Axsome’s Symbravo: FDA-Approved Migraine Treatment Featuring Cyclodextrin-Based Delivery

More than two and a half years after the FDA rejected its migraine treatment, Axsome Therapeutics, Inc. received an approval for the drug on Thursday to treat acute migraines with or without aura. The drug, previously called AXS-07, will be branded as Symbravo.

The oral drug, branded Symbravo, was approved for the acute treatment of the condition characterized by recurrent attacks of moderate to severe throbbing and pulsating pain on one side of the head.

Symbravo is a combination drug with a drug delivery system called MoSaic that contains also meloxicam encapsualted in the cavity of sulfobutyl-BCD.

This will be the 2nd oral formulation containing SBECD on the market.

CarboHyde at University of Szeged

Just when you thought you knew everyting about cyclodextrins…

It could be a fascinating Hollywood movie title, yet now, this is the keynote Balázs Attila Kondoros delivered this morning at a conference (Symposium of Young Researcher on Pharmaceutical Technology, Biotechnology and Regulatory Science) for young formulation scientists at University of Szeged.

Later Tamas Kiss, PhD was chairing a session too, so our team members got important roles today.

Also, the conference, features almost 10 presentations about cyclodextrin applications. Such active research in the area is both heartwarming and reassuring.

Cationic Cyclodextrin-Based Carriers for Drug and Nucleic Acid Delivery

Today’s cyclodextrin:
Check out our latest review fresh from the oven on cationic cyclodextrins for drug and nucleic acid delivery.

This contribution to science is a fruit of our collaboration with Eötvös Loránd University and Semmelweis University (Szabolcs Béni and Adila Nazli).

Special thanks to Milo Malanga PhD as well as Bicyclos HEurope for the funding.

Cationic Cyclodextrin-Based Carriers for Drug and Nucleic Acid Delivery

Can cyclodextrins inactivate Zika virus?

This great study from University of Nebraska-Lincoln and University of South Dakota deals with the correlation of BCD and ZIKV inactation.

While its not clear totally what kind of CD is used, results show that BCD can inactivate or ‘sterilize’ ZIKV in cell culture fluids and is immunogenic in mice opening the possibility of creating a vaccine.

Zika virus (ZIKV) infection is associated with life-threatening diseases in humans. To date, there are no available FDA-approved therapies or vaccines for the specific treatment or prevention of ZIKV infection. Variation in the ZIKV envelope protein (Env), along with its complex quaternary structure, presents challenges to synthetic approaches for developing an effective vaccine and broadly neutralizing antibodies (bnAbs). We hypothesized that beta-cyclodextrin (BCD) could be used to uniquely inactivate infectious ZIKV without disruption of Env.

Potential applications:
– BCD-inactivated ZIKV can be used as a safe substrate in assays for the evaluation of vaccine and antibody candidates that require intact Env proteins.
– Topical products containing BCD can possibly be used as prophylaxis to protect against sexually transmitted ZIKV infection.
– BCD-inactivated ZIKV is immunogenic in mice, raising the possibility that this product could be directly used to produce an effective vaccine or novel therapeutic antibodies.

Inactivation of Zika Virus with Hydroxypropyl-Beta-Cyclodextrin

carbohyde, zika virus, cyclodextrin

Can cyclodextrins and dextrans revolutionize gut health?

This review highlights the exciting potential of these compounds to support the gut microbiome. Conducted in collaboration with Université Clermont Auvergne, the study was authored by Anna G. and Emmanuelle Lainé, under the supervision of Judyta Cielecka-Piontek.

It explores how cyclodextrins and dextrans can promote the growth of beneficial bacteria like Bifidobacterium and Lactobacillus and enhance the production of short-chain fatty acids essential for gut health. This review also sheds light on their overlooked prebiotic potential.

The gut microbiome plays a key role in digestion, metabolism, and overall vitality.

Dive into the insights provided in this comprehensive review: How Do Cyclodextrins and Dextrans Affect the Gut Microbiome? Review of Prebiotic Activity

Methyl-Beta-Cyclodextrin Restores Aberrant Bone Morphogenetic Protein

Today’s cyclodextrin is about their potential in osteoporosis.

This paper was published by University of Delaware who found that after treating bone marrow stromal cells with methyl-β-cyclodextrin, a disruptor of cellular endocytosis, bone morphogenetic protein (BMP) signaling is restored in 15-month-old mice, as shown by von Kossa assays.

MβCD has the potential to restore BMP receptor type Ia function, and the BMP signaling pathway offers a promising avenue for future OP therapies.

Congrats to Daniel Halloran, Venu Pandit, Kelechi Blessing Chukwuocha and Anja Nohe for their great work!

Methyl-Beta-Cyclodextrin Restores Aberrant Bone Morphogenetic Protein 2-Signaling in Bone Marrow Stromal Cells Obtained from Aged C57BL/6 Mice

Degradable plastics including movable cyclodextrin crosslinking units

Today’s cyclodextrin is about enforcing recyclable plastic with CDs.

A collaborative work performed by Nara Laboratory, Kyoeisha Chemical Co. and various departments of Osaka University might make a step further in achieving a sustainable society with the development of advanced degradable plastics including movable cyclodextrin crosslinking units.

In a study published recently in Chem [link to the artickle], the researchers have revealed that developing polymers with movable crosslinks not only increases their strength but also promotes degradation by enzymes under mild conditions.

The movable crosslinks are cyclodextrins, which are threaded on one polymer strand and attached to another, endowing the resulting plastics with increased toughness and durability. Cyclodextrins being nontoxic, biodegradable, and widely available, making them attractive as a polymer component.

The cyclodextrin crosslinks also enabled the degradation of the polymers during subsequent enzymatic treatment because their bulky structure increased the free volume in the polymer network, which improved access of the enzyme to the target cleavage sites on the polymer chains.

These advanced biodegradable plastics can readily be broken down by enzymes into useful precursor molecules that could be reused in further materials, suppressing waste generation and contributing to the development of a sustainable industry.

Preparation of ingredients for producing bread with reduced glycemic index 

Today’s cyclodextrin is about producing bread, of course, with a low glycemic index.

This invention from Universidad de Granada describes a preparation of ingredients that includes alpha-cyclodextrin and other ingredients. These ingredients permit the production of a dough suitable for traditional processing and making bread with a reduced glycemic index.

This preparation adds at least 5 g ACD to 50 g starch.

In the Scientific Opinion of the Panel on Dietetic Products, Nutrition and Allergies of the European Food Safety Authority (EFSA), two intervention studies showed that alpha-cyclodextrin added to starch significantly affected the postprandial glycemic response without disproportionately increasing the postprandial insulin response. This did not occur when it was added to sucrose.

Based on the data presented, the Panel concluded that a cause-and-effect relationship is established between the consumption of alpha-cyclodextrin with starch-containing meals and a reduction of postprandial glycemic response. The panel considers that at least 5 g of alpha-cyclodextrin per 50 g of starch should be consumed to obtain the claimed effect.

The target population of this health claim is adults who wish to reduce their postprandial glycemic response [EFSA. Scientific Opinion on the substantiation of health claims related to alpha-cyclodextrin and reduction of post-prandial glycaemic responses (ID 2926, further assessment) according to Article 13 (1) of Regulation (EC) No 1924/2006. EFSA Journal 2012 10 (6): 2713].

You can read the patent here: Espacenet – Description

carbohyde, alfa-cyclodextrin, producing bread