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Pralatrexate - from bench to bedside.

机译:Pralatrexate-从长凳到床头。

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摘要

Pralatrexate (PDX, 10-propargyl 10-deazaaminopterin) is an exciting new chemotherapeutic agent with promising activity in T-cell lymphomas and non-small cell lung cancer. It has been granted approval by the Food and Drug administration (FDA) for use in the treatment of relapsed and refractory peripheral T-cell lymphomas (PTCL). Pralatrexate belongs to a class of antineoplastic agents known as antifolates that also include methotrexate, pemetrexed and ralitrexed. Pralatrexate was rationally designed to have high affinity for the one carbon-reduced folate carrier (RFC-1) which leads to better cellular internalization of the drug and a greater antitumor effect than methotrexate. The following monograph is a story of the development of this drug in a systematic fashion from the bench to the bedside.
机译:Pralatrexate(PDX,10-炔丙基10-脱氮杂min蝶呤)是一种激动人心的新型化疗药物,在T细胞淋巴瘤和非小细胞肺癌中具有广阔的前景。它已获得美国食品药品管理局(FDA)的批准,可用于治疗复发性和难治性外周T细胞淋巴瘤(PTCL)。 Pralatrexate属于一类抗肿瘤药,称为抗叶酸药,还包括甲氨蝶呤,培美曲塞和雷利曲塞。合理设计Pralatrexate,使其对一种碳还原叶酸载体(RFC-1)具有高亲和力,与甲氨蝶呤相比,该载体可更好地实现药物的细胞内在化并具有更大的抗肿瘤作用。以下专着是从长凳到床头有系统地介绍这种药物开发的故事。

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