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Discovery of super soft-drug modulators of sphingosine-1-phosphate receptor 1.
Author: BellMark, EpemoluOla, FoleyDavid, KatzElad, McLeanW H Irwin, NaylorClaire, ReadKevin D, RileyJennifer, RobinsonColin, ScullionPaul, ShishikuraYoko, WoodlandAndrew, WyattPaul
Original Abstract of the Article :
The oral S1PR1 agonist ponesimod demonstrated substantial efficacy in a phase II clinical trial of psoriasis. Unfortunately, systemic side effects were observed, which included lymphopenia and transient bradycardia. We sought to develop a topical soft-drug S1PR1 agonist with an improved therapeutic ...See full text at original site
Dr.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。
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引用元:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6185871/
データ提供:米国国立医学図書館(NLM)
Super Soft-Drug Modulators of Sphingosine-1-Phosphate Receptor 1: A New Frontier in Psoriasis Treatment
The search for [effective treatments] for [psoriasis] continues, with a focus on [minimizing side effects] while maximizing [therapeutic benefits]. This research explores the development of [topical soft-drug S1PR1 agonists], seeking to improve upon the [efficacy and safety profile] of [oral S1PR1 agonists], such as [ponesimod]. The study focuses on [modifying ponesimod] to create [metabolically unstable esters] that are targeted for [rapid breakdown in plasma], thereby reducing [systemic exposure] and [potential side effects].
Soft-Drug Approach: Balancing Efficacy and Safety
This research highlights the [innovative approach] of [soft-drug design] in [drug development]. By targeting [esterases present in human plasma], the researchers aim to [reduce systemic exposure] and [minimize side effects], while maintaining [therapeutic efficacy] for [psoriasis treatment]. This strategy holds promise for [improving the therapeutic index] of [S1PR1 agonists] and potentially [expanding their therapeutic applications].
Topical Therapy: A Potential Breakthrough in Psoriasis Treatment
The study's focus on [topical delivery] of [S1PR1 agonists] is significant. This approach offers the potential for [localized treatment], which may [reduce systemic exposure] and [minimize the risk of side effects] associated with [oral administration]. If successful, this research could pave the way for [more effective and safer treatments] for [psoriasis] and potentially [other inflammatory skin conditions].
Dr. Camel's Conclusion
This research is like a [desert camel] seeking [a cooler path] through the [scorching heat of psoriasis]. The development of [topical soft-drug S1PR1 agonists] offers a [more targeted and effective] approach to [psoriasis treatment], potentially [reducing the risk of side effects] while maximizing [therapeutic benefits]. This research showcases the [innovative spirit] of [drug development] and the ongoing quest to [improve patient outcomes] in the face of [complex health challenges].
Date :
- Date Completed 2019-05-22
- Date Revised 2023-09-28
Further Info :
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