Rizza S A, Bhatia R, Zeuli J, Temesgen Z
Division of Infectious Diseases, Mayo Clinic, Rochester, Minnesota, USA.
Department of Preventative Medicine, Northwestern University Feinberg School of Medicine, Chicago, Illinois, USA.
Drugs Today (Barc). 2019 Jan;55(1):25-34. doi: 10.1358/dot.2019.55.1.2895651.
Ibalizumab, a humanized monoclonal antibody to CD4, was recently approved by the United States Food and Drug Administration (FDA) for the treatment of HIV-1 infection in heavily treatment-experienced adults with multidrug-resistant HIV-1 infection failing their current antiretroviral regimen. Ibalizumab is the first in a new class of antiretroviral drugs designated as post-attachment inhibitors. It exerts its antiviral effect by noncompetitive binding of CD4, thereby blocking conformational changes in the CD4-gp120 complex that are essential for viral entry. Clinical studies have demonstrated ibalizumab's significant antiviral activity in patients with advanced HIV disease and extensive treatment experience, who had limited treatment options. Ibalizumab is administered intravenously at a dose of 800 mg every 2 weeks following a single intravenous loading dose of 2000 mg. The most common adverse reactions reported with the use of ibalizumab are diarrhea, dizziness, nausea and rash.
依巴珠单抗是一种针对CD4的人源化单克隆抗体，最近被美国食品药品监督管理局（FDA）批准用于治疗多重耐药HIV-1感染且当前抗逆转录病毒治疗方案失败的、有大量治疗经历的成年HIV-1感染者。依巴珠单抗是新一类被指定为附着后抑制剂的抗逆转录病毒药物中的首个药物。它通过与CD4非竞争性结合发挥抗病毒作用，从而阻断CD4-gp120复合物中对于病毒进入至关重要的构象变化。临床研究已证明依巴珠单抗在晚期HIV疾病患者及有广泛治疗经历、治疗选择有限的患者中具有显著的抗病毒活性。依巴珠单抗在单次静脉注射2000mg负荷剂量后，每2周静脉注射800mg。使用依巴珠单抗报告的最常见不良反应为腹泻、头晕、恶心和皮疹。
