Remdesivir is an adenosine nucleotide prodrug that is metabolized intracellularly to nucleoside triphosphate metabolite (active). (firstline.org)
Ribahep ( Ribavirin) is readily phosphorylated intracellularly by adenosine kinase to Ribahep ( Ribavirin) mono-, di-, and triphosphate metabolites. (heethealthcare.net)
Inhibits3
It is converted intracellularly to the diphosphate, which inhibits the synthesis of hepatitis B virus DNA through competition for the enzyme reverse transcriptase and incorporation into the viral DNA. (abcmedicalnotes.com)
PCSK9 inhibits the reuse of LDL receptors in the liver by breaking them down intracellularly. (lipidtools.com)
Phosphorylated intracellularly where it inhibits HIV reverse transcriptase, resulting in inhibition of viral replication. (unboundmedicine.com)
Phosphate2
It is activated intracellularly by deoxycytidine kinase (dCK), which adds a phosphate group to the 5' position of the deoxyribose group. (biomedcentral.com)
PF-07321332 is also a covalent inhibitor , but its warhead is a phosphate prodrug , a hydroxyketone . (precisionvaccinations.com)
Liver1
These studies show that benzil and a dimethylbenzil analogue efficiently enter cells and inhibit human intestinal carboxylesterase and rabbit liver carboxylesterase intracellularly. (inra.fr)
Inhibition1
This inhibition results in reduced cytotoxicity to CPT-11 due to the lack of carboxylesterase-mediated conversion of the prodrug to SN-38. (inra.fr)
Active2
Unionized metronidazole is selective for anaerobic bacteria due to their ability to intracellularly reduce metronidazole to its active form. (pharmfair.com)
Metabolism and elimination - MTX is a prodrug that becomes active only when polyglutamated within cells. (medilib.ir)
Lack1
Some cancer cells are resistant to MTX because they lack adequate mechanisms for transporting the drug intracellularly. (medquizzes.net)
Nucleoside5
Nucleoside and nucleotide analogs are prodrugs that must be metabolized intracellularly to exert their activity. (medscape.com)
Molnupiravir is a type II prodrug of synthetic nucleoside derivative N⁴- hydroxycytidine. (zopiclonebuy.com)
As an adenosine nucleotide prodrug, remdesivir is metabolized to an active nucleoside triphosphate metabolite, after being distributed into cells. (unboundmedicine.com)
Tenofovir alafenamide (TAF) is a prodrug of the active metabolite tenofovir, which belongs to the drug group of nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs). (npra.gov.my)
An alkoxyalkyl ester prodrug containing the synthetic, acyclic nucleoside monophosphate analog cidofovir linked, through its phosphonate group, to a lipid, 3-hexadecyloxy-1-propanol, with antiviral activity against double-stranded DNA viruses. (blogspot.com)
Anticancer prodrugs2
The obtained results provide useful chemical information about the photoreaction between photoactivatable Pt(IV) anticancer prodrugs and human telomeric DNA. (bvsalud.org)
2. Carbon nanotubes based electrochemical biosensor for detection of formaldehyde released from a cancer cell line treated with formaldehyde-releasing anticancer prodrugs. (nih.gov)
Depletion1
3. Formaldehyde-releasing prodrugs specifically affect cancer cells by depletion of intracellular glutathione and augmentation of reactive oxygen species. (nih.gov)
Selective2
A prodrug improves the selective interaction of a drug with the cells and tissues of gastrointestinal system. (zopiclonebuy.com)
Unionized metronidazole is selective for anaerobic bacteria due to their ability to intracellularly reduce metronidazole to its active form. (illumina.com)
Inactive4
Prodrugs, the pharmacologically inactive derivatives of active drugs, are designed to maximize the amount of active drug that reaches its site of action, through manipulation of the physicochemical, biopharmaceutical or pharmacokinetic properties of the drug. (ijcrr.com)
They described prodrugs as pharmacologically inactive chemical derivatives that could be used to alter the physicochemical properties of drugs, in a temporary manner, to increase their usefulness and/or to decrease associated toxicity2 .Subsequently such drug-derivatives have also been called „latentiated drugs? (ijcrr.com)
Carrier linked prodrug Contain a group that can be easily removed enzymatically (such as ester) to reveal the true drugs as shown in fig.1.Ideally the group removed is pharmacologically inactive and nontoxic while the connecting bond must be labile for efficient activation in vivo. (ijcrr.com)
Dexedrine is purely the right handed enantiomer of amphetamine, while Vyvanse is the right handed enantiomer with lysine attached, thus making it an inactive prodrug. (medicalvs.com)
Triphosphate1
Remdesivir is a prodrug that is metabolized intracellularly to the active metabolite, remdesivir triphosphate. (unboundmedicine.com)
Bioavailability1
Before understanding about a prodrug, it is important to understand about bioavailability of a drug. (zopiclonebuy.com)
Derivative1
Thus, prodrug can be defined as a drug derivative that undergoes biotransformation enzymatically or nonenzymatically, inside the body before exhibiting its therapeutic effect. (ijcrr.com)
Compound1
In medical terms, a prodrug is a medication or compound that after administration is converted by the body or metabolized into a pharmacologically active drug. (zopiclonebuy.com)
Mechanism1
Such special damages of Pt(IV) prodrugs on human telomeric DNA implicate its active role in the mechanism of Pt(IV) prodrugs and further support the unique sequence-dependent photointeraction profile of complex 1 reacting with DNA. (bvsalud.org)
Overcome1
13. Formaldehyde-releasing prodrugs in combination with adriamycin can overcome cellular drug resistance. (nih.gov)
Treatment3
Molnupiravir was subsequently converted for modification purposes and developed into a prodrug for treatment of Encephalitis in 2013 before its reuse in 2021. (zopiclonebuy.com)
The development of prodrugs promises to be very effective method for treatment of diseases in future. (ijcrr.com)
Tenofovir disoproxil fumarate (TDF), the older tenofovir prodrug that is widely used for the treatment of HIV infection and hepatitis B infections, was first internationally approved for use in 2001 3-4 . (npra.gov.my)
Activity4
Ideal properties of prodrug It should have intrinsic pharmacological activity that means it should not change receptor configuration that is necessary for pharmacological response. (ijcrr.com)
1. The role of intracellularly released formaldehyde and butyric acid in the anticancer activity of acyloxyalkyl esters. (nih.gov)
5. Novel prodrugs of tegafur that display improved anticancer activity and antiangiogenic properties. (nih.gov)
A benzyl styryl sulfone analog, and a disodium phosphate ester prodrug of ON 013100, with potential antineoplastic activity. (blogspot.com)
Review1
In this mini review, prodrugs are discussed with a focus on the viability of the prodrug approach as a means of attaining targeted drug delivery. (ijcrr.com)
Form1
5-Aminolevulinic acid is a prodrug that enters the heme biosynthetic pathway and is metabolized intracellularly to form the photosensitizing molecule protoporphyrin IX (PpIX). (medscape.com)
Drug2
prodrugs, targeting, targeted drug delivery. (ijcrr.com)
Limitation of prodrug 7 The problem associated with prodrug design is its toxicity which is due to Formation of unexpected metabolite from the total drug conjugates. (ijcrr.com)