Paper Details

  1. Home
  2. Paper Details

Inhibitors of HIV-1 Attachment: The Discovery and Development of Temsavir and its Prodrug Fostemsavir.

Author: ConlonDavid A, EastgateMartin D, GraselaDennis M, KadowJohn F, KrystalMark R, LangleyDavid R, MeanwellNicholas A, Nowicka-SansBeata, TimminsPeter, WangTao

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Overview

This drug annotation summarizes the discovery of temsavir, an inhibitor of HIV-1 entry, and its development into fostemsavir, an extended release formulation suitable for phase 3 clinical trials. Temsavir exhibited improved antiviral and pharmacokinetic profiles compared to its predecessor, while fostemsavir was designed to address absorption issues. The article outlines the structure-activity and structure-liability studies leading to the discovery of temsavir and the clinical studies conducted with fostemsavir.
Paper Details　
Original Abstract of the Article :
Human immunodeficiency virus-1 (HIV-1) infection currently requires lifelong therapy with drugs that are used in combination to control viremia. The indole-3-glyoxamide 6 was discovered as an inhibitor of HIV-1 infectivity using a phenotypic screen and derivatives of this compound were found to inte...See full text at original site
Dr.Camel IconDr.Camel's Paper Summary Blogラクダ博士について

ラクダ博士は、Health Journal が論文の内容を分かりやすく解説するために作成した架空のキャラクターです。
難解な医学論文を、専門知識のない方にも理解しやすいように、噛み砕いて説明することを目指しています。

* ラクダ博士による解説は、あくまで論文の要点をまとめたものであり、原論文の完全な代替となるものではありません。詳細な内容については、必ず原論文をご参照ください。
* ラクダ博士は架空のキャラクターであり、実際の医学研究者や医療従事者とは一切関係がありません。
* 解説の内容は Health Journal が独自に解釈・作成したものであり、原論文の著者または出版社の見解を反映するものではありません。


引用元：
https://doi.org/10.1021/acs.jmedchem.7b01337

データ提供：米国国立医学図書館（NLM）

Temsavir and Fostemsavir: A New Oasis in the Desert of HIV-1 Infection

HIV-1 infection, a chronic viral disease, can feel like navigating a relentless desert, with ongoing challenges and the need for constant vigilance. This article explores the development of temsavir and its prodrug, fostemsavir, as potential new treatments for HIV-1 infection. The authors delve into the discovery and development of these compounds, highlighting their unique mechanism of action and their potential to disrupt the HIV-1 entry process.

Navigating the Desert of HIV-1 Infection: Exploring New Treatment Options

Temsavir and fostemsavir, through their novel mechanism of action, offer promising new avenues for HIV-1 treatment. By targeting the virus's entry process, these compounds hold the potential to disrupt the infection cycle and provide a new weapon in the fight against HIV-1.

Finding an Oasis of Hope: Strategies for HIV-1 Management

Managing HIV-1 infection requires a multi-faceted approach, including medication, lifestyle modifications, and regular monitoring. It's crucial to consult with a healthcare professional to develop a personalized management plan that addresses your specific needs and maximizes treatment outcomes.

Dr. Camel's Conclusion

The desert of HIV-1 infection can be a daunting and unforgiving landscape. This article highlights the potential of temsavir and fostemsavir to offer a new oasis of hope, providing innovative treatment options that target the virus's entry process. By embracing new treatments and engaging in proactive management, we can work towards improving the lives of individuals living with HIV-1 and creating a brighter future.

Date :
  1. Date Completed 2019-02-25
  2. Date Revised 2019-04-11
Further Info :

Pubmed ID

29271653

DOI: Digital Object Identifier

10.1021/acs.jmedchem.7b01337

Related Literature

Article Analysis
・Effects of fostemsavir
SNS
PICO Info
in preparation
Languages

English

Positive IndicatorAn AI analysis index that serves as a benchmark for how positive the results of the study are. Note that it is a benchmark and requires careful interpretation and consideration of different perspectives.

This site uses cookies. Visit our privacy policy page or click the link in any footer for more information and to change your preferences.