Research & Development
Structure-based Drug Design
Ardea Biosciences uses structure-based drug design, which incorporates multiple scientific disciplines, including biology, crystallography, medicinal chemistry and computer modeling, in order to most efficiently develop new therapeutic candidates.
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Discovery Biology
Structure-based Drug Design
X-Ray Crystallography
Medicinal Chemistry
Our experienced biology team is creating a better understanding of how small molecule drugs interact with targets. This team of scientists clone, express and purify related families of protein targets across multiple therapeutic areas to gain insights into their function. We have developed novel functional and mechanistic assays to guide lead optimization efforts during the early drug discovery process. Additionally, this group is responsible for developing biomarker assays, or tests to determine the biological activity of a compound in humans, that may be used in clinical development to identify patient populations and to guide dosing.
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Structure-based Drug Design
In structure-based drug design, scientists use detailed knowledge of the targeted sites of protein targets associated with particular diseases to design synthetic compounds that fight the disease. The active site of an enzyme is one such example into which a chemical or biological molecule fits to initiate a biochemical reaction. Structure-based drug design aims to create an inhibitor that will bind to the active site of a targeted enzyme, thereby preventing the normal chemical and physiological reaction and ultimately halting the progression of the disease.
Ardea Biosciences' structure-based drug design involves the integrated application of traditional biology and medicinal chemistry along with an array of advanced technologies, including X-ray crystallography and computer modeling of molecular structures, to focus on the active site characterization of the target proteins that control cellular processes related to diseases.
Once a target is selected, researchers use X-ray crystallography to determine the precise three-dimensional molecular structure of the proteins.
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X-ray Crystallography
Reiterative analysis and compound modification are possible because of the structural data obtained by X-ray crystallography at each stage. This capability renders structure-based drug design a powerful tool for rapid and efficient development of drugs that are highly specific for particular protein target sites.
Ardea Biosciences' scientists use X-ray crystallography to determine the structure of its target proteins. This structure is used to design potential compounds that will fit the active site of the target. Scientists then use crystallography to study how compounds bind with the active site of the target protein. Using information gained through crystallography, researchers refine the compounds to improve their performance. The redesigned lead compound is then synthesized and further refined and analyzed in a reiterative process.
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Medicinal chemistry is a scientific discipline at the intersection of chemistry and pharmacy involved with designing, synthesizing and developing pharmaceutical drugs. Medicinal chemistry involves the identification, synthesis and development of new chemical entities suitable for therapeutic use. It also includes the study of existing drugs, their biological properties, and their quantitative structure-activity relationships. It is a highly interdisciplinary science combining organic chemistry with biochemistry, computational chemistry, pharmacology, molecular biology, statistics, and physical chemistry.
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Process chemistry results in pharmaceutical manufacturing routes that are safe, efficient, and scalable. It is sometimes referred to as the interface of organic chemistry with business. The chemistry itself is an applied form of organic chemistry targeted at specific molecules. It's more than just the ability to make the molecule. It's the ability to make it with a high degree of specificity and quality, cost effectively, with low impact on the environment.
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Pharmaceutical Development
The aim of pharmaceutical development is to design a quality product with a manufacturing process that consistently delivers the intended performance of the product. The information and knowledge gained from pharmaceutical development studies and manufacturing experience provide scientific understanding to support the establishment of the design space, specifications and manufacturing controls. Through pharmaceutical development, the dosage form and formulation are determined, including those aspects of drug excipients, container closure systems, and manufacturing processes that are critical to product quality.
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Preclinical Development
Preclinical development is a stage in the development of a new drug that begins before clinical trials (testing in humans) can begin, and during which important safety and pharmacology data is collected. The primary goals of preclinical studies are to determine a drug's pharmacodynamics (PD), pharmacokinetics (PK), absorption, distribution, metabolism and excretion (ADME), and toxicity through animal testing. This data allows researchers to allometrically estimate a safe starting dose of the drug for clinical trials in humans. Typically, both in vitro and in vivo tests will be performed. Studies of a drug's toxicity include which organs are targeted by that drug, as well as if there are any long-term carcinogenic effects or toxic effects on mammalian reproduction. The information collected from these studies is vital so that safe human testing can begin.
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Clinical Development-Regulatory
We have assembled expertise in both clinical development and regulatory affairs, including quality assurance, through our employees and consultants. Our in-house Quality Assurance Unit oversees the conduct of GLP bioanalytical and analytical chemistry work. Ardea Biosciences is building relationships and accessing thought leaders with key academic medical centers for viral diseases, cancer and inflammatory diseases, which we believe will facilitate clinical trial design and choice of patient population for our therapeutic products. We also use quantitative, selective measures of biologic activity as related to a drug’s mechanism of action or biomarkers, as an integral element of our clinical design strategy to select patients, predict clinical dose and optimize clinical development.
Regulatory authorities require preclinical testing and three phases of human clinical trials of increasing complexity to prove the safety and efficacy of every new product. Clinical Development at Ardea oversees the clinical testing of all potential products, though the actual testing is conducted in collaboration with physicians and other medical personnel at medical centers throughout North America and Europe.
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Our experienced biology team is creating a better understanding of how small molecule drugs interact with targets. This team of scientists clone, express and purify related families of protein targets across multiple therapeutic areas to gain insights into their function. We have developed novel functional and mechanistic assays to guide lead optimization efforts during the early drug discovery process. Additionally, this group is responsible for developing biomarker assays, or tests to determine the biological activity of a compound in humans, that may be used in clinical development to identify patient populations and to guide dosing.
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