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

Paper Details 
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
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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 :
  1. Date Completed 2019-05-22
  2. Date Revised 2023-09-28
Further Info :

Pubmed ID

30143424

DOI: Digital Object Identifier

PMC6185871

Related Literature

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.

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