• Following a drug repurposing approach, we aimed to investigate and compare the antibacterial and antibiofilm activities of different classes of phosphate prodrugs (HepDirect, cycloSal, SATE and mix SATE) of antiviral and anticancer FDA-approved nucleoside drugs [zidovudine (AZT), floxouridine (FUDR) and gemcitabine (GEM)] against a variety of pathogenic Gram-positive and -negative bacteria. (nih.gov)
  • Due to the selective breaking of the azo link by azoreductases discharged by the gut microbiota, azo prodrugs of 5-Amino Salicylic Acid (5-ASA), 4-ASA, anticancer drugs, and novel leads useful in colonic illnesses have been examined in this work for colon directed drug delivery. (digiwire.co.in)
  • In a new report now published on Science Advances , Gongyuan Liu and a team of scientists in chemistry, biomedical engineering and bioengineering at the City University of Hong Kong in China presented cyaninplatin as a Platinum (IV) anticancer prodrug. (worldmedicinefoundation.com)
  • Photoactivatable platinum (IV) prodrugs are therapeutically advantageous since they originate from platinum anticancer prodrugs for high stability and easy functionalization. (worldmedicinefoundation.com)
  • Development of 5-fluorouracil-dichloroacetate mutual prodrugs as anticancer agents. (bvsalud.org)
  • Conclusion: A dibasic, self-activating prodrug (Compound 24) has been created which displays a much-increased lung tissue retention relative to the parent drug (Compound 1). (nottingham.ac.uk)
  • A prodrug is a pharmacologically inactive medication or compound that, after intake, 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)
  • Our study suggests that compound WRQ-2 is a potential gemcitabine prodrug and worth of further antitumor activity investigation. (go.jp)
  • A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug. (wakehealth.edu)
  • In this thesis, two amide prodrugs have been synthesized of the anti-infective agent Ciprofloxacin, and their potential advantages in fighting bacteria over the respective parent compound have been demonstrated. (alquds.edu)
  • After a pharmacokinetics assessment of a drug and its metabolite or a prodrug and its parent-drug, several parameters can be calculated. (eurekaselect.com)
  • Beclomethasone dipropionate is a prodrug where the major metabolite is beclomethasone-17-monopropionate (B17MP). (janusinfo.se)
  • The amino acid ester derivatives of 6-deoxypenciclovir, 11-20, were synthesized as potential prodrugs of penciclovir, and were evaluated for their oral penciclovir bioavailability in mice and rats. (ewha.ac.kr)
  • Aspirin, acetylsalicylic acid, first made by Felix Hoffmann at Bayer in 1897, is a synthetic prodrug of salicylic acid. (wikipedia.org)
  • The phosphate component itself was modified to a phosphoramidate, forming a ProTide (Prodrug NucleoTide). (uwo.ca)
  • Ten prodrugs were synthesized and screened for antibacterial activity against seven Gram-negative and two Gram-positive isolates fully susceptible to traditional antibiotics, alongside six Gram-negative and five Gram-positive isolates with resistance mechanisms. (nih.gov)
  • The prodrugs showed decreased antibacterial activity compared with the parent nucleosides. (nih.gov)
  • 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)
  • Prodrugs have better delivery properties that surpass the parent drug molecule [ 1 ]. (ijpsonline.com)
  • Prodrugs are derivatives of drug molecules that are pharmacologically inactive but require either chemical or enzymatic transformation to release the active drug in vivo in order to exert a pharmacological effect. (ijpsonline.com)
  • We have prepared derivatives of erythromycin B as putative paediatric prodrugs, taking advantage of the much improved acid stability of erythromycin B relative to erythromycin A. Thus, erythromycin B enol ether ethyl succinate is very poorly soluble in water, and its hydrolysis is undetectable in conditions resembling the medicine bottle. (nih.gov)
  • These prodrugs subsequently undergo enzymatic or non-enzymatic cleavage to release the active drug moiety (figure 1) [ 12 , 13 ]. (ijpsonline.com)
  • Chapter 4: Investigates how the dibasic moiety of the prodrug design affects the distribution of the prodrug in lung tissue. (nottingham.ac.uk)
  • By taking a lysosome-targeting fluorescent probe, replacing the functionality responsible for its lysosome targeting nature with the dibasic prodrug moiety, a distribution comparison can be created. (nottingham.ac.uk)
  • This chapter attempted to visualise the effect of incorporating a dibasic moiety into the prodrug design on the distribution and organelle sequestration. (nottingham.ac.uk)
  • Different strategies to target hypoxic cancer cells and/or HIFs include hypoxia-activated prodrugs and inhibition of HIF dimerization, mRNA or protein expression, DNA binding capacity, and transcriptional activity. (lu.se)
  • Tegafur, a prodrug of 5-fluorouracil (5-FU), is an oral fluorouracil antitumor drug used for the management of adenocarcinomas. (cun.es)
  • For example, a systemically administered prodrug could remain inactive until it reaches the TME, where it becomes activated and launches a powerful antitumor response. (genengnews.com)
  • Ciclopirox Prodrug has demonstrated anti-tumor activity in preclinical models of non-muscle invasive and muscle-invasive bladder cancer. (kucancercenter.org)
  • Now, a team of researchers at Kyoto University has developed a prodrug form of curcumin, TBP1901 , that has shown anti-tumor effects without toxicities. (polyphenols-site.com)
  • The investigators used "prodrug" vinblastine-N-oxide, known in a low oxygen environments within the body, such as those within solid tumors, to turn into vinblastine. (medgadget.com)
  • Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug 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)
  • Prodrugs can be classified into two major types, based on how the body converts the prodrug into the final active drug form: Type I prodrugs are bioactivated inside the cells (intracellularly). (wikipedia.org)
  • The prodrug approach using various carriers has evolved as a significant tool in surmounting different obstacles in relation to drug formulation and targeting. (ijpsonline.com)
  • Prodrug concept is justified because it enables the active drug to overcome the barrier that would impede it from reaching the site of action to exert the required pharmacological activity. (ijpsonline.com)
  • Prodrugs are a type of drug that are administered in an inactive form and are activated by body enzyme which is a common method in medicinal chemistry to aid in improving potency. (uwo.ca)
  • Chapter 2: Describes the use of prodrug systems as mechanisms for improving drug delivery. (nottingham.ac.uk)
  • The subsequent in-vivo pharmacokinetic studies demonstrate that when inhaled independently, over 99% of the active drug was eliminated from the lung tissue within 3 hours, but when delivered as a prodrug, sustained prodrug activation meant that the drug was present in the lung at a pharmaceutically relevant concentration for over 24 hours, with no detected exposure of the drug to blood plasma. (nottingham.ac.uk)
  • Included is the design and attempted synthesis of a series of prodrugs, which based on the results of chapter 1, would be interesting candidates for an in-vivo PK study to determine their duration of action relative to the parent drug candidates, and thus feasibility as sustained release delivery agents. (nottingham.ac.uk)
  • The anti-cancer drug, called Ciclopirox Prodrug, or CPX-POM, was discovered at The University of Kansas Cancer Center. (kucancercenter.org)
  • Reduction of the prodrug loperamide oxide to its active drug loperamide in the gut of rats, dogs, and humans. (aspetjournals.org)
  • The in vitro susceptibility for both prodrugs was determined against Escherichia coli, staphylococcus aureus, and pseudomonas, and compared to that of the parent drug Ciprofloxacin, using disc diffusion method, and broth diffusion method. (alquds.edu)
  • The prodrug overcame drug resistance as a result of combinatorial therapy mechanisms, which included the release of platinum chemotherapeutics, the breakdown of intracellular reductants, and a large release of reactive oxygen species. (worldmedicinefoundation.com)
  • The molecular prodrugs augmented therapeutic behavior of the original drug moieties to accomplish personalized, location-specific treatment with reduced side-effects. (worldmedicinefoundation.com)
  • Bempedoic acid , the drug we studied, is a prodrug. (medscape.com)
  • Type II prodrugs are bioactivated extracellularly, 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)
  • Liu and colleagues used energy-conversion chemistry to activate the prodrugs by using exogeneous stimuli to realize therapeutic courses. (worldmedicinefoundation.com)
  • The prodrug additionally functioned as a multi-imaging contrast agent to accomplish high-resolution ultrasound imaging, near-infrared optical imaging and photoacoustic computed tomography prior to therapeutic intervention. (worldmedicinefoundation.com)
  • Examples of Type II prodrugs are salicin (described above) and certain antibody-, gene- or virus-directed enzyme prodrugs used in chemotherapy or immunotherapy. (wikipedia.org)
  • A unique approach to circumvent solubility issues involves coadministration of a hydrophilic prodrug with an exogenous converting enzyme. (healthpartners.com)
  • We describe a prodrug concept in which the target enzyme MMP12 produces its own inhibitor in a two-step activation procedure. (elsevierpure.com)
  • If applied in vivo in the future, these prodrugs might release the active entity in a highly specific manner only at such sites where enzyme activity resides. (elsevierpure.com)
  • The prodrug strategy implementation in the last 20 y has led to a steady advancement in the biopharmaceutical, physicochemical and/or pharmacokinetic attributes of the pharmacologically active compounds. (ijpsonline.com)
  • The orally-administered prodrug of cidofovir, CMX001, and a series of other compounds are currently being investigated. (who.int)
  • cycloSal-GEM-monophosphate (MP) prodrugs 20a and 20b were the most active agents against Gram-positive bacteria (Enterococcus faecalis and Staphylococcus aureus) and retained their activity against antibiotic-resistant isolates. (nih.gov)
  • Synergistic effects of co-administration of suicide gene expressing mesenchymal stem cells and prodrug-encapsulated liposome on aggressive lung melanoma metastases in mice. (stembook.org)
  • Of the prodrugs tested in mice and rats, 6-deoxypenciclovir O-l-valinate (13), O-l-isoleucinate (15), and O,O-di-glycinate (16) showed significantly higher urinary recovery of penciclovir compared with that of penciclovir, but those are somewhat lower than that of famciclovir. (ewha.ac.kr)
  • Type IB agents rely on metabolic enzymes, especially in hepatic cells, to bioactivate the prodrugs intracellularly to active drugs. (wikipedia.org)
  • The result was that the prodrug was much better at penetrating tumors and being activated to kill nearby cells than when injected without liposome shells. (medgadget.com)
  • The company's prodrugs are called Indukine molecules, and they are designed to unleash pro-inflammatory mechanisms on tumors while preventing unwanted side effects on nontarget tissue. (genengnews.com)
  • Approximately 10% of all marketed drugs worldwide can be considered prodrugs. (wikipedia.org)
  • The prodrug approach is rapidly becoming a crucial part in the stratagem of delivery of drugs. (ijpsonline.com)
  • Around 10 % of marketed medicines can be categorized as prodrugs currently, and also that during 2008, 33 % of approved small molecular weight drugs were prodrugs [ 5 - 7 ]. (ijpsonline.com)
  • Carrier-linked prodrugs are for drugs with major drawbacks, which are linked to a nontoxic carrier or promoiety through covalent linkage to change or get rid of their undesirable physicochemical properties. (ijpsonline.com)
  • We refer to these bioconjugates as two-step activation prodrugs since two reactions are finally required to liberate the actual organic drugs. (uzh.ch)
  • Florida-based KemPharm uses its ligand activated therapy technology to develop proprietary prodrugs, improved versions of approved and commonly prescribed drugs. (streetwisereports.com)
  • The imidazotetrazine ring is an acid-stable precursor and prodrug of highly reactive alkyl diazonium ions. (hud.ac.uk)
  • One of the company's IL-2 Indukine molecules, the WTX-124 prodrug, has shown promise in preclinical studies. (genengnews.com)
  • This trial represents an important first step in our strategy to evaluate the combined activity of Ciclopirox Prodrug and standard-of-care surgical, chemotherapy and immunotherapy treatments in bladder cancer patients," said Tammy Ham, president and chief executive officer of CicloMed LLC. (kucancercenter.org)
  • An attractive cancer immunotherapy approach is the prodrug. (genengnews.com)
  • All the prodrugs showed a good stability both in pH 7.4 phosphate buffer and in pH 2.0 buffer, and they were readily hydrolyzed by rat plasma. (unict.it)
  • Among the different prodrug approaches, the cycloSal prodrugs appeared the most effective. (nih.gov)
  • The researchers loaded this prodrug into liposomes, vesicles made of lipids, and delivered it into animals with non-small cell lung cancer. (medgadget.com)
  • Chapter 3: Develops further the prodrug system introduced in chapter 1, this time focusing on an intracellular PI3K δ target. (nottingham.ac.uk)
  • Werewolf Therapeutics develops tumor-activated immunotherapeutic prodrugs. (genengnews.com)
  • Type IA prodrugs include many antimicrobial and chemotherapy agents (e.g., 5-flurouracil). (wikipedia.org)
  • Most of the prodrugs tested displayed very potent preventive antibiofilm specific activity, but not curative. (nih.gov)
  • In particular, cycloSal (17a) and mix SATE (26) AZT prodrugs combine the lowest cytotoxicity with high and broad antibacterial and antibiofilm activity against Gram-negative bacteria. (nih.gov)
  • In the mouse acetic acid induced writhing assay, the prodrugs exhibited, following acute administration, a good analgesic activity. (unict.it)
  • In all cases, new mutual prodrugs showed a higher cytotoxic activity toward cancer models and lower to normal cell models than the parent 5-FU itself. (bvsalud.org)
  • The final products of the produced prodrugs were obtained as powders and in high yields. (alquds.edu)
  • Seven prodrugs were approved in 2015 and six in 2017. (wikipedia.org)
  • One of the most useful strategies for delivering medications to the colon via the oral route is the prodrug strategy. (digiwire.co.in)
  • All three prodrugs are soluble and stable in water. (uzh.ch)
  • A Mixed-Type prodrug is one that is bioactivated at multiple sites, either in parallel or sequential steps. (wikipedia.org)
  • The remaining 70% is KemPharm's prodrug, serdexmethylphenidate, which extends relief for about 13 hours. (streetwisereports.com)
  • By avoiding "cytokine sink" and peripheral toxicity, our SmartKine® platform significantly extends the pharmacokinetics of cytokines, powering next-generation prodrugs with improved safety profiles. (ask-gene.com)
  • We are led by a team of pioneering scientists focused on a shared goal: to make AskGene Pharma the global leader in cytokine prodrugs, providing safer and better medicines for saving patients' lives. (ask-gene.com)
  • The objective of this review is to provide the researchers with a compilation of which carriers would be suitable for prodrug synthesis and what would be their benefits. (ijpsonline.com)
  • Properties and selection of carriers or promoeities is a very important parameter in successful prodrug design. (ijpsonline.com)
  • The high conversion rate of curcumin prodrug TBP1901 to curcumin in bone marrow warrants its clinical application for diseases growing in the marrow like multiple myeloma and leukemia. (polyphenols-site.com)