today’s cyclodextrin:
Not entirely new, yet very important invention by
Daniel Wils and Caroline PERREAU from Roquette: methyl cyclodextrin is presented in the treatment and/or prevention of hepatic steatosis and related diseases via reduced lipid accumulation in the liver.
You can view the complete patent on Espacenet.
Genetically modified cells comprise a cluster of proteins capable of importing an acceptor oligosaccharide of at least three or four monosaccharide units into the cell. These cells are capable of producing human milk oligosaccharides.
Manos A. Papadakis from DSM
See the full patent on Patentscope
Interested in learning about monoclonal antibodies (mABs), how they are made, and what they are used for in research, diagnosis, and therapy?
Here is a nice article by Yuning Wang: What are Monoclonal Antibodies? – Rapid Novor
Cobalt and chromium are constituents of metal alloys for biomedical use, including dental prostheses. Thus, the release of these ions in the human body can lead to harmful biological effects.
The influence of oligosaccharides (α-, β-and γ-cyclodextrin), and a polysaccharide, sodium hyaluronate, on the diffusion of aqueous solutions of cobalt and chromium chlorides is presented by Ana Catarina Ribeiro et al. at Universidade de Coimbra.
It has been found that β-cyclodextrin has the highest interaction towards cobalt and chromium ions. This work will contribute to unveiling the mechanisms responsible for transport by diffusion in aqueous solutions and, therefore, mitigating the potential toxicity inherent to those metal ions.
See the full article on mdpi.com
today’s cyclodextrin:
is bringing again closer the application of metal-organic frameworks to practice in pharma, food, and environmental applications after setting their foot in cosmetics already.
A sustained-release #antibacterial membrane is presented: the cyclodextrin-based metal-organic framework (CD-MOF) and a silver nitrate short-chain alcohol solution are blended to prepare a CD-MOF then combined with caffeic acid short-chain alcohol solution to prepare a CD-MOF loaded with both nano-silver and caffeic acid. Then PDMS is added to obtain a membrane casting solution which is coated onto a membrane support material, performing vacuum drying and stripping from the membrane support material to obtain the antibacterial membrane.
The sustained-release antibacterial membrane can be applied to applied research in the fields of food, environment, etc.
Zhejiang University & Jiangnan University
today’s #cyclodextrin:
Vayamed Cannakits® hits the markets: novel formulation kits enabling a cannabis-enriched Nasal Spray, and Vaginal/Rectal Suppositories is now available. This innovation makes Vayamed the first cannabis company in Germany to expand the therapy spectrum with new dosage forms.
Depending on the final formulation, the kit contains an excipient mixture composed of vegetable oil, hydroxylated fat, and 2-hydroxypropyl-β-cyclodextrin or polyethylene glycol stearate.
Marco Ternelli – Sanity Group
See the full patent on Espacenet
Clinical Degrader Drugs
Targeted protein degradation (TPD) is an emerging field in drug discovery that aims to selectively remove disease-causing proteins from cells. By directly targeting and eliminating proteins, TPD has the potential to address a wider range of disease targets, including those that have been traditionally considered “undruggable.”
Many highly selective PROTAC molecules with improved drug-like properties are entering clinical trials.
Some of the most exciting compounds being profiled are highlighted below
💊Vepdegrestrant (ARV-471), an orally bioavailable estrogen receptor (ER) protein degrader for the treatment of patients with locally advanced or metastatic ER+/HER2- breast cancer.
💊Bavdegalutamide (ARV-110), an orally bioavailable androgen receptor (AR) protein degrader for the treatment of metastatic castration-resistant prostate cancer (mCRPC).
💊ARV-766, an orally bioavailable AR degrader for the treatment of mCRPC.
💊NX-2127, an orally bioavailable Bruton’s tyrosine kinase (BTK), Ikaros (IKZF1) and Aiolos (IKZF3) degrader for the treatment of R/R B cell malignancies.
💊NX-5948, an orally bioavailable BTK degrader for the treatment of R/R B cell malignancies.
💉DT-2216, an IV administered selective B-cell lymphoma-extra large (Bcl-XL) protein degrader for the treatment of T-cell lymphomas.
💉FHD-609, an IV administered BRD9 protein degrader for the treatment of synovial sarcoma.
💊CFT1946, an orally bioavailable mutant BRAF kinase protein degrader for the treatment of various BRAF V600E-driven cancers.
💊CFT8634, an orally bioavailable BRD9 protein degrader for the treatment of synovial sarcoma.
💊KT-474, an orally bioavailable IRAK4 protein degrader for the treatment hidradenitis suppurativa (HS) and atopic dermatitis (AD).
💉KT-413, an IV administered IRAK4, IKZF1 and IKZF3 protein degrader for the treatment of MYD88-mutant B cell lymphomas.
💉KT-333, an IV administered STAT3 protein degrader for the treatment of Peripheral T-cell Lymphoma (PTCL).
💉KT-253, an IV administered MDM2 protein degrader for the treatment of r/r high grade myeloid malignancies and solid tumors.
Tools
💉SD-36, an IV administered STAT3 tool protein degrader.
💉MD-224, an IV administered MDM2 tool protein degrader.
Another amazing summary from Chris De Savi.
today’s cyclodextrin:
CD-based microneedle patches for the delivery of water-insoluble drugs:
A patch incorporates biodegradable microneedles that are fabricated from naturally derived polymer conjugates of gelatin methacryloyl and β-cyclodextrin. When curcumin, an unstable and water-insoluble anticancer therapeutic agent, is loaded as an example, its stability and solubility are improved due to the formation of inclusion complex.
Wujin Sun; Xingwu Zhou
today’s cyclodextrin:
CD-supported capillary gel electrophoresis analysis of proteins and peptides including SDS–protein complexes, by Dániel Sárközy and Andras Guttman from the University of Debrecen. Addition of γ-cyclodextrin to the sheath liquid efficiently removed the SDS content of the sample and the background electrolyte in the flow reactor section by inclusion complexation, while maintaining good separation efficiency and decreasing ion suppression.
This is a fascinating question:
Are LNPs of mRNA drugs mere excipients or part of the drug?
Nanomedicines are complex drugs where components that have typically been regarded as excipients may now be considered part of the active ingredient. The distinction between the active ingredient and excipients for nanomedicines has important consequences for regulatory review and product development. The dissimilarity in the review of the recent RNA-based lipid nanoparticles highlights the need for further regulatory alignment on this topic.
To aid with this journey, both the US FDA and the European Medicines Agency have produced helpful guidelines. These documents, some specifically related to nanomedicines, provide the drug developer with a framework for selecting the appropriate regulatory path towards clinical trials and eventual product approval. The relevant pathway will then determine the type and amount of data that will be required for regulatory review. For example, a novel drug will likely require full Phase I to Phase III clinical trials, whereas a nano-formulation of an existing drug may qualify for an abridged/abbreviated review or as a generic formulation.
Dr. Eva Hemmrich & Scott McNeil
