Drug, drugs strategies

Despite the presence of the more lipophilic side-chain in 18, compared to the glycerol side-chain of 12, a pro-drug strategy was necessary to achieve sufficient oral bioavailabUity. Thus, the ethyl ester pro-drug form of 18, oseltamivir (GS 4104,... 

Decision trees for optimal drug design strategies have been proposed by Topliss [64] and by Purcell et al. [65]. 

Topical therapy is the initial drug treatment strategy for patients with mild to moderate psoriasis. It is estimated that approximately 70% to 80% of all patients with psoriasis can he treated adequately with use of topical therapy.1 Topical therapies include corticosteroids, coal tar products, anthralin, vitamin D3 analogues such as calcipotriol, retinoids such as tazarotene, and topical immunomodulators such as tacrolimus and pime-crolimus.18 Vitamin D3 analogues and topical retinoids all affect keratinocyte functions and the immune response. Currently, these are in wider use than is either anthralin or coal tar preparations. 

Hall W, Solowij N and Lemon J (1994). The Health and Psychological Consequences of Cannabis Use (National Drug Strategy Monograph Series No. 25). Australian Government Publishing Service, Canberra. 

Tukker, G., Houston, J. B., Huang, S.-M., Optimizing drug development strategies to assess drug metabolism/ transporter interaction potential — toward a consensus, Clin. Pharmacol. Ther. 2001, 70, 103-114. 

Overall, the prodrug approach is a well-established strategy to improve the bioavailability and targeting of pharmacophores, and is a vital component in the development of therapeutics and drug-delivery strategies. 

Lastly, pharmacogenomics could provide new tools for the design of more specific and active CNS pharmaceuticals. The efficacy of a broad spectrum of neuro-pharmaceutical drugs is often complicated by their inability to reach their site of action because of the BBB. One way to overcome this is to use carrier-mediated transport at the luminal and/or abluminal membranes of the endothelial cells of the BBB. This will provide a physiologically based drug delivery strategy for the brain by designing new chemical entities or fused proteins that can cross the BBB via these transporters. 

T. Coviello, P. Matricardi, and F. Alhaique, Drug delivery strategies using polysaccharidic gels, Expert Opin. Drug Deliv., 3 (2006) 395 -04. 

Given such difficulties, it is not unsurprising that bioavailabilities below 1 per cent are often recorded in the context of oral biopharmaceutical drug delivery. Strategies pursued to improve bioavailability include physically protecting the drug via encapsulation and formulation as microemulsions/microparticulates, as well as inclusion of protease inhibitors and permeability... 

Our next step was to assess whether the methodology used to calculate hydration free energy differences for simple carbonyl-containing compounds9 was suitable for heteroaromatic bases. Since our drug design strategy entailed analysis of purine riboside hydration, a series of azanaphthalenes was initially selected for analysis in part because of their structural similarity to purines and in part because of the extensive... 

The use of BRMs to treat human disease has its origins in the use of bacterial toxins to treat cancer by William B. Coley.73 These early studies resulted in the use of microbi-ally-derived substances such as BCG, Picibanil, carbohydrates from plants or fungi such as Krestin and Lentinan, other products such as Biostim and Broncho-Vaxom, as well as thymic extracts (Table 9.4). However, the lot-to-lot variation in the manufacture of these drugs has dampened enthusiasm. Equally, the focus on MOAs in drug development strategies has also dampened developmental efforts. The particulate nature of some BRMs can also result in pulmonary thrombosis and respiratory distress following i.v. injection. However, BRMs are commonly used to treat bladder cancer and derivatives of natural products are routinely used clinically. 

Klabunde, T. and Hessler, G. (2002) Drug design strategies for targeting G protein-coupled receptors. ChemBioChem 3,928-944. 

An increasing number of preclinical and clinical studies have been conducted in recent years aiming to clarify the barrier function of the colonic epithelium in more detail and to devise drug delivery strategies, for example, by modulating factors limiting colonic drug absorption. For preclinical... 

---