PURPOSE The success of enzyme/prodrug cancer therapy is limited by the uncertainty in the delivery of the enzyme in vivo. This study shows the use of noninvasive magnetic resonance (MR) and optical imaging to image the delivery of a prodrug enzyme. With this capability, prodrug administration can be timed so that the enzyme concentration is high in the tumor and low in systemic circulation and ...

Valnemulin, successfully developed by Sandoz in 1984, is a new generation derivative of pleuromutilin related to tiamulin. Valnemulin has low water-solubility, a short half-life period, low bioavailability, and instability. The application of valnemulin was restricted. Therefore, finding a more moderate delivery system is necessary to improve the shortcomings of valnemulin. The purpose of the s...

The N-ethoxycarbonylmorpholine moiety was evaluated as a novel prodrug moiety for carboxylic acid containing drugs represented by diclofenac (1). Compound 2, the N-ethoxycarbonylmorpholine ester of diclofenac was synthesized and evaluated as a potential prodrug. The stability of the synthesized prodrug was evaluated in solutions of pH 1 and 7.4, and in plasma. The ester's half lives were found ...

Many therapeutic agents are manufactured and administered in prodrug forms. In this paper, a new classification system for prodrugs is proposed to provide useful information about where in the body a prodrug is converted to the active drug. In this system, prodrugs are classified into Type I or Type II and the respective Subtypes IA, IB, IIA, IIB or IIC based on their sites of conversion into t...

In light of the continued threat antimicrobial-resistant bacteria, new strategies to expand repertoire antimicrobial compounds are necessary. Prodrugs an underexploited strategy in this effort. Here, we report on enhanced activity a prodrug toward bacteria having enzyme capable its activation. A screen led us sulfurol ester antibiotic trans-3-(4-chlorobenzoyl)acrylic acid. An endogenous esteras...

Midodrine is a prodrug metabolized to the peripheral acting alpha agonist desglymidodrine and used treat orthostatic hypotension. Reports of overdose are rare, consequently there little gu...

Background Host defence peptide (HDP) has multiple properties [1,2] potentiating it as a novel anticancer agent. However disadvantages include systemic toxicity [3]. To address this, a prodrug was developed and the aim was to assess toxicity differentials between this prodrug and its active peptide component on T84 colonic carcinoma cells. Prodrug bio activation mechanism was also assessed by u...

Etodolac, a nonsteroidal antiinflammatory drug, widely used in arthritis is associated with gastric ulceration and irritation due to presence of free carboxylic group. The current investigation reports synthesis of mutual amide prodrug of etodolac by masking free carboxylic group with glucosamine, a nutritional supplement for treatment of arthritis. Confirmation and characterization of the stru...