichi Sato,et al.  Clinical characteristics of thyroid abnormalities induced by sunitinib treatment in Japanese patients with renal cell carcinoma. , 2010, Endocrine journal.