The lipophilic character of quercetin suggests that it can cross enterocyte membranes via simple diffusion. Therefore, it should be more bioavailable than its glucosides, which require preliminary hydrolysis or active transport for absorption. However, the published human studies show that quercetin is less bioavailable than its glucosides. Assuming that low bioavailability of quercetin aglycon...

Sorafenib (Nexavar ; Bayer Pharmaceuticals, West Haven, CT) (Fig. 1A) and sunitinib (Sutent ; Pfizer Inc., New York, NY) (Fig. 1B) are orally bioavailable, small molecule inhibitors of multiple intracellular and receptor protein kinases that are components of signaling pathways that control tumor growth and angiogenesis. These agents have similar drug profiles and overlapping targets, which are...

Several drug discovery and design endevours are focused on an exhaustive exploration of the drug-like chemical space with the final goal of identifying compounds that can be developed clinically. The traditional drug-like chemical space has been defined using old drugs with empirical rules such as the Lipinski’s Rule-of-Five (RO5). Therefore, promising drug candidates may be overlooked because ...

Background: Deferasirox is an orally bioavailable synthetic, tridentate iron chelator that binds iron at a 2:1 ratio. The generic brand for this drug is still not available in Indonesia. We aimed to compare the efficacy between the generic drug and its innovator (Exjade®) by a study of bioequivalence in Indonesia among healthy volunteers. Methods: An open-label, single-dose, two-sequence, rand...

I glad to see James Maskalyk’s review of grapefruit and drug interactions, as I have been concerned for some time about the need to increase awareness of this issue. However, I would like to comment on drugs that were listed as if the effects were equal. Some patients enjoy grapefruit, and it is unkind to impose an unnecessary prohibition. The magnitude of the grapefruit effect is related to th...

Leishmaniasis is a parasitic infection that afflicts approximately 12 million people worldwide. There are several limitations to the approved drug therapies for leishmaniasis, including moderate to severe toxicity, growing drug resistance, and the need for extended dosing. Moreover, miltefosine is currently the only orally available drug therapy for this infection. We addressed the pressing nee...

BACKGROUND Gonadal steroid levels decline with age in men. Whether low testosterone levels affect the development of common age-related disorders, including physical functioning and falling, is unclear. METHODS This longitudinal, observational follow-up study sought to determine whether low testosterone levels are associated with physical performance and fall risk in older men. A total of 258...

Over the last decade, there has been an increasing effort to fight inflammatory conditions establishing new multitarget approaches. Chronic inflammation is implicated in many multifactorial diseases, constituting a great economic burden and chronic health problem. In attempt develop potent multifunctional anti-inflammatory agents, cinnamic-pyrrole hybrid (6) was synthesized screened for its ant...

Despite the numerous articles appearing in scientific journals, very few field applications of phytoextraction have been successfully realized. To overcome the imbalance between the technology’s potential and its drawbacks, there is growing interest in the use of plants to reduce only the fraction that is the most hazardous to the environment and human health, that is to target the bioavailable...