Phosphate ester prodrug
WebApr 27, 2024 · Fospropofol (Lusedra) is a phosphonooxymethyl prodrug of the sedative or hypnotic drug propofol in which the phosphate promoiety is linked to the sterically … Webprodrug activation processes. Ester prodrugs to enhance oral absorption Oral absorption is a key component of oral bioavailability. Kevin Beaumont (Pfizer Ltd, UK) discussed issues …
Phosphate ester prodrug
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WebJul 31, 2007 · An increasing number of phosphate esters of pharmaceutical interest (mainly antiviral agents and signaling regulators) has encouraged the advancement of the … WebOseltamivir phosphate is an ethyl ester prodrug requiring ester hydrolysis for conversion to the active form, oseltamivir carboxylate. ... In 2-year carcinogenicity studies in mice and rats given daily oral doses of the prodrug oseltamivir phosphate up to 400 mg/kg and 500 mg/kg, respectively, the prodrug and the active form oseltamivir ...
WebDec 13, 2024 · Aquavan® is a phosphate ester prodrug of the analgesic drug propofol (Banaszczyk et al., 2002) that employs a phosphonooxymethyl spacer approach that has been successfully employed for fosphenytoin … WebMar 3, 2024 · Cyclic phosphate ester derivative 18c exhibits much higher anti-proliferative activity than positive control NUC-1031 with IC 50 s of 3.6–19.2 nM on multiple cancer …
WebOnce the prodrug gets into the systemic circulation or target tissues, the ester prodrug moiety may be cleaved through an enzymatic and/or chemical process to release the corresponding free acid of phosphinate, phosphonate, or phosphate to achieve the desirable biological effect. WebAug 21, 2014 · 3′,5′-Cyclic phosphate ester prodrugs (Figure 26) are part of an interesting prodrug concept that led to the discovery of PSI-352938, a compound that demonstrated anti-HCV efficacy in vitro and in human phase 1 trials. The activation of these derivatives to the monophosphate involves, first, an enzymatic P–O-dealkylation by CYP3A4 and ...
Weborganophosphate. [ or″gah-no-fos´fāt] an organic ester of a phosphate such as phosphoric acid with an organic compound such as glucose or sorbitol; see also organophosphorus. …
WebFosphenytoin is a phosphate ester prodrug developed as an alternative to intravenous phenytoin for acute treatment of seizures. Advantages include more convenient and rapid intravenous administration, availability for intramuscular injection, and low potential for adverse local reactions at injectio … dyson ball operating manualWebAug 28, 2008 · Preformulation studies were performed on a hemiglutarate ester prodrug of Δ 9-tetrahydrocannabinol (THC-HG), to facilitate the development of stable formulations by hot-melt methods.The various studies performed included solid-state thermal characterization, pKa, logP, aqueous and pH dependent solubility, pH stability and effect … dyson ball multi floor origin blueWebMay 1, 2001 · Fosphenytoin is a phosphate ester prodrug of phenytoin with an improved solubility and better tolerance after intramuscular or intravenous administration. It is rapidly hydrolyzed in vivo to phenytoin with a half-life of 5–15 min. The prodrug is not pharmacologically active, but it has been shown to cross-react in various immunoassays … dyson ball multifloor uprightWebMay 20, 2024 · ANP prodrugs with suitable pharmacokinetics include amino acid phosphoramidates, pivaloyloxymethyl (POM) and isopropoxycarbonyloxymethyl (POC) esters, alkyl and alkoxyalkyl esters, … csc of gilroy caWebMar 20, 2003 · This approach is particularly valuable in the case of biologically active phosphates because of the high intrinsic hydrophilicity and the multitude of biological … dyson ball multi floor vacuum cleanersWebBy the design of phosphate ester prodrugs, the poor aqueous solubility of various drugs such as estramustine and prednisolone could be addressed. When given orally these prodrugs rapidly dissolve in gastrointestinal (GI) fluids, yet being efficiently absorbed from the intestinal mucosa. Their high membrane permeability is ascribed to the ... dyson ball no suctionWebPhosphate prodrugs of amines are made to increase solubility, owing to the presence of the highly ionized species in the GI tract. ... Prodrugs are ester derivatives synthesized using the alcoholic functional group at the C-2 or the C-7 position of paclitaxel [70,71]. Such prodrugs have produced cytotoxic activity comparable to paclitaxel ... dyson ball multi floor reviews