Gilead’s Captisol-enabled Remdesivir Approved for Use in Renally Impaired Patients
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How it Works

How It Works

Traditional formulation systems for very insoluble and/or unstable active pharmaceutical ingredients (APIs) have involved a combination of organic solvents, surfactants and extreme pH conditions. These formulations may precipitate upon injection, or may cause irritation and adverse reactions. At times, these approaches are inadequate for solubilizing enough active agent for a preferred formulation.

Captisol® Solubilizes

Neutral, cationic and anionic APIs have been effectively associated with Captisol®. Aqueous solubilities have increased by a factor of 10 to 25,000, depending on the compound. In contrast to other solubilization technologies, product or traditional formulation system, the feasibility and solubility effectiveness of Captisol® can be rapidly assessed with a few simple lab experiments.

Captisol® Facilitates Delivery

Typically, the inherent pharmacokinetics and pharmacodynamics of the drug are unaffected by Captisol®, however onset may be manipulated and dose sparing maybe observed compared to classical formulations such as co-solvent based, emulsions or suspensions. Upon administration, Captisol® is readily and essentially completely renally eliminated. Captisol® formulations are biocompatible and can be administered parenterally, orally, ophthalmically, nasally, topically and via inhalation.

Captisol® is Safe

Captisol® was designed to maximize safety by eliminating the potentially damaging effects produced by the parent beta-cyclodextrin. In-vitro experiments and in-vivo acute, subchronic and chronic toxicity studies have provided safety data to support the development and approval of Captisol® drug formulations in man.

Captisol® Stabilizes

Interaction with Captisol® provides a beneficial and protected environment for the API in its lipophilic cavity, while Captisol's hydrophilic surface provides excellent water solubility- boosting both solubility and stability. Interaction of the API with Captisol® can reduce decomposition by protecting labile regions from the potential reactants in the aqueous environment. 

Captisol® Facilitates Faster Development

Using Captisol® early in the development process can increase the number of candidates that can be evaluated, decrease development time and increase lead candidate survivability. Captisol® enables an aqueous formulation for many water insoluble APIs as oral, nasal, topical, ophthalmic or liquid-presented medications. 

Captisol®, a Validated Technology

These commercial products are marketed around the world.

Baxter International Baxter International
Pfizer Pfizer
Pfizer Pfizer
Pfizer Pfizer
Amgen Amgen
Acrotech Acrotech
Merck Merck
Lundbeck Lundbeck
Melinta Melinta
Gilead Gilead
Bristol Myers Squibb Bristol Myers Squibb
Sage Sage
Sedor Sedor
Novartis Novartis