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卡博特韦(一种 HIV 整合酶链转移抑制剂)专利申请出版物的文献综述。

A literature review of the patent application publications on cabotegravir - an HIV integrase strand transfer inhibitor.

机构信息

Faculty of Pharmacy, University of Ljubljana, Ljubljana, Slovenia.

Analytics Department, Lek Pharmaceuticals d.d., Sandoz Development Center Slovenia, Ljubljana, Slovenia.

出版信息

Expert Opin Ther Pat. 2020 Mar;30(3):195-208. doi: 10.1080/13543776.2020.1717470. Epub 2020 Jan 27.

Abstract

: Studies presented in the patent applications demonstrate that a new integrase strand transfer inhibitor cabotegravir might be used as long-acting antiretroviral formulation or delivery system that reduces dosing frequency and may therefore increase adherence and thus pre-exposure prophylaxis (PrEP) and treatment efficacy against HIV. As announced in 2019, the developer ViiV Healthcare seeks US and EU approval of long-acting, injectable HIV treatment.: This review covers all the patent applications published until October 2019 with cabotegravir in the examples or claim section of the patent application document. The patent applications cover drug substance synthesis, solid-state forms, therapeutic applications, and efficacy as well as the potential formulations of cabotegravir alone or in combination with other anti-HIV agents.: The results from multiple clinical studies suggest that cabotegravir can be used as PrEP agent and treatment agent against HIV. Multiple studies use cabotegravir in combination with other anti-HIV agents such as rilpivirine. Cabotegravir in combination with rilpivirine is an interesting therapeutic, due to the possibility of formulating long-acting formulation with dosing interval of every 4 weeks or less, thus reducing daily pill burden and improving patient's compliance.

摘要

专利申请中的研究表明,新型整合酶链转移抑制剂卡博特韦(cabotegravir)可作为长效抗逆转录病毒制剂或输送系统,减少给药频率,从而提高患者的服药依从性,进而提高暴露前预防(PrEP)和治疗 HIV 的效果。如 2019 年宣布的那样,研发公司 ViiV Healthcare 正在寻求美国和欧盟批准长效、可注射的 HIV 治疗药物。

本综述涵盖了截至 2019 年 10 月公布的所有专利申请,这些专利申请中在示例或权利要求部分包含卡博特韦。专利申请涵盖药物物质合成、固态形式、治疗应用以及卡博特韦的疗效和潜在制剂,包括单独使用卡博特韦或与其他抗 HIV 药物联合使用的制剂。

多项临床研究结果表明,卡博特韦可用作 HIV 的 PrEP 药物和治疗药物。多项研究将卡博特韦与其他抗 HIV 药物如利匹韦林联合使用。卡博特韦与利匹韦林联合使用是一种很有前途的治疗方法,因为有可能将其制成每 4 周或更短时间给药一次的长效制剂,从而减少每日服药负担,提高患者的依从性。

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