Due to the lack of effective drugs, trypanosomiases and leishmaniases pose a major threat to many million people living in resource-poor countries. Despite this, there has been little research and development for new drugs in the field, and little progress has been made in the treatment of these diseases over the past decades. However, in very recent years, thanks also to the involvement of several philanthropic organizations, the chemotherapeutic arsenal has broadened with the introduction of the first combination therapy. The optimal clinical efficacy and safety of nifurtimox–eflornithine combination against second-stage human African trypanosomiasis represents an encouraging first step towards more effective and more affordable treatments. Along the same line, single chemical entities able to modulate multiple targets simultaneously (the so called multi-target-directed.ligands, MTDLs) may offer the potential of a superior efficacy and lower cost than the current available drugs. Furthermore, with respect to combinations,, MTDLs should provide a simpler regimen for antitrypanosomatid therapy. Herein, examples of MTDLs taken from studies in the author’s laboratory will be discussed.
Multi-Target-Directed Ligands as innovative tools to combat Trypanosomatid diseases
BOLOGNESI, MARIA LAURA
2011
Abstract
Due to the lack of effective drugs, trypanosomiases and leishmaniases pose a major threat to many million people living in resource-poor countries. Despite this, there has been little research and development for new drugs in the field, and little progress has been made in the treatment of these diseases over the past decades. However, in very recent years, thanks also to the involvement of several philanthropic organizations, the chemotherapeutic arsenal has broadened with the introduction of the first combination therapy. The optimal clinical efficacy and safety of nifurtimox–eflornithine combination against second-stage human African trypanosomiasis represents an encouraging first step towards more effective and more affordable treatments. Along the same line, single chemical entities able to modulate multiple targets simultaneously (the so called multi-target-directed.ligands, MTDLs) may offer the potential of a superior efficacy and lower cost than the current available drugs. Furthermore, with respect to combinations,, MTDLs should provide a simpler regimen for antitrypanosomatid therapy. Herein, examples of MTDLs taken from studies in the author’s laboratory will be discussed.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
