Selective removal of 7-ketocholesterol by a novel atherosclerosis therapeutic candidate reverts foam cells to a macrophage-like phenotype

Today’s cyclodextrin:

Say hello to Cyclarity Therapeutics‘s UDP-003, a promising new therapeutic that goes beyond managing atherosclerosis — it aims to reverse it by targeting one of its nastiest culprits: 7-ketocholesterol (7KC), a toxic oxidized form of cholesterol. 🧨🧬

Here’s what the science says:
🧼 UDP-003 selectively removes 7KC, a molecule notorious for turning immune cells into dysfunctional foam cells — the building blocks of atherosclerotic plaque
🔄 By clearing out 7KC, foam cells regain their phagocytic power and reduce harmful features like oxidative stress and lipid accumulation
🧲 The treatment downregulates CD47, a “don’t eat me” signal, and restores efferocytosis, helping clean up dead cells in plaques
🚽 7KC is not just neutralized — it’s flushed out via urine, suggesting effective systemic detox
✅ Preclinical safety looks good, and a Phase 1 clinical trial is already underway!

💡 Bottom line: By targeting the molecular root — not just the symptoms — of atherosclerosis, UDP-003 could become the first truly disease-modifying therapy for this global cardiovascular killer 🛡️❤️

Selective removal of 7-ketocholesterol by a novel atherosclerosis therapeutic candidate reverts foam cells to a macrophage-like phenotype – Atherosclerosis

HPBCD will be dosed in patients with diabetic kidney disease in Q2 2025

Today’s cyclodextrin:
ZyVersa Therapeutics Inc.‘ Cholesterol Efflux Mediator VAR 200 (HPBCD) will be dosed in patients with diabetic kidney disease in Q2 2025.

The first patient is expected to be treated in a phase 2a clinical trial in patients with DKD by the end of June of 2025. The intent of the study is to obtain renal patient proof-of-concept for VAR 200 prior to initiating a larger phase 2a/b for VAR 200’s lead indication, FSGS. The DKD study will evaluate VAR 200’s safety and efficacy (% change in proteinuria from baseline to week 12) in eight patients with type 2 diabetes who have diabetic kidney disease. This data will provide insights for designing the subsequent phase 2a/b FSGS study. The DKD study will be conducted at two clinical research sites.

I cannot wait to see how this goes!
ZyVersa Therapeutics Reports First Quarter 2025 Financial Results and Highlights Pipeline Progress :: ZyVersa Therapeutics, Inc.

Fascinating Hungarian invention in ophthalmic application

After oral and parenteral formulation, ophthalmics are the 3rd most popular for cyclodextrin use.

Here is a fascinating Hungarian invention in the field of ophthalmology from Semmelweis University and University of Szeged.

US20250108034 EYE DROP FORMULATION

An ocular formulation comprising a cyclodextrin-formulated L-Ascorbic acid 6-palmitate (ASP), preferably for the treatment of fibrosis in the cornea, corneal haze, and wound.

Heartiest congratulations to György Tibor Balogh, PhD, DSc, dr. habil and his team and Gábor Katona, Ildiko Csoka and their team.

We hope to see many more of similar great solutions to come!

Optimizing 6-benzylaminopurine for micropropagation: A cyclodextrin monomers and polymers approach

What a personal milestone!

Our youngest one, Dani Bisericaru was still at Università degli Studi di Torino when he did this work that now led to his first first-author paper.

Special gratitude goes to Francesco Trotta and Adrián Matencio Durán for their excellent mentorship of Dani that we enjoy to this very day at CarboHyde.

So check out and learn how this research lays the foundation of the eco-friendly use of cyclodextrin-based polymers for micropropagation improvement.

Optimizing 6-benzylaminopurine for micropropagation: A cyclodextrin monomers and polymers approach – ScienceDirect

Exceptional stability of the sugammadex-solasodine complex: Insights from experimental and theoretical studies

A new paper out!

Sugammadex (SGM) is the first cyclodextrin (CD)-based selective relaxant binding agent. We investigated its ability to capture natural aminosteroid phytotoxins, and assessed its potential as an antidote for intoxication.

SGM significantly increased cell survival and reduced Solasodine (the toxic alkaloid chosen as model compound) toxicity in mHippoE-14 mouse hippocampal embryonic cells, supporting the hypothesis that SGM could act as an antidote to SS’s toxic effects.

Special thanks for the fantastic teamwork:
Eszter KalydiSemmelweis University
Fanni Sebák, Éva Moussong József Kardos, Andrea Bodor Szabolcs BéniEötvös Loránd University
Béla FiserUniversity of Miskolc
Babak MinofarUniversity of Lodz
Milo Malanga PhD – CarboHyde

Exceptional stability of the sugammadex-solasodine complex: Insights from experimental and theoretical studies – ScienceDirect

Formulation and investigation of differently charged β-cyclodextrin-based meloxicam potassium containing nasal powders

Today’s cyclodextrin is a nice formulation study from one of the best Hungarian pharmaceutical universities, the University of Szeged, who study various excipients – CDs among others – that have an important role in nasal formulations to increase the permeability of the mucosa and prolong the residence time of the drug.

The charged cyclodextrin-based formulations showed significantly higher adhesive force values regardless of the presence of PVA. The drug release was fast and complete, and the permeation of meloxicam was enhanced.

Patricia Varga, Anett Németh, Scarlett Zeiringer, Eva Roblegg, Budai-Szűcs Mária, Csilla Balla-Bartos, Rita Ambrus

Formulation and investigation of differently charged β-cyclodextrin-based meloxicam potassium containing nasal powders – ScienceDirect

The application of cyclodextrins in drug solubilization and stabilization of nanoparticles for drug delivery and biomedical applications

Not many things get better with years passing but some do.
Things like:
– whiskey,
– wine
– blue jeans
– friendships
and Thorsteinn Loftsson

This was my first thought when reading this paper, which I coauthored with Hay Man Saung Hnin Soe and Phatsawee Jansook on cyclodextrin-based nanoparticles.

This review emphasizes the role of cyclodextrins (CDs) in stabilizing colloidal nanoparticles (NPs) and improving drug solubility. The integration of CDs with NPs offers a synergistic strategy that enhances drug delivery and expands the scope of biomedical applications. Furthermore, the review thoroughly explores the potential of CDs to boost the stability and therapeutic effectiveness of colloidal NPs, positioning them as promising candidates for advanced drug delivery systems

The application of cyclodextrins in drug solubilization and stabilization of nanoparticles for drug delivery and biomedical applications – ScienceDirect

Axsome Therapeutics Announces FDA Acceptance of NDA Resubmission for AXS-07 for the Acute Treatment of Migraine

Today’s cyclodextrin update brings news of the 2nd oral drug to be marketed using sulfobutylether-beta-CD.

Axsome Therapeutics, Inc. has announced that the U.S. FDA has acknowledged the resubmission of the NDA for AXS-07, an oral, rapidly absorbed, multi-mechanistic investigational medicine for the acute treatment of migraine. AXS-07 combines MoSEIC™ meloxicam and rizatriptan, offering a new molecular entity for migraine treatment enabled by Axsome’s innovative technology.

About Migraine
Migraine is a serious neurological condition characterized by recurrent attacks of pulsating, often severe and disabling head pain associated with nausea, sensitivity to light, and sensitivity to sound. An estimated 39 million Americans suffer from migraine, and it is the leading cause of disability among neurological disorders in the United States according to the American Migraine Foundation. Published surveys of migraine sufferers found that more than 70% are not fully satisfied with their current treatment and desire therapies that work faster, more consistently, and result in less symptom recurrence.

About AXS-07
AXS-07 is a novel, oral, rapidly absorbed, multi-mechanistic investigational medicine for the acute treatment of migraine, consisting of MoSEIC™ meloxicam and rizatriptan. Meloxicam is a new molecular entity for migraine enabled by Axsome’s MoSEIC (Molecular Solubility Enhanced Inclusion Complex) technology, which results in rapid absorption of meloxicam while maintaining a long plasma half-life. Meloxicam is a COX-2 preferential non-steroidal anti-inflammatory drug and rizatriptan is a 5-HT1B/1D agonist. AXS-07 is designed to provide rapid, enhanced and consistent relief of migraine, with reduced symptom recurrence. AXS-07 is covered by more than 200 issued U.S. and international patents which provide protection until at least 2038. AXS-07 is not approved by the FDA.

Axsome Therapeutics Announces FDA Acceptance of NDA Resubmission for AXS-07 for the Acute Treatment of Migraine | Axsome Therapeutics, Inc. (gcs-web.com)