2017年7月18日，FDA批准Puma公司Nerlynx(neratinib)上市，用于早期HER2+乳腺癌患者的扩展辅助治疗（术后使用Herceptin之后的维持治疗），以降低乳腺癌复发风险。Nerlynx是FDA批准的首个扩展辅助疗法。
FDA血液学和肿瘤产品办公室主任Richard Pazdur表示：“HER2+乳腺癌是一种侵袭性癌症，肿瘤会扩散到身体其他部位。这类患者现在在完成初始治疗后，有了远离复发风险的新选择”。
乳腺癌是美国最常见的癌症类型。美国国立癌症研究所估计，2017年将有252710名女性被新确诊为乳腺癌，40610名女性死于乳腺癌。乳腺癌患者中HER2+患者的比例大约为15%。
neratinib是EGFR/HER2抑制剂，其疗效和安全性在一项涉及2840例在前2年接受曲妥珠单抗治疗的早期HRE2+乳腺癌患者的随机研究中得到证实。结果显示，neratinib治疗2年后，未发生任何形式复发或死亡的患者比例为94.2%，安慰剂组为91.9%。
neratinib组最常见的不良反应包括腹泻、恶心、腹痛、疲劳、呕吐、皮疹、肿胀和口疮、食欲减退、肌肉痉挛、消化不良、肝功能损伤（AST或ALT水平升高）、皮肤干燥、体重减轻、泌尿系统感染等。
患者在首次接受neratinib治疗前，应提前56天给予 loperamide 以预防严重腹泻。临床使用上同时需要使用抗腹泻药、营养液和电解质来管理腹泻不良反应
Nerlynx Available for Extended Adjuvant Tx of HER2+ Early Stage Breast Cancer
Puma Biotechnology announced the launch of Nerlynx (neratinib) for the extended adjuvant treatment of adults with early stage HER2-overexpressed/amplified breast cancer following adjuvant trastuzumab-based therapy.
The approval was supported by data from the Phase 3 multicenter, randomized, double-blind, placebo-controlled ExteNET trial (n=2,840) following adjuvant treatment with trastuzumab. Women with early stage HER2+ breast cancer were randomized to either Nerlynx or placebo for 1 year. The data showed invasive disease-free survival (iDFS) was seen in 94.2% of patients treated with Nerlynx vs. 91.9% in patients who received placebo after follow-up of 2 years (hazard ratio [HR] 0.66, 95% CI: 0.49, 0.90; P=0.008).
The most frequently reported adverse effects were diarrhea, nausea, abdominal pain, fatigue, vomiting, rash, stomatitis, decreased appetite, muscle spasms, dyspepsia, AST/ALT increase, nail disorder, dry skin, abdominal distention, epistaxis, weight loss, and urinary tract infection
Nerlynx, a kinase inhibitor, initially received approval from the Food and Drug Administration (FDA) in July 2017. Nerlynx is available as 40mg strength tablets in 126- and 180-count bottles |
