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vital statistics - Protagonist Therapeutics
vital statistics - Protagonist Therapeutics

... unique therapeutic potential, but, in the traditional oral formulations, peptides have serious drawbacks in stability and pharmacokinetic properties. “Our intent is to create novel chemical entities that will capture the best of both worlds, meaning the convenience and PK (pharmacokinetics) characte ...
The Horse: Drugs for the Deworming War
The Horse: Drugs for the Deworming War

... animal testing, and the generic manufacturer's only burden of proof is chemical identity. While a patent is in effect, the manufacturer of a drug operates in the absence of competition and can charge what the market will bear. Generic drugs generally can be sold at lower prices, however, because dev ...
Bioavailability - physicochemical and dosage form factors
Bioavailability - physicochemical and dosage form factors

... The concentration of drug in solution in the bulk of the gastrointestinal fluids will be influenced by such factors as the rate of removal of dissolved drug by absorption through the gastrointestinal- blood barrier, and by the volume of fluid available for dissolution, which will be dependent on the ...
oral bioavailability and first-pass effects
oral bioavailability and first-pass effects

... only assumptions are linear pharmacokinetics and constant clearance between treatments. These methods are also suitable for the assessment of metabolite bioavailability after drug administration and the quantitative determination of sites of biotransformation and metabolite formation in vivo. ...
Ming Li Talk about Bioinformatics
Ming Li Talk about Bioinformatics

... protein folding and stability. ...
Drugs of Abuse
Drugs of Abuse

... Some psychoactive drugs, such as phenothiazines, haloperidol, and tricyclic antidepressants are not included in this classification of "psychoactive drugs of abuse" because they are seldom chronically abused. ...
The Development of Deuterium-Containing Drugs
The Development of Deuterium-Containing Drugs

... that has received little attention to date – but when applied to compounds with well-understood therapeutic utility, selective deuteration can be used to create new drugs that address significant unmet medical needs. Selective incorporation of deuterium in place of hydrogen (deuteration) has the uni ...
One drug trial, six men, disaster… - Direct-MS
One drug trial, six men, disaster… - Direct-MS

... that would eventually dampen down the immune system. But published studies examined by New Scientist suggest that its action on T-cells, far from having the intended effect, led to the violent and uncontrolled reactions seen in the drug trial. TGN1412 is a monoclonal antibody, a class of drug design ...
The Development of Deuterium-Containing Drugs
The Development of Deuterium-Containing Drugs

... that has received little attention to date – but when applied to compounds with well-understood therapeutic utility, selective deuteration can be used to create new drugs that address significant unmet medical needs. Selective incorporation of deuterium in place of hydrogen (deuteration) has the uni ...
Adverse Drug Reactions to Antibiotics and Major Antibiotic Drug
Adverse Drug Reactions to Antibiotics and Major Antibiotic Drug

... These reactions occur owing to interaction between the drug and a circulating or membranebound protein (drug-induced hemolytic anemia) to cause production of a circulating antibody of the IgG ot IgM class with subsequent complement activation The most common target for this type of immune-mediated d ...
No End in Sight: The Abuse of Prescription Narcotics
No End in Sight: The Abuse of Prescription Narcotics

... All derivatives of the opium poppy are classified as narcotics and share common properties in the brain. All narcotics enter through the central nervous system (brain and spinal cord) to exert  their  effects.  In  the  brain  they  bind  to  specific  opioid  “receptors”  (so-called  “G-protein cou ...
Table of Valid Genomic Biomarkers in the Context of
Table of Valid Genomic Biomarkers in the Context of

... side of the drug name. All approved drugs in this table are linked to labels at Drugs@FDA which can be accessed by clicking over symbols under the left side of the drug name. The table will be updated on a quarterly basis. The information provided in “label context” is taken from different sections ...
5.5 Illicit drug use—current and future issues
5.5 Illicit drug use—current and future issues

... Use and misuse of pharmaceutical drugs including opioids Pharmaceutical drugs provide a broad range of benefits to improve the health and quality of life of Australians. The fact that some medicines are also subject to misuse does not detract from these benefits. However, pharmaceutical misuse is an ...
H INHIBITORS OF HIV-1 REVERSE TRANSCRIPTASE  Research Article
H INHIBITORS OF HIV-1 REVERSE TRANSCRIPTASE Research Article

... Objective: In the present study, we have designed and synthesized 15 novel 3-(1,3-dioxo-3a,4-dihydro-1H-isoindol-2(3H,7H,7aH)-yl)-N-(substituted phenyl) propanamide 4(a-o) analogs. Methods: Docking studies for all the derivatives 4(a-o) were performed using molecular modeling software autodock 4.2. ...
Slide 1
Slide 1

... fulfill all the properties that are required from a drug (e.g. physicochemical and ADME/Tox properties). Pharmacophore can direct chemists to include/exclude specific chemical groups. ...
Essay B5 Chem 151 Professor Whitesell Amphetamines Imagine for
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... as sulfate salt under the drug name Adderall is prescribed as a treatment for attention deficit hyperactive disorder (ADHD). Adderall is a racemic mixture of dextroamphetamine and levoamphetamine (the D and L forms of the drug). Interestingly, it was found that dextroamphetamine form has a stronger ...
Drugs and Toxicology
Drugs and Toxicology

... is all that is necessary (“aggregate weight based law”)  Quantitative analysis indicates how much of that sample is made up of a controlled substance (percentage of the total for each controlled substance present in a sample) © 2007 The McGraw-Hill Companies, all rights reserved. ...
Oral Absorption and the Biopharmaceutics Classification
Oral Absorption and the Biopharmaceutics Classification

... diffusion is the most predominant pathway for drug absorption, while paracellular diffusion is usually absent when molecules are larger than approximately 200 Dalton (4). However, small hydrophilic molecules such as water can cross the intercellular space readily. Disease states may increase the cha ...
Slides - Stanford University
Slides - Stanford University

... Stochastic simulation on a roadmap and MC simulation converge to the same distribution p (Boltzman): For any set S, e>0, d>0, g>0, there exists N such that a roadmap with N milestones has error bounded by: ...
STRUCTURAL ACTIVITY RELATIONSHIP AMONG THE
STRUCTURAL ACTIVITY RELATIONSHIP AMONG THE

... • SARS is the study of relationship between a drug’s molecular structure and the drug’s biological activity. ...
bluecrossca formulary
bluecrossca formulary

... Pacific Blue Cross. 2. HEPATITIS C DRUGS — There are new treatments for Hepatitis C that are considered cures in virtually all patients. The course of treatment is typically 8 to 12 weeks, and up to 24 weeks in certain cases. Treatment costs $50,000 to over $130,000 per patient, depending on the dr ...
The Organic Chemistry of Drug Design and Drug Action
The Organic Chemistry of Drug Design and Drug Action

... FIGURE 3.17 (A) Dose–response curve for a full inverse agonist (Z); (B) effect of a competitive antagonist on the response of a full inverse agonist (a, b, and c represent increasing concentrations of the added antagonist or natural ligand to Z); and (C) dose–response curve for a partial inverse ago ...
Parkinson`s Disease (PD) and Treatment
Parkinson`s Disease (PD) and Treatment

... Drug therapy – MAO-B Inhibitors MAO-B is an enzyme that metabolizes dopamine.  From the breakdown of dopamine, hydrogen peroxide is produced, which the oxidative stress can damage dopaminergic neurons in the substantia nigra. (Possibly neuroprotective)  MAO-B inhibitor delays or reduces the metab ...
FORMULATION AND EVALUATION OF SUSTAINED RELEASE MULTIPLE EMULSION OF HYDROXYPROGESTERONE Research Article
FORMULATION AND EVALUATION OF SUSTAINED RELEASE MULTIPLE EMULSION OF HYDROXYPROGESTERONE Research Article

... of the drug diffused out was relatively small. The resulting emulsions by this simplified and less energy intensive processes complies with droplet size requirements and are stable over several months. Keywords: Parenteral emulsions, Formulation, Hydroxyprogesterone caproate, Multiple emulsions. INT ...
Montse Fabrega`s presentation
Montse Fabrega`s presentation

... C. Biomedical applications: structure-based drug design ...
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Drug design



Drug design, sometimes referred to as rational drug design or simply rational design, is the inventive process of finding new medications based on the knowledge of a biological target. The drug is most commonly an organic small molecule that activates or inhibits the function of a biomolecule such as a protein, which in turn results in a therapeutic benefit to the patient. In the most basic sense, drug design involves the design of molecules that are complementary in shape and charge to the biomolecular target with which they interact and therefore will bind to it. Drug design frequently but not necessarily relies on computer modeling techniques. This type of modeling is often referred to as computer-aided drug design. Finally, drug design that relies on the knowledge of the three-dimensional structure of the biomolecular target is known as structure-based drug design. In addition to small molecules, biopharmaceuticals and especially therapeutic antibodies are an increasingly important class of drugs and computational methods for improving the affinity, selectivity, and stability of these protein-based therapeutics have also been developed.The phrase ""drug design"" is to some extent a misnomer. A more accurate term is ligand design (i.e., design of a molecule that will bind tightly to its target). Although design techniques for prediction of binding affinity are reasonably successful, there are many other properties, such as bioavailability, metabolic half-life, side effects, etc., that first must be optimized before a ligand can become a safe and efficacious drug. These other characteristics are often difficult to predict with rational design techniques. Nevertheless, due to high attrition rates, especially during clinical phases of drug development, more attention is being focused early in the drug design process on selecting candidate drugs whose physicochemical properties are predicted to result in fewer complications during development and hence more likely to lead to an approved, marketed drug. Furthermore, in vitro experiments complemented with computation methods are increasingly used in early drug discovery to select compounds with more favorable ADME (absorption, distribution, metabolism, and excretion) and toxicological profiles.
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