What are Bioreductive drugs?

What are Bioreductive drugs?

Bioreductive drugs are inactive prodrugs that are converted into potent cytotoxins under conditions of either low oxygen tension or in the presence of high levels of specific reductases.

What are the uses of prodrug?

Prodrugs can be used to improve drug delivery or pharmacokinetics, to decrease toxicity, or to target the drug to specific cells or tissues. Ester and phosphate hydrolysis are widely used in prodrug design because of their simplicity, but such approaches are relatively ineffective for targeting drugs to specific sites.

How do hypoxia activated prodrugs work?

Hypoxia-activated prodrugs (HAPs), also referred to as bioreductive drugs, are compounds that can be selectively reduced by specific reductases under hypoxic conditions to form cytotoxic agents that precisely target hypoxic tumor cells and have little toxicity to normal tissue.

Is paracetamol a prodrug?

Thus, paracetamol acts as a pro-drug, the active one being a cannabinoid. These findings finally explain the mechanism of action of paracetamol and the peculiarity of its effects, including the behavioral ones.

Is captopril a prodrug?

Captopril, one of the few ACE inhibitors that is not a prodrug, competes with ATI for binding to ACE and inhibits and enzymatic proteolysis of ATI to ATII. Decreasing ATII levels in the body decreases blood pressure by inhibiting the pressor effects of ATII as described in the Pharmacology section above.

Is omeprazole a prodrug?

Omeprazole is a prodrug which is converted to its active form only at the site of action, namely the parietal cell. There it binds irreversibly with H+-K+-ATPase (the gastric proton pump), which causes an effective and long-lasting inhibition of gastric acid secretion.

Is ibuprofen a prodrug?

The prodrug is synthesized with paracetamol esters (Fig. ​34) of some NSAIDs (aspirin, ibuprofen, naproxen, diclofenac, flufenamic acid and indomethacin) and evaluated for gastric toxicity [27]. The synthesized prodrugs had a better therapeutic index than the parent drugs [28].

Is enalapril a prodrug?

1 Enalapril maleate is a prodrug which when administered orally is hydrolysed to release the active converting enzyme inhibitor enalaprilat. Enalapril maleate is 60% absorbed and 40% bioavailable as enalaprilat.

Is ramipril a prodrug?

Ramipril is a prodrug that undergoes de-esterification in the liver to form ramiprilat, its active metabolite. Ramipril rapidly distributes to all tissues, with the liver, kidneys and lungs showing markedly higher concentrations of the drug than the blood.

Is pantoprazole a prodrug?

Pantoprazole is an acid-activated prodrug, as protonation is required to form the active compound, which is capable of reacting with free SH groups on the ATPase enzyme.

Is lansoprazole a prodrug?

As a PPI, lansoprazole is a prodrug and requires protonation via an acidic environment to become activated.

Is rabeprazole a prodrug?

Rabeprazole is a prodrug and is converted to the active form in the acidic secretory canaliculi of parietal cells. Because the inhibition is irreversible, acid secretion is suppressed for 24 to 48 hours, until new proton pump molecules have been synthesized and transported to the cell membrane.

Is esomeprazole a prodrug?

Esomeprazole is the S-enantiomer of [Chemical:omeprazole] [Article:11985491]. Esomeprazole is a prodrug that is activated by the acid environment in the stomach to an acid or sulfonamide form [Article:18679668]. Esomeprazole is metabolized primarily by CYP2C19 and CYP3A4 [Article:16338278].