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Marine-Sourced Anti-Cancer and Cancer Pain Control Agents in Clinical and Late Preclinical Development †

机译:在临床和后期临床前开发中使用海洋来源的抗癌和癌痛控制剂†

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摘要

The marine habitat has produced a significant number of very potent marine-derived agents that have the potential to inhibit the growth of human tumor cells in vitro and, in a number of cases, in both in vivo murine models and in humans. Although many agents have entered clinical trials in cancer, to date, only Cytarabine, Yondelis® (ET743), Eribulin (a synthetic derivative based on the structure of halichondrin B), and the dolastatin 10 derivative, monomethylauristatin E (MMAE or vedotin) as a warhead, have been approved for use in humans (Adcetris®). In this review, we show the compounds derived from marine sources that are currently in clinical trials against cancer. We have included brief discussions of the approved agents, where they are in trials to extend their initial approved activity (a common practice once an agent is approved), and have also included an extensive discussion of the use of auristatin derivatives as warheads, plus an area that has rarely been covered, the use of marine-derived agents to ameliorate the pain from cancers in humans, and to act as an adjuvant in immunological therapies.
机译:海洋栖息地已经产生了许多非常有效的海洋来源的物质,它们具有在体外以及在许多情况下在体内鼠模型和人类中抑制人肿瘤细胞生长的潜力。尽管许多药物已进入癌症的临床试验,但迄今为止,只有阿糖胞苷,Yondelis ®(ET743),依立布林(基于halichondrin B结构的合成衍生物)和dolastatin 10衍生物Monomethylauristatin E(MMAE或vedotin)作为战斗部已被批准用于人类(Adcetris ®)。在这篇综述中,我们显示了目前正处于抗癌临床试验中的海洋来源化合物。我们对获准药物进行了简短的讨论,他们正在试验中以扩大其最初的获批准的活动(一旦药物被批准,这是一种惯例),还广泛讨论了使用auristatin衍生物作为战斗部,以及很少涉及的领域是使用海洋来源的药物来减轻人类癌症引起的疼痛,并在免疫疗法中起辅助作用。

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