Crocetin and related oxygen diffusion‐enhancing compounds: Review of chemical synthesis, pharmacology, clinical development, and novel therapeutic applications
The current pandemic forced us to introspect and revisit our armamentarium of medicinal agents which could be life‐saving in emergency situations. Oxygen diffusion‐enhancing compounds represent one such class of potential therapeutic agents, particularly in ischemic conditions. As rewarding as the n...
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| Published in | Drug development research Vol. 82; no. 7; pp. 883 - 895 |
|---|---|
| Main Authors | , , , |
| Format | Journal Article |
| Language | English |
| Published |
Hoboken, USA
John Wiley & Sons, Inc
01.11.2021
Wiley Subscription Services, Inc |
| Subjects | |
| Online Access | Get full text |
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| Abstract | The current pandemic forced us to introspect and revisit our armamentarium of medicinal agents which could be life‐saving in emergency situations. Oxygen diffusion‐enhancing compounds represent one such class of potential therapeutic agents, particularly in ischemic conditions. As rewarding as the name suggests, these agents, represented by the most advanced and first‐in‐class molecule, trans‐sodium crocetinate (TSC), are the subject of intense clinical investigation, including Phase 1b/2b clinical trials for COVID‐19. Being a successor of a natural product, crocetin, TSC is being investigated for various cancers as a radiosensitizer owing to its oxygen diffusion enhancement capability. The unique properties of TSC make it a promising therapeutic agent for various ailments such as hemorrhagic shock, stroke, heart attack, among others. The present review outlines various (bio)synthetic strategies, pharmacological aspects, clinical overview and potential therapeutic benefits of crocetin and related compounds including TSC. The recent literature focusing on the delivery aspects of these compounds is covered as well to paint the complete picture to the curious reader. Given the potential TSC holds as a first‐in‐class agent, small‐ and/or macromolecular therapeutics based on the core concept of improved oxygen diffusion from blood to the surrounding tissues where it is needed the most, will be developed in future and satisfy the unmet medical need for many diseases and disorders. |
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| AbstractList | The current pandemic forced us to introspect and revisit our armamentarium of medicinal agents which could be life‐saving in emergency situations. Oxygen diffusion‐enhancing compounds represent one such class of potential therapeutic agents, particularly in ischemic conditions. As rewarding as the name suggests, these agents, represented by the most advanced and first‐in‐class molecule, trans‐sodium crocetinate (TSC), are the subject of intense clinical investigation, including Phase 1b/2b clinical trials for COVID‐19. Being a successor of a natural product, crocetin, TSC is being investigated for various cancers as a radiosensitizer owing to its oxygen diffusion enhancement capability. The unique properties of TSC make it a promising therapeutic agent for various ailments such as hemorrhagic shock, stroke, heart attack, among others. The present review outlines various (bio)synthetic strategies, pharmacological aspects, clinical overview and potential therapeutic benefits of crocetin and related compounds including TSC. The recent literature focusing on the delivery aspects of these compounds is covered as well to paint the complete picture to the curious reader. Given the potential TSC holds as a first‐in‐class agent, small‐ and/or macromolecular therapeutics based on the core concept of improved oxygen diffusion from blood to the surrounding tissues where it is needed the most, will be developed in future and satisfy the unmet medical need for many diseases and disorders. The current pandemic forced us to introspect and revisit our armamentarium of medicinal agents which could be life-saving in emergency situations. Oxygen diffusion-enhancing compounds represent one such class of potential therapeutic agents, particularly in ischemic conditions. As rewarding as the name suggests, these agents, represented by the most advanced and first-in-class molecule, trans-sodium crocetinate (TSC), are the subject of intense clinical investigation, including Phase 1b/2b clinical trials for COVID-19. Being a successor of a natural product, crocetin, TSC is being investigated for various cancers as a radiosensitizer owing to its oxygen diffusion enhancement capability. The unique properties of TSC make it a promising therapeutic agent for various ailments such as hemorrhagic shock, stroke, heart attack, among others. The present review outlines various (bio)synthetic strategies, pharmacological aspects, clinical overview and potential therapeutic benefits of crocetin and related compounds including TSC. The recent literature focusing on the delivery aspects of these compounds is covered as well to paint the complete picture to the curious reader. Given the potential TSC holds as a first-in-class agent, small- and/or macromolecular therapeutics based on the core concept of improved oxygen diffusion from blood to the surrounding tissues where it is needed the most, will be developed in future and satisfy the unmet medical need for many diseases and disorders.The current pandemic forced us to introspect and revisit our armamentarium of medicinal agents which could be life-saving in emergency situations. Oxygen diffusion-enhancing compounds represent one such class of potential therapeutic agents, particularly in ischemic conditions. As rewarding as the name suggests, these agents, represented by the most advanced and first-in-class molecule, trans-sodium crocetinate (TSC), are the subject of intense clinical investigation, including Phase 1b/2b clinical trials for COVID-19. Being a successor of a natural product, crocetin, TSC is being investigated for various cancers as a radiosensitizer owing to its oxygen diffusion enhancement capability. The unique properties of TSC make it a promising therapeutic agent for various ailments such as hemorrhagic shock, stroke, heart attack, among others. The present review outlines various (bio)synthetic strategies, pharmacological aspects, clinical overview and potential therapeutic benefits of crocetin and related compounds including TSC. The recent literature focusing on the delivery aspects of these compounds is covered as well to paint the complete picture to the curious reader. Given the potential TSC holds as a first-in-class agent, small- and/or macromolecular therapeutics based on the core concept of improved oxygen diffusion from blood to the surrounding tissues where it is needed the most, will be developed in future and satisfy the unmet medical need for many diseases and disorders. |
| Author | Joshi, Shreerang V. Jain, Ashvi S. Shah, Hriday M. Kharkar, Prashant S. |
| AuthorAffiliation | 1 Department of Pharmaceutical Sciences and Technology Institute of Chemical Technology Mumbai India |
| AuthorAffiliation_xml | – name: 1 Department of Pharmaceutical Sciences and Technology Institute of Chemical Technology Mumbai India |
| Author_xml | – sequence: 1 givenname: Hriday M. surname: Shah fullname: Shah, Hriday M. organization: Institute of Chemical Technology – sequence: 2 givenname: Ashvi S. surname: Jain fullname: Jain, Ashvi S. organization: Institute of Chemical Technology – sequence: 3 givenname: Shreerang V. surname: Joshi fullname: Joshi, Shreerang V. organization: Institute of Chemical Technology – sequence: 4 givenname: Prashant S. orcidid: 0000-0003-1955-7223 surname: Kharkar fullname: Kharkar, Prashant S. email: ps.kharkar@ictmumbai.edu.in organization: Institute of Chemical Technology |
| BackLink | https://www.ncbi.nlm.nih.gov/pubmed/33817811$$D View this record in MEDLINE/PubMed |
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| Keywords | glioblastoma multiforme crocin trans-sodium crocetinate TSC oxygen diffusion-enhancing compounds Crocetin |
| Language | English |
| License | 2021 Wiley Periodicals, LLC. This article is being made freely available through PubMed Central as part of the COVID-19 public health emergency response. It can be used for unrestricted research re-use and analysis in any form or by any means with acknowledgement of the original source, for the duration of the public health emergency. |
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| Snippet | The current pandemic forced us to introspect and revisit our armamentarium of medicinal agents which could be life‐saving in emergency situations. Oxygen... The current pandemic forced us to introspect and revisit our armamentarium of medicinal agents which could be life-saving in emergency situations. Oxygen... |
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| SubjectTerms | Chemical compounds Chemical synthesis Clinical trials COVID-19 Crocetin crocin Diffusion Emergency medical services glioblastoma multiforme Hemorrhage Ischemia Macromolecules Myocardial infarction Natural products Oxygen oxygen diffusion‐enhancing compounds Pandemics Pharmacology Review Reviews Therapeutic applications trans‐sodium crocetinate TSC |
| Title | Crocetin and related oxygen diffusion‐enhancing compounds: Review of chemical synthesis, pharmacology, clinical development, and novel therapeutic applications |
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