首页> 外文期刊>Recent patents on anti-infective drug discovery >Parenteral patent drug S/GSK1265744 has the potential to be an effective agent in pre-exposure prophylaxis against HIV infection
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Parenteral patent drug S/GSK1265744 has the potential to be an effective agent in pre-exposure prophylaxis against HIV infection

机译:肠胃外专利药S / GSK1265744有可能成为预防HIV感染的暴露前预防的有效药物

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The continuing HIV epidemic has driven advancements in antiretroviral therapy. New therapeutic targets have been identified over the past years, one of which has been the Integrase enzyme. This is responsible for integrating HIV pro-DNA into the host cell genome and has proved a successful drug target. Efforts have also been made to improve the pharmacokinetic parameters of current drug therapy and utilise these techniques in maximising drug therapeutic effect whilst minimising adverse events. An exciting example of new technologies is that of nanotechnology where drugs can be specifically targeted to certain tissues and drug delivery can be improved by utilising biological molecules and structures. Pre-exposure prophylaxis is also an area of much interest currently both on an individual and population level. Compliance is however a major issue with daily medication to prevent HIV acquisition as has been demonstrated with contraceptive agents. However if long acting compounds can be developed, compliance can be improved. The patent drug currently being developed through nanotechnology as an analogue of Dolutegravir, GSK1265744 LAP (Long Acting Parenteral) has shown promise as a Long Acting Integrase Inhibitor with potential action both as a therapeutic agent but also in pre-exposure prophylaxis. The favourable pharmacokinetic profile and therapeutic efficacy in comparison to other compounds of the same class demonstrate it to be a promising advance. However given current limitations in study material, further randomised studies with long term follow up are required to fully evaluate the value of the patent drug GSK1265744 LAP in action in both seropositive and seronegative individuals.
机译:持续的艾滋病毒流行推动了抗逆转录病毒疗法的发展。在过去的几年中,已经确定了新的治疗靶标,其中之一就是整合酶。这负责将HIV原DNA整合到宿主细胞基因组中,并已证明是成功的药物靶标。还已经做出努力来改善当前药物治疗的药代动力学参数,并利用这些技术来最大化药物治疗效果同时最小化不良事件。新技术的一个令人振奋的例子是纳米技术,其中药物可以专门针对某些组织,并且可以通过利用生物分子和结构来改善药物的递送。暴露前预防也是目前个人和人群都非常关注的领域。然而,如避孕药所证明的那样,依从性是日常药物预防HIV感染的主要问题。但是,如果可以开发出长效化合物,则顺应性可以得到改善。目前正在通过纳米技术作为Dolutegravir的类似物开发的专利药物GSK1265744 LAP(长效肠胃外药物)显示出有望作为长效整合酶抑制剂的潜在作用,既可作为治疗剂,也可用于预防接触前。与相同类别的其他化合物相比,其良好的药代动力学特征和治疗功效证明这是有希望的进展。但是,鉴于研究材料的当前局限性,需要进一步的长期随访随机研究以全面评估专利药物GSK1265744 LAP在血清反应阳性和血清阴性个体中的作用价值。

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