使用合成的氯毒素（TM-601）针对神经胶质瘤和其他恶性肿瘤进行靶向抗肿瘤治疗。,Expert Opinion on Drug Delivery

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使用合成的氯毒素（TM-601）针对神经胶质瘤和其他恶性肿瘤进行靶向抗肿瘤治疗。
Expert Opinion on Drug Delivery ( IF 5.0 ) Pub Date : 2007-03-06 , DOI: 10.1517/17425247.4.2.175
Adam N Mamelak ₁ , Douglas B Jacoby

Affiliation

癌症的靶向疗法是一个快速发展的领域，但是已证明难以鉴定肿瘤特异性配体。氯毒素（CTX）是从以色列黄色巨蝎Leiurus Quinquestriatus毒液中分离出来的一种小的36个氨基酸的神经毒素。有趣的是，已发现该肽优先结合多种人类恶性肿瘤，但几乎不结合或不结合正常人类组织。该肽的合成形式（TM-601）已被生产出来，并与碘131（131I-TM-601）共价连接，作为将放射线靶向肿瘤细胞的一种手段。对于复发性神经胶质瘤（一种恶性脑肿瘤）的患者，已经完成了临床前研究和I期临床试验。这些研究表明，腔内给药131I-TM-601显得安全，毒性最小，并以高亲和力和长时间结合恶性神经胶质瘤。该药物使用更高剂量的放射性和重复局部给药的II期试验正在进行中。此外，I期试验已经开始招募，该试验评估了系统递送的131I-TM-601是否可用于对转移性实体瘤和原发性神经胶质瘤进行成像。由于其体积小，选择性的肿瘤结合特性，最小的毒性和相对易操作性，CTX代表了许多癌症的潜在重要靶向剂。一项I期试验已经开始招募，该试验评估了系统递送的131I-TM-601是否可用于对转移性实体瘤和原发性神经胶质瘤进行成像。由于其体积小，选择性的肿瘤结合特性，最小的毒性和相对易操作性，CTX代表了许多癌症的潜在重要靶向剂。一项I期试验已经开始招募，该试验评估了系统递送的131I-TM-601是否可用于对转移性实体瘤和原发性神经胶质瘤进行成像。由于其体积小，选择性的肿瘤结合特性，最小的毒性和相对易操作性，CTX代表了许多癌症的潜在重要靶向剂。

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Targeted delivery of antitumoral therapy to glioma and other malignancies with synthetic chlorotoxin (TM-601).

Targeted therapies for cancer is a rapidly advancing field, but the identification of tumor-specific ligands has proven difficult. Chlorotoxin (CTX) is a small, 36 amino acid neurotoxin isolated from the venom of the Giant Yellow Israeli scorpion Leiurus Quinquestriatus. Interestingly, the peptide has been found to preferentially bind to a variety of human malignancies, but shows little or no binding to normal human tissues. A synthetic version of this peptide (TM-601) has been manufactured and covalently linked to iodine 131 (131I-TM-601) as a means of targeting radiation to tumor cells. Preclinical studies and Phase I clinical trials have been completed in patients with recurrent glioma, a type of malignant brain tumor. These studies demonstrated that intracavitary dosing of 131I-TM-601 appears safe, minimally toxic, and binds malignant glioma with high affinity and for long durations. A Phase II trial of this agent using higher doses of radioactivity and repeated local administrations is underway. In addition, enrolment has begun in a Phase I trial evaluating whether systemically delivered 131I-TM-601 can be used to image metastatic solid tumors and primary gliomas. Due to its small size, selective tumor binding properties, minimal toxicity and relative ease of manipulation, CTX represents a potentially important targeting agent for many cancers.

更新日期：2019-11-01

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