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  • hydroxyl
  • A method is provided for converting therapeutic glycosidase inhibitors to novel prodrugs by phosphorylation of a free hydroxyl group on the molecule to substantially reduce the glycosidase inhibitory activity without thereby substantially reducing the therapeutic activity. (google.es)
  • ester
  • Viread is a carbonate-based prodrug, as opposed to the ester-based prodrugs mentioned previously. (wikibooks.org)
  • The carbonate group contained in this prodrug has been found to be more stable than the ester groups contained in the aforementioned prodrugs, while maximum absorption is reached more slowly. (wikibooks.org)
  • Liguzinediol (LZDO) ester prodrugs 3 - 5 were synthesized and evaluated in vitro and in vivo for their potential use in prolonging the half-life of the parent drug LZDO ( 1a ) in vivo . (mdpi.com)
  • The drug is a phosphate ester and prodrug of miproxifene (DP-TAT-59) with improved water solubility that was better suited for clinical development. (wikipedia.org)
  • Miproxifene is the active metabolite of miproxifene phosphate (TAT-59), a phosphate ester and prodrug of miproxifene that was developed to improve its water solubility. (wikipedia.org)
  • compound
  • The Mixed-Type compound can be further distinguished as a Parallel Mixed-Type or Sequential Mixed-Type prodrug depending on the conversion processes that proceed with, either in concurrent or in sequential steps. (mdpi.com)
  • However, some prodrugs lack an obvious carrier or promoiety but instead result from a molecular modification of the prodrug itself, which generates a new active compound. (aspetjournals.org)
  • The half-life of the parent compound was prolonged after intragastric administration of prodrug 3 , which was found to be a superior prodrug candidate for increasing myocardial contractility. (mdpi.com)
  • A prodrug is a medication or compound that, after administration, is metabolized (i.e., converted within the body) into a pharmacologically active drug. (wikipedia.org)
  • However, terfenadine was discovered to be the prodrug of the active molecule, fexofenadine, which does not carry the same risks as the parent compound. (wikipedia.org)
  • Loratadine, another non-sedating antihistamine, is the prodrug of desloratadine, which is largely responsible for the antihistaminergic effects of the parent compound. (wikipedia.org)
  • drug
  • Looking on how the human body converts the prodrug into the final active drug form, there are actually two major types of prodrugs. (wikibooks.org)
  • Esters are found most commonly in commercial prodrugs, such as the drug oseltamivir. (wikibooks.org)
  • In this paper, a new classification system for prodrugs is proposed to provide useful information about where in the body a prodrug is converted to the active drug. (mdpi.com)
  • In conclusion, the new system of classification will add to existing knowledge of prodrug classifications, and will provide improved insight into the contributory roles of both prodrug and active drug in the product's efficacy and safety, and their risk-benefit assessment. (mdpi.com)
  • Compounds that are weak or inactive until the body transforms them into an active drug are called prodrugs , and this is the first situation that I can think of where a legal prodrug has been found for an illegal drug. (mindhacks.com)
  • In most cases, prodrugs are simple chemical derivatives that are only one or two chemical or enzymatic steps away from the active parent drug. (aspetjournals.org)
  • Numerous prodrugs designed to overcome formulation, delivery, and toxicity barriers to drug utilization have reached the market. (aspetjournals.org)
  • The rationale behind the use of prodrugs is generally to optimize the so-called "drug-like" properties [i.e., absorption, distribution, metabolism, and excretion (ADME 1 ) properties] because they can cause considerable problems in subsequent drug development, if unfavourable ( Table 1 ). (aspetjournals.org)
  • This can not only improve the efficacy of the drug but also decrease systemic and/or unwanted tissue/organ-specific toxicity (T). Development of a prodrug with improved properties may also represent a life-cycle management opportunity. (aspetjournals.org)
  • If anything, this alternative should be considered in the early stages of preclinical development, bearing in mind that prodrugs may alter the tissue distribution, efficacy, and even toxicity of the parent drug. (aspetjournals.org)
  • Despite these impressive numbers, we have only begun to appreciate the full potential of the prodrug approach in modern drug development, and many novel prodrug innovations await discovery. (aspetjournals.org)
  • Choose the menu Chemistry/Generate Drug from Prodrug and a dialog box will be displayed. (molsoft.com)
  • You can choose to output the results in the "in-addition" mode where the converted drug will be in the row below the prodrug or "replace original" whereby the prodrug will be replaced with the converted drug. (molsoft.com)
  • These results indicate that attachment of phenylalanine to a cationic drug via an amide bond from the meta-position of its aromatic ring could be highly applicable in prodrug design for LAT1-mediated CNS-delivery of not only anionic but also cationic polar drugs. (springer.com)
  • Pavan B, Dalpiaz A. Prodrugs and endogenous transporters: are they suitable tools for drug targeting into the central nervous system? (springer.com)
  • This chapter reviews the liver-targeting strategies explored to date and, more specifically, the strengths and weaknesses of various prodrug strategies used for liver-specific drug delivery. (springer.com)
  • CORALVILLE, Iowa, May 10, 2016 (GLOBE NEWSWIRE) -- KemPharm, Inc. (NASDAQ:KMPH), a clinical-stage specialty pharmaceutical company focused on the discovery and development of proprietary prodrugs, today announced that KP511, KemPharm's prodrug of hydromorphone, has been granted "Fast Track" designation by the U.S. Food and Drug Administration (FDA). (cnbc.com)
  • Colloidal drug and prodrug conjugates have unique targeting characteristics for tumor vasculature from the blood and for the lymphatics draining a tissue injection site. (epfl.ch)
  • Instead of administering a drug directly, a corresponding prodrug might be used instead to improve how a medicine is absorbed, distributed, metabolized, and excreted (ADME). (wikipedia.org)
  • Prodrugs are often designed to improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract. (wikipedia.org)
  • A prodrug may be used to improve how selectively the drug interacts with cells or processes that are not its intended target. (wikipedia.org)
  • The reasons for this type of formulation may be because the drug is more stable during manufacture and storage as the prodrug form, or because the prodrug is better absorbed by the body or has superior pharmacokinetics (e.g., lisdexamphetamine). (wikipedia.org)
  • uptake
  • Here, we attempted to enhance the brain uptake of cationic dopamine by utilizing the large amino acid transporter 1 (LAT1) at the BBB by prodrug approach. (springer.com)
  • The brain uptake after intravenous administration and the dopamine-releasing ability in the rat striatum after intraperitoneal administration were also determined for the most promising prodrug. (springer.com)
  • Brain uptake of ketoprofen-lysine prodrug in rats. (springer.com)
  • bioavailability
  • Another fallacy is that prodrugs are simply of academic interest and do not have industrial applications in attempts to overcome bioavailability and toxicity problems. (aspetjournals.org)
  • generate
  • It is expected that continued studies to optimize the bystander effects and other properties of prodrugs and the activated species they generate will contribute to improvements in the effectiveness of suicide gene therapy. (hindawi.com)
  • Select the reactions you wish to use to generate the prodrug. (molsoft.com)
  • KemPharm utilizes its LAT platform technology to generate improved prodrug versions of FDA-approved drugs in the high need areas of pain, ADHD and other CNS disorders. (cnbc.com)
  • therapeutic
  • Many therapeutic agents are manufactured and administered in prodrug forms. (mdpi.com)
  • Type IA prodrugs refer to those that are converted at the cellular targets of therapeutic actions, whereas Type IB prodrugs' conversion occurs in the primary metabolic tissues such as liver, gut, or lung. (mdpi.com)
  • As disclosed previously, we are planning to develop KP511 as an extended-release prodrug product candidate that could offer the potential to deter certain common methods of abuse while providing the same pharmacokinetic and therapeutic effect as existing hydromorphone products when taken as intended. (cnbc.com)
  • Type II prodrugs are bioactivated extracelluarly, either in the milieu of GI fluids (Type IIA), within the systemic circulation and/or other extracellular fluid compartments (Type IIB), or near therapeutic target tissues/cells (Type IIC), relying on common enzymes such as esterases and phosphatases or target directed enzymes. (wikipedia.org)
  • sulfide
  • Since the polymers carry a free terminal thiol group resulting from the ring-opening polymerization of the propylene sulfide monomer, we sought to prepare prodrug block copolymers with tioguanine linked by a reduction-sensitive disulfide bond. (epfl.ch)
  • In comparison with a poly(ethylene glycol) prodrug polymer, we show that the rate of tioguanine release can be controlled by changing the poly(propylene sulfide) block length and that the tioguanine remains bioactive with cultured cells. (epfl.ch)
  • commonly
  • Probably the most commonly used illicit prodrug is heroin, which is metabolised into morphine in the body, but both are Class A drugs in the UK so there's no legal benefit to having one rather than the other. (mindhacks.com)
  • preclinical
  • NEW HAVEN, Conn., Nov. 2, 2013 (GLOBE NEWSWIRE) -- Achillion Pharmaceuticals, Inc. (Nasdaq:ACHN) today announced a poster presentation detailing the preclinical profile of ACH-3422, a uridine-analog nucleotide prodrug being advanced for the potential treatment of chronic hepatitis C viral infection (HCV). (cnbc.com)
  • proprietary
  • KemPharm believes that this proprietary design offers the potential to restrict the release of the active hydromorphone component until the prodrug is metabolized following oral administration. (cnbc.com)
  • KemPharm is a clinical-stage specialty pharmaceutical company focused on the discovery and development of proprietary prodrugs to treat serious medical conditions through its LAT platform technology. (cnbc.com)
  • Steps
  • A Mixed-Type prodrug is one that is bioactivated at multiple sites, either in parallel or sequential steps. (wikipedia.org)
  • overcome
  • Problems of standard drugs that could potentially be overcome by the use of prodrugs include insufficient absorption when absorbed orally, limited solubility, and irritation associated with administration. (wikibooks.org)
  • metabolic
  • Esterification is useful because it is often able to render the parent steroid into a prodrug of itself with altered chemical properties such as improved metabolic stability, water solubility, and/or lipophilicity. (wikipedia.org)
  • Brain
  • The phenylalanine prodrug was taken up into the brain after intravenous injection but after intraperitoneal injection the prodrug did not elevate striatal dopamine concentrations above those achieved by corresponding L -dopa treatment. (springer.com)
  • Characteristics
  • Prodrugs can be designed to bioconvert based upon the specific characteristics of the enzymes that catalyze the reaction, specifically substrate recognition. (wikibooks.org)
  • properties
  • Both prodrugs and their activated species should have good distributive properties, so that the resulting bystander effects can maximize the effectiveness of the therapy, since gene transduction efficiencies are generally low. (hindawi.com)
  • A total of 42 prodrugs explored for use in suicide gene therapy with 12 different enzymes are discussed, particularly in terms of their physiocochemical properties. (hindawi.com)
  • The prodrug concept has been used to improve undesirable properties of drugs since the late 19th century, although it was only at the end of the 1950s that the actual term prodrug was introduced for the first time. (aspetjournals.org)
  • Although the development of a prodrug can be very challenging, the prodrug approach represents a feasible way to improve the erratic properties of investigational drugs or drugs already on the market. (aspetjournals.org)
  • Although prodrug design is very challenging, it can still be more feasible and faster than searching for an entirely new therapeutically active agent with suitable ADMET properties. (aspetjournals.org)
  • Diazeniumdiolate-based aspirin prodrugs have previously been shown to retain the anti-inflammatory properties of aspirin while protecting against the common side effect of stomach ulceration. (sigmaaldrich.com)
  • Note 2: Prodrugs can thus be viewed as drugs containing specialized nontoxic protective groups used in a transient manner to alter or to eliminate undesirable properties in the parent molecule. (wikipedia.org)
  • drugs
  • Prodrugs are useful in that they can be used to avoid negative physiological effects associated with the absorption of standard drugs. (wikibooks.org)
  • The bioconversion of the prodrugs to their active parent drugs is by way of enzyme activity of hydrolases. (wikibooks.org)
  • In fact, approximately 20% of all small molecular drugs approved during the period 2000 to 2008 were prodrugs. (aspetjournals.org)
  • In addition, the prodrug strategy has been used to increase the selectivity of drugs for their intended target. (aspetjournals.org)
  • forms
  • Many of the early antimetabolite-based prodrugs provide very polar activated forms that have limited abilities to diffuse across cell membranes, and rely on gap junctions between cells for their bystander effects. (hindawi.com)
  • parent
  • Initial analysis of two new prodrugs of aspirin that also release either nitroxyl (HNO) or nitric oxide (NO) demonstrated increased cytotoxicity toward human lung carcinoma cells compared to either aspirin or the parent nitrogen oxide donor. (sigmaaldrich.com)
  • Both prodrugs reduced growth of breast adenocarcinoma cells more effectively than the parent compounds while not being appreciably cytotoxic in a related nontumorigenic cell line (MCF-10A). (sigmaaldrich.com)
  • found
  • Prodrugs 3 - 5 were found to display a potent positive inotropic effect on the myocardium, without the risk of arrhythmia. (mdpi.com)