Pfizer Oncology, 50 Pequot Ave MS6025-A3266, New London, CT 06320, USA.
Expert Opin Biol Ther. 2010 Apr;10(4):575-85. doi: 10.1517/14712591003689980.
Figitumumab is being developed as a highly potent and specific fully human IgG2 monoclonal antibody against the IGF Type 1 receptor (IGF-IR) for the treatment of cancer.
This manuscript reviews the rationale, preclinical data and early clinical results of the figitumumab development program. Early trials were initiated in 2003 and initial reports appeared in 2006.
Figitumumab has an effective half life of approximately 20 days and has been generally well tolerated in clinical trials. Initial pharmacodynamic studies suggested that IGF-IR overexpression and increased bioactivity of IGFs constitute independent mechanisms of tumor sensitivity to figitumumab. Single-agent activity has been noted in Ewing's sarcoma and a recently completed proof-of-concept study suggested that figitumumab may be active in NSCLC.
The strong biologic rationale for IGF-IR targeting in multiple types of human cancer and the feasibility of combination with full doses of therapies that constitute the standard of care in a variety of oncology indications have justified an expanded clinical program in multiple areas of unmet medical need in oncology.
菲特鲁单抗被开发为一种针对 IGF 型 1 受体 (IGF-IR) 的高活性和特异性的全人 IgG2 单克隆抗体，用于治疗癌症。
本文综述了菲特鲁单抗开发项目的基本原理、临床前数据和早期临床结果。早期试验始于 2003 年，初步报告于 2006 年发表。
菲特鲁单抗的有效半衰期约为 20 天，在临床试验中通常具有良好的耐受性。初步的药效学研究表明，IGF-IR 过表达和 IGF 生物活性的增加构成了肿瘤对菲特鲁单抗敏感性的独立机制。在尤文肉瘤中已经观察到单药活性，最近完成的一项概念验证研究表明，菲特鲁单抗可能对 NSCLC 有效。
在多种人类癌症中针对 IGF-IR 进行靶向治疗的强有力的生物学原理，以及与构成各种肿瘤学适应证标准治疗的全剂量疗法联合应用的可行性，已经证明在肿瘤学中多个未满足医疗需求领域扩大临床项目是合理的。
