Current Pharmaceutical Design - Volume 15, Issue 2, 2009

The first targeted therapeutic is presented by penicillin that was discovered by Alexander Fleming in 1928. The first radioactive-tracer experiments were performed as early as in 1913 by Fritz Haber, Ernest Rutherford and George Charles de Hevesy. The term “Magic bullet” was released by Paul Ehrlich and refers to the concept of selectively targeting a distinct bacterium without affecting other organisms. HIV infection which was Read More

Since protein kinases are frequently mutated or otherwise deregulated in human malignancies, they serve as a target for differentiating between tumor cells and normal tissues. Imatinib mesylat (IM), an inhibitor of the BCR-ABL tyrosine kinase was introduced in 2001 and has revolutionized the treatment of patients with chronic myeloid leukemia (CML). Since 2005 a second generation of tyrosine kinase inhibitors is to follow in I Read More

Pharmaceuticals have historically been produced by either chemical synthesis or whole cell fermentation. The former is applied to synthetic small molecules while the latter to natural products. As a result of recent advances in rapid discovery of enzymes through genome mining and metagenomics, and their tunability in functions and stability through directed evolution, biocatalysis is emerging to be a transformationa Read More

Packaging small-molecule drugs into nanoparticles improves their bio-availability, bio-compatibility and safety profiles. Multifunctional particles carrying large drug payloads for targeted transport, immune evasion and favourable drug release kinetics at the target site, require a certain minimum size usually 30-300 nm diameter, so are nanoparticles. Targeting particles to a disease site can signal the presence of the dise Read More

Delivering a drug to a specific target in the body is comparable to the “magic bullet principle” applied in Nuclear Medicine. If clinical medicine today found treatment options by targeting specific receptors, proteins or enzymes by “small-molecule drugs” it utilizes concepts that have been initially described by Nobel Laureate George von Hevesy as “tracer principle”. This article is going to show that molecular imaging probes in Nuc Read More

Targeted therapies have improved and will continue to improve the outcome of lung cancer. Current strategies focus on the blockade of growth factor receptors and the inhibition of angiogenesis. Epidermal growth factor receptor (EGFR)-directed tyrosine kinase inhibitors (TKIs) have already been established as a treatment option in patients with advanced non-small cell lung cancer (NSCLC) progressing after prior treatment Read More

It is now exactly 100 years ago (1908) that Paul Ehrlich, who is regarded as the inventor of the concept of targeted therapy, received the Nobel Prize for Medicine. His initial perception leading to this theory was derived from observations that certain substances are capable of selectively staining either tissues or microorganisms. These observations culminated in the discovery of the inorganic mercury compound arsphena Read More