PUBLICATION ALERT JUNE 2020
FORMULATION FORUM – Application of Captisol® Technology to Enable the Formulation of Remdesivir in Treating COVID-19
James Pipkin, PhD, Vince Antle, PhD, and Rebecca Garcia-Fandiño, PhD, explain why more Captisol® than ever is required to meet Gilead’s bold goals of making remdesivir available to COVID-19 patients in the US and to hundreds of countries around the world.
OPTIMIZED DRUG SOLUBILITY & STABILITY
Captisol is the trade name for Ligand’s solvent-free processed modified cyclodextrin preparation. Captisol is a patent-protected mixture of chemically modified cyclodextrins with a modifying structure to optimize drug solubility and stability. Captisol was invented and developed by scientists at the University of Kansas’ Higuchi Biosciences Center specifically for drug development and formulation.
Captisol overcomes solubility and stability hurdles faced during each phase of development. Captisol can make a substance more soluble and an agent more stable. Captisol can convert a solid to a liquid or an oil to an aqueous solution. Combinatorial chemistry, high throughput screening (HTS), and molecular genetics have led to an increase in the number of insoluble and unstable molecules, peptides, and proteins being investigated for their therapeutic activity. There are currently more than 50 Captisol-enabled products in clinical development. This unique technology has enabled several FDA-approved products, including Amgen’s KYPROLIS®, Baxter International’s
NEXTERONE®, Gilead’s VEKLURY®, Acrotech Biopharma L.L.C.’s and CASI Pharmaceuticals’ EVOMELA®, Melinta Therapeutics’ BAXDELATM and Sage Therapeutics’ ZULRESSOTM. There are many Captisol-enabled products currently in various stages of development.
SEAMLESS TRANSITION TO CLINICAL TRIALS
Captisol may increase systemic exposure for toxicology studies of investigative compounds and has a proven clinical safety record. In early development, Captisol formulation can lead to a seamless transition from nonclinical safety to clinical trials. Captisol-enabled products are approved in more than 60 countries.
MULTIPLE ADMINISTRATION ROUTES ENSURE TARGETED DELIVERY
Captisol’s chemical structure was designed to create new products by improving solubility, stability, bioavailability, and dosing of active pharmaceutical ingredients. Routes of administration investigated include parenteral, oral, ophthalmic, nasal, topical, and inhalation products. Once inside the body, Captisol releases the drug agent, which then travels to its target. The interaction between Captisol and the agent is not permanent, and Captisol is safely expressed from the kidneys.
PATENTED & VALIDATED MANUFACTURING
Of all modified cyclodextrins, Captisol is an ingredient in the most approved products in the U.S. Manufactured under cGMP, at multiple locations, using a patented and validated all-aqueous process, annual manufacturing capacity is being increased to 500 MT. Captisol is supplied in ultralow endotoxin, ultra-low bioburden, low-chloride forms in 100g, 1kg, 5kg, and 20kg packages for R&D use. Commercial pack sizes include 1kg, 5kg, and 20kg, with the ability to fill metric-ton orders.
Posted Date: 12/3/2020
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