Veklury® (remdesivir) formulations inhibit initial membrane-coupled events of SARS-CoV-2 infection due to their sulfobutylether-β-cyclodextrin content

carbohydrates, drug delivery,

It has always been a bit of a mystery that given the antiviral effect of certain cyclodextrin, we can attribute all the antiviral effect of Veklury to remdesivir, which takes 3% of the formulation or maybe SBECD (97% of the formulation) also has some role. Researchers from University of Debrecen explore those questions.
Veklury® and different cholesterol-depleting cyclodextrins (CDs) reduced the binding of the spike receptor binding domain to ACE2 and spike trimer internalization for Wuhan-Hu-1, Delta, and Omicron variants. Correlations of these effects with cholesterol-dependent changes in membrane structure and decreased, lipid raft-dependent ACE2-TMPRSS2 interaction establish that SBECD is not simply a vehicle but also an effector in Veklury® due to its cholesterol-depleting potential.
Gyorgy Panyi, Florina Zakany et al.

See the full article here.

Synthesis of an amphiphilic vancomycin aglycone derivative inspired by polymyxins: overcoming glycopeptide resistance in Gram-positive and Gram-negative bacteria in synergy with teicoplanin in vitro

carbohydrates, ,

A fascinating journey in the world of novel glycopeptide antibiotics with stops such as overcoming resistance in Gram-positive and Gram-negative bacteria and combined antiviral and antibiotic effects guided by  Anikó Borbás and her group at University of Debrecen supported by several international KOLs in the field (Ilona Bakai-Bereczki, Ferenc Fenyvesi, Pal Herczegh, Eszter Ostorhazi, Henrietta Papp, Batta Gyula, Ana Mitrović, Janko Kos, István Hajdu, Dávid Bajusz, György Keseru, et al)

See the corresponding articles on nature.com:

Synthesis of an amphiphilic vancomycin aglycone derivative inspired by polymyxins: overcoming glycopeptide resistance in Gram-positive and Gram-negative bacteria in synergy with teicoplanin in vitro

Semisynthetic teicoplanin derivatives with dual antimicrobial activity against SARS-CoV-2 and multiresistant bacteria


Synthetic biomarkers for differential serological diagnosis of Cutaneous Leishmaniasis (CL) caused by various Leishmania species

carbohydrates, ,

Great patent on neoglycoconjugates and/or glycosides containing glycan selected from Galpα1,3Galfβ, Galpα1,6Galpα1,3Galfβ, or Galpα1,3Galfβ1,3Manpα and their use as diagnostic or prognostic biomarkers, vaccines, treating or detecting parasitic diseases, such as cutaneous leishmaniasis are disclosed.
The University of Texas at El Paso – Igor Almeida, Rosa Amelia Maldonado, Alvaro Acosta-Serrano, Susana Portillo et al.

See the full patent on Espacenet

Targeting bacterial virulence as a novel treatment against AMR infections

drug development, ,

Have you known that Arivin Therapeutics uses cyclodextrin for targeting bacterial virulence as a novel treatment against AMR infections? Among their MoA claims, the following are listed:
– Targeting virulence factors is effective, also against extensively resistant isolates
– Targeting virulence avoids rapid resistance
– Direct reduction in inflammatory responses
– Potentiates the function of antibiotics
Also, there is a spectacular video about how CDs develop their effect as antibacterials.

https://arivintx.com/our-science

Cyclodextrins: Only Pharmaceutical Excipients or Full-Fledged Drug Candidates?

Today's cyclodextrin, , , , ,

What is the future of cyclodextrin: excipient or API?
A very timely review from University of Debrecen (Gyorgy Panyi, Florina Zakany, et al.) discussing #molecular targets, mechanism of action, and ongoing research in several diseases. Which do you think holds the future?

See the full article here