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CycloLab is committed to support the extension of the current knowledge of cyclodextrins and is actively participating in exploring the limits of their potential applications. CycloLab is open to enter into co-developments and collaborations in the below topics. In case you are interested to learn further details, please
Sugammadex and related compounds
Sugammadex is one of the greatest success in the history of cyclodextrins. There is an increasing interest for this product and for the development of Sugammadex since the recent approval by the FDA is estimated to have a 3-4-fold increase in the global sales of the product.
CycloLab has vast experience in the production of perhalogenated-γ-CD intermediates and have performed several studies to develop Sugammadex, supported by sensitive analytical tools to characterize the products. Our current focus is on the isolation and declaration of primary reference standard materials including the API and its intermediates as well as a great number of custom synthesized potential process impurities.
In order to have a better understanding on what CycloLab offers in this topic, please check out
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Per-anhydro CDs are modified not on the hydroxyls but on the glucose core. They are single CD isomers. This core-modification of the glucopyranose conformation results in fundamental changes of the anhydro-CDs compared to traditional CDs, such as: moderate hydrophobic outer surface and rather hydrophilic inner cavity. This change has many potential uses, like:
application of per-anhydro CDs as complexing agents in immobilizing toxic metals: lanthanides, uranyl- and cobalt-salts in aqueous solutions,
binding radioactive metal wastes, heavy metal toxicants,
in therapy as antidotes for metal intoxications as chelating agents,
in imaging, diagnostics: e.g. as gadolinium complexing agent in MRI tests.
Also, anhydro-CDs may have their own pharmacological effect that CycloLab has been exploring in several therapeutic areas using a family of anhydro CD derivatives.
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Cyclodextrin enabled diclofenac injection (generic Dyloject)
There are several different types of diclofenac injectable formulations - containing 75 mg API - to treat moderate to severe post-operative pain (Akis, Dynapar, Voltaren/Voltarol, Dyloject). Many of these have the disadvantage to contain detergents like TWEEN or co-solvents, have volume above FDA’s guidance, high osmolality or poor physical stability.
CycloLab has developed a ready-to-use formulation with desirable physico-chemical stability, isosmotic property, pH close to interstitial liquid, without detergents or co-solvents, in only 2 mL. Both from a patient compliance and an economic perspective, these products are superior to all those listed above and currently on the market.
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Cyclodextrins as antidotes low-molecular-weight heparins
A family of specific cyclodextrin derivatives have been prepared in order to find a suitable potent inhibitor antidote against Heparin and/or LMWH (low molecular weight synthetic heparins), like a Sugammadex analogue, a tailor-made heparinoid reversal agent for intensive care/therapy. The chemical and technological fine-tuning of the most promising leads is currently ongoing.
In order to have a better understanding on how CDs may be useful as low-molecular-weight heparin antidotes, please check out
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Cyclodextrins in biological products
The use of monoclonal antibodies as therapeutic agents has been increasing steadily over the last decade for the treatment of various conditions. Currently, it is a several multibillion market, and dozens of products have been already approved globally.
There is often a need to deliver a large dose of the protein, so there is a trend toward developing commercially viable liquid formulations of highly concentrated antibodies. Such concentrated solutions are associated with a number of challenges, including optimization of production processes, chemical and physical stability of the final product, preventing aggregation. Also solution viscosity becomes a critical quality attribute.
CycloLab is focusing protein “glyco-engineering”, or physical „glycosylation” of biologics by non-covalent, weak interactions between protein hydrophobic domains, plus to establish electrostatic interactions by finding and designing suitable candidate excipients to overcome these difficulties in biological products, replacing traditional and less safe excipients (e.g. detergents) currently applied in these formulations.
In order to have a better understanding on how CDs may be useful in protein formulations, please check out
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Cyclodextrins as a new class of antibiotics
Many bacteria regulate their cooperative activities through releasing, sensing and responding to small signaling molecules. In infectious diseases the invading bacteria need to reach a critical cell density before they express virulence. Complexation of signal molecules by CDs opens the way for the development of CD-based signal traps – a novel strategy for fighting against bacterial infections via suppressing quorum sensing, the communication between bacterial cells. This concept does not aim to kill the bacteria but to decrease their virulence.
Our current efforts are focused on designing and preparing lead molecules both generally applicable to encapsulate signaling molecules and also specialized for certain bacterial species. These candidates will be suitable to be used in combination products, improving the efficiency of antibiotics, especially against multiresistant bacteria and also as single APIs, adjuvant therapies to slow down the spread of the infection and ease the symptoms.
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