Sapna Fnu, Athwal Pal Satyajit Singh, Kumar Mukesh, Randhawa Sandeep, Kahlon Sukhmanii
Internal Medicine, Lal Medical Center, Kashmore, PAK.
Internal Medicine, Saraswathi Institute of Medical Sciences, Hapur, IND.
Cureus. 2020 Aug 2;12(8):e9522. doi: 10.7759/cureus.9522.
Breast cancer is a frequently occurring malignancy in women. Immunologically, breast cancers can be classified into four subtypes depending on the types of receptors present and their expression profiles. These are estrogen positive, progesterone positive, human epidermal growth factor receptor type 2 (HER2) positive, and triple-negative as identified by immunohistochemistry. This classification is the basis of response to treatment, prognosis, and survival. With the identification of HER2 receptor overexpression, targeted therapies with anti-HER2 agents have been developed. The first-line therapy approved for HER2 positive tumors is trastuzumab and pertuzumab linked to taxane and further treatment with an antibody-drug conjugate to achieve satisfactory outcomes. Tyrosine kinase overexpression can be treated with lapatinib, which has also been approved for improving survival and is used in combination with capecitabine. Acquired resistance in HER2 positive tumors is shown in many cases due to genetic or epigenetic modifications. Therefore, it is very important to plan therapeutic strategies and design effective treatment approaches. For a long time, only two agents, trastuzumab and lapatinib, have been approved by the Food and Drug Administration (FDA) for the treatment of HER2 positive breast cancers. There has been no appropriate treatment for trastuzumab resistance and its failure to reduce tumor growth. Lapatinib was approved by the FDA in 2007 for HER2 positive breast cancer. Three existing therapy options after trastuzumab resistance was proposed by clinicians: continuation of trastuzumab, starting therapy with lapatinib, and the synergistic use of trastuzumab and lapatinib. There have been several effective therapies proposed for HER2 positive breast cancers in correlation with clinical trials. Discovering the mechanisms of trastuzumab resistance would increase its response to therapy and better clinical outcome. Clinicians are being continuously challenged by the resistance mechanisms and bioavailability of the drugs in the treatment of metastatic breast cancers. The addition of new drugs to the chemotherapeutic regimen increases the complexity, burden of side effects, and chances of relapse. Novel anti-HER2 agents have been directed towards therapy making a major paradigm shift.
乳腺癌是女性中常见的恶性肿瘤。从免疫学角度来看,乳腺癌可根据存在的受体类型及其表达谱分为四种亚型。通过免疫组织化学鉴定,这些亚型分别为雌激素阳性、孕激素阳性、人表皮生长因子受体2(HER2)阳性和三阴性。这种分类是治疗反应、预后和生存情况的基础。随着HER2受体过表达的发现,已开发出针对HER2的靶向治疗药物。批准用于HER2阳性肿瘤的一线治疗药物是与紫杉烷联用的曲妥珠单抗和帕妥珠单抗,以及进一步使用抗体-药物偶联物进行治疗以取得满意疗效。酪氨酸激酶过表达可用拉帕替尼治疗,拉帕替尼也已被批准用于提高生存率,并与卡培他滨联合使用。在许多情况下,HER2阳性肿瘤会因基因或表观遗传修饰而出现获得性耐药。因此,规划治疗策略和设计有效的治疗方法非常重要。长期以来,美国食品药品监督管理局(FDA)仅批准了两种药物——曲妥珠单抗和拉帕替尼用于治疗HER2阳性乳腺癌。对于曲妥珠单抗耐药及其无法抑制肿瘤生长的情况,一直没有合适的治疗方法。拉帕替尼于2007年被FDA批准用于治疗HER2阳性乳腺癌。临床医生提出了曲妥珠单抗耐药后的三种现有治疗方案:继续使用曲妥珠单抗、开始使用拉帕替尼治疗以及联合使用曲妥珠单抗和拉帕替尼。与临床试验相关的针对HER2阳性乳腺癌的几种有效治疗方法已被提出。发现曲妥珠单抗耐药的机制将提高其治疗反应并改善临床结局。在转移性乳腺癌的治疗中,临床医生不断受到耐药机制和药物生物利用度的挑战。在化疗方案中添加新药会增加复杂性、副作用负担和复发几率。新型抗HER2药物已朝着治疗方向实现了重大范式转变。