Factbites
 Where results make sense
About us   |   Why use us?   |   Reviews   |   PR   |   Contact us  

Topic: Prodrug


Related Topics

In the News (Wed 2 Dec 09)

  
  Prodrug - definition from Biology-Online.org
A compound that is converted within the body into its active form that has medical effects.
prodrugs useful when the active drug may be too toxic to administer ter systemically, the active drug is absorbed poorly by the digestive tract, or the body breaks down the active drug before it reaches its target.
This page was last modified 06:56, 22 August 2006.
www.biology-online.org /dictionary/Prodrug   (129 words)

  
  Targeted Prodrug Design to Optimize Drug Delivery
In the prodrug approach, site-specific drug delivery can be obtained from tissue-specific activation of a prodrug, which is the result of metabolism by an enzyme that is either unique for the tissue or present at a higher concentration (compared with other tissues); thus, it activates the prodrug more efficiently.
Of these glycosidic prodrugs, the dexamethasone glucoside appeared to be the better candidate, with nearly 60% of the orally administered prodrugs reaching the caecum as a free steroid, while orally administered parent steroids were absorbed almost exclusively from the small intestine.
Carrier-mediated intestinal absorption of valacyclovir, the L-valyl ester prodrug of acyclovir: 1.
www.aapsj.org /view.asp?art=ps020106   (4711 words)

  
  S R Roffler Lab - prodrug abstracts
BHAMG, the glucuronide prodrug of p-hydroxyaniline mustard (pHAM), was relatively nontoxic in vivo.
These prodrugs were characterized in vitro for their usefulness in ADEPT and were compared with the previously described prodrugs epirubicin-glucuronide and doxorubicin-nitrophenyl-glucuronide.
The ability of the potential prodrugs to act as substrates for CPG2 was determined (kinetic parameters KM and kcat), and the chemical stability was measured for all the compounds.
www.ibms.sinica.edu.tw /~sroff/prodrug_abstracts.html   (11161 words)

  
 BioMed Central | Full text | Synthesis and preliminary cytotoxicity study of a cephalosporin-CC-1065 analogue prodrug
Due to the slow non-enzymatic degradation of the cephalosporins in solution [39], the ratio of toxicity of cephalosporin-containing prodrugs to their corresponding free drugs is generally not very high.
For example, a cephalosporin-doxorubicin prodrug was 9-fold less toxic than free doxrubicin against tumor cells in vitro, but caused tumor regression when tested in tumor xenograft models [40].
A cephalosporin-vinca alkaloid prodrug was 5-fold less toxic than the free drug against tumor cells in vitro, but was highly effective in tumor xenograft models in vivo [41].
www.biomedcentral.com /1472-6769/1/4   (2551 words)

  
 INSIDE AAPS: Focus Groups - Prodrug Focus Group
Prodrug strategies have traditionally been used to address ADMET liabilities of marketed compounds or as tools in late-stage problem solving for drug development candidates.
The goals of the Prodrug Focus Group are to expand drug delivery knowledge of prodrug possibilities through education, impact the direction of prodrug research through long-range programming, encourage interdisciplinary collaborations in prodrug research, encourage innovative use of new technologies to solve prodrug problems, and provide a common prodrug forum for universities, industry, and government.
Prodrugs will be used more often and sooner as a means of overcoming the physical/chemical liabilities of active therapeutic agents so that more innovative therapies will reach the market place.
www.aapspharmaceutica.com /inside/focus_groups/Prodrug/index.asp   (482 words)

  
 Targeted Prodrug Design to Optimize Drug Delivery
In the prodrug approach, site-specific drug delivery can be obtained from tissue-specific activation of a prodrug, which is the result of metabolism by an enzyme that is either unique for the tissue or present at a higher concentration (compared with other tissues); thus, it activates the prodrug more efficiently.
Of these glycosidic prodrugs, the dexamethasone glucoside appeared to be the better candidate, with nearly 60% of the orally administered prodrugs reaching the caecum as a free steroid, while orally administered parent steroids were absorbed almost exclusively from the small intestine.
Carrier-mediated intestinal absorption of valacyclovir, the L-valyl ester prodrug of acyclovir: 1.
www.aapspharmsci.org /view.asp?art=ps020106   (4711 words)

  
 Johns Hopkins studies prodrug chemotherapy - U.S. cancer scientists say prodrug chemotherapy is a new str...
Johns Hopkins studies prodrug chemotherapy - U.S. cancer scientists say prodrug chemotherapy is a new str...
If the prodrug is injected before the enzyme clears from normal tissue, it could produce an array of side effects, the researchers said.
The scientists describe the synthesis and early laboratory testing of the first prodrug-activating enzyme that can be imaged in tissue to time administration of the prodrug in the Nov. 29 issue of the Journal of the American Chemical Society.
www.politicalgateway.com /news/read/48712   (205 words)

  
 Chemical Stabilization of a ?9-Tetrahydrocannabinol Prodrug in Polymeric Matrix Systems Produced by a Hot-melt Method: ...
It was found that 8.4% of the prodrug degraded during the process of incorporation using the hot-melt method.
This hydrolytic reaction may be owing to the presence of moisture in the matrices or possible interaction of the ether and hydroxyl groups of PEO (and/or other additives) with the drug molecules via hydrogen bonds, thereby causing hydrolysis of the ester.
Stability of the ester prodrug could therefore be optimized in the solid-state by altering the formulation ingredients and by the use of an appropriate agent that adjusts the microenvironmental pH of the product close to the pH of maximum stability.
www.aapspharmscitech.org /view.asp?art=pt070371   (6208 words)

  
 Prodrug-activating systems in suicide gene therapy -- Springer and Niculescu-Duvaz 105 (9): 1161 -- Journal of Clinical ...
Subsequently, a prodrug is administered that is converted to the active drug by the foreign enzyme expressed inside or on the surface of tumor cells.
The doxorubicin prodrug (1) is cleaved by carboxypeptidase G2 (CPG2), releasing the glutamic acid (3) and an unstable intermediate (2).
(21) or alter the lipophilicity of the prodrug (22).
www.jci.org /cgi/content/full/105/9/1161   (4603 words)

  
 Prodrug definition - Medical Dictionary definitions of popular medical terms easily defined on MedTerms
Prodrug definition - Medical Dictionary definitions of popular medical terms easily defined on MedTerms
A prodrug must undergo chemical conversion by metabolic processes before becoming an active pharmacological agent.
It is not active in its ingested form.
www.medterms.com /script/main/art.asp?articlekey=23992   (157 words)

Try your search on: Qwika (all wikis)

Factbites
  About us   |   Why use us?   |   Reviews   |   Press   |   Contact us  
Copyright © 2005-2007 www.factbites.com Usage implies agreement with terms.