Comparison of the Efficacy and Safety of Adamgammadex with Sugammadex for Reversal of Rocuronium-Induced Neuromuscular Block: Results of a Phase II Clinical Trial

The success of Sugammadex inspired several further cyclodextrin research, including the development of other antidotes and discovering “follow-up” compounds for the same indication. The most advanced candidate in this field is Adamgammadex (developed by Adamerck) with its efficacy recently compared to SGM in a Phase II trial lead by Sichuan University. Although it was used in 2-3 times higher concentrations, the previously reported adverse effects were not observed in this study, including anaphylaxis, haemorrhage, recurarization, abnormal basic vital signs, or lengthened QRS intervals and QT intervals. Adamgammadex was found to be effective for reversing rocuronium-induced neuromuscular block as sugammadex.

See the full article here

Degree and distribution of substitution of hydroxypropyl-β-cyclodextrin in enantioselective liquid-liquid extraction and countercurrent chromatographic enantioseparation

Using CDs in enantioseparation is rather straightforward. On an analytical level. However, preparation is a completely different question. Potential solutions for this problem and the impact of CD types are explored in the study of Zhejiang University of Technology and Jiaxing University, discussing applications in CPC and liquid-liquid extraction.

See the full article here

Beren Awarded Expedited Roadmap for Treatment of Homozygous Familial Hypercholesterolemia

Fascinating news from Beren Therapeutics:
Beren Awarded Expedited Roadmap for Treatment of Homozygous Familial Hypercholesterolemia
Beren’s novel lead asset, BRN-002, was awarded an Innovation Passport under the United Kingdom’s Innovative Licensing and Access Pathway (ILAP), for the reversal of atherosclerosis in patients with Homozygous Familial Hypercholesterolemia. The ILAP aims to accelerate the time to market for innovative medicines that address the needs of patients with life-threatening or seriously debilitating diseases.
“We are excited to begin work under ILAP and look forward to collaborating with other regulators, payors, and governments to expedite the development and identify and remove access barriers.” – commented Jason Camm, CEO. Jules Payne from HEART UK – The Cholesterol Charity added that “Significant unmet needs remain, and with this advancement, we are hopeful for a new treatment option that can truly alter the course of the disease for the children and patients living with HoFH.”
Beren Therapeutics, P.B.C. is currently in stealth.

See the full article here

Formulations with reduced degradation of polysorbate

Using CDs to formulate proteins, dominantly to prevent aggregation is more or less known; there are CDs marketed for such uses (Roquette – Kleptose Biopharma) still, no product is on the market.
This patent from Genentech (Brian ConnollyLydia HamburgEmily Holz) proposes another feature: when using CDs with monoclonal antibodies, degradation of polysorbates is also reduced.

Fully Symmetric Cyclodextrin Polycarboxylates: How to Determine Reliable Protonation Constants from NMR Titration Data

We are happy to share the most recent paper of Milo Malanga Ph.D. on acid-base properties of cyclodextrin, particularly Sugammadex and its analogs developed together with Semmelweis University (Szabolcs BéniEszter Kalydi), Richter Gedeon Nyrt. / Magyarország (Zoltán Szakács), Gábor Benkovics PhD and Dóra Ujj.
The pH-dependent charge of these compounds can now be accurately calculated in support of designing new analytical methods to exploit their charge-dependent molecular recognition, such as in cyclodextrin-aided chiral capillary electrophoresis.


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

What is the future of cyclodextrin: excipient or API?
A very timely review from University of Debrecen (Gyorgy PanyiFlorina 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

Co-Delivery of 8-Hydroxyquinoline Glycoconjugates and Doxorubicin by Supramolecular Hydrogel Based on α-Cyclodextrin and pH-Responsive Micelles for Enhanced Tumor Treatment

Two birds with one stone:
This study of the Silesian University of Technology and the Polish Academy of Sciences is close to our hearts as we both deal with glycoconjugates and cyclodextrin. They show the delivery of 8-Hydroxyquinoline Glycoconjugates and Doxorubicin using ACD-based hydrogel for enhanced tumor treatment.

Monika D. Gabriela Pastuch Piotr Kurcok 

See the full article here

Molecular docking approach for prediction of enantioseparation of miconazole using cyclodextrin derivatives as chiral selector

I have spent several years studying the chiral recognition of CDs and always considered that selectivity is unpredictable and needs to be tested. In the paper of Jenderal Soedirman University (Ainaya Halwa Lathufa, Uyi Sulaeman, et al.) and Hassan Aboul-Enein enatioseparation of miconazole with molecular docking is predicted using CD derivatives such as sulfated-β-cyclodextrin, hydroxypropyl-β-cyclodextrin, and hydroxypropyl-γ-cyclodextrin as chiral selectors.

See the full article here.

The problem is that all these CDs are composites consisting of hundreds of different specific molecules, which makes proper modeling, so to say, “challenging.” But what do you think?

If you want to vote, click on the link below!

https://www.linkedin.com/posts/tamassohajda_cyclodextrin-chiral-analyticalchemistry-activity-7001422316689608704–S6w?utm_source=share&utm_medium=member_desktop