Paclitaxel and docetaxel are established as the standards of care, either as monotherapy or in combination with other cytotoxic agents in metastasic breast cancer. In order to improve the efficiency of solvent-based paclitaxel and to overcome its drawbacks in terms of safety, a solvent-free formulation has been developed. This work is a review of the albumin-bound paclitaxel data relative to its pharmacodynamic and pharmacokinetic profiles, its therapeutic efficiency and its safety of use. The activity of albumin-bound paclitaxel in phase II and III trials indicates its significant clinical efficiency in the treatment of metastatic breast cancer. In lung and pancreatic cancer and in melanoma, the use of albumin-bound paclitaxel leads to interesting results which require further investigations. Preclinical and clinical studies have shown that albumin-bound paclitaxel is associated with a better tolerance compared to standard paclitaxel.
Twenty
nine original 3-nitroimidazo[1,2-a]pyridine
derivatives, bearing a phenylthio (or benzylthio) moiety at position
8 of the scaffold, were synthesized. In vitro evaluation
highlighted compound 5 as an antiparasitic hit molecule
displaying low cytotoxicity for the human HepG2 cell line (CC50 > 100 μM) alongside good antileishmanial activities
(IC50 = 1–2.1 μM) against L. donovani, L. infantum, and L. major; and
good antitrypanosomal activities (IC50 = 1.3–2.2
μM) against T. brucei brucei and T.
cruzi, in comparison to several reference drugs such as miltefosine,
fexinidazole, eflornithine, and benznidazole (IC50 = 0.6
to 13.3 μM). Molecule 5, presenting a low reduction
potential (E° = −0.63 V), was shown to
be selectively bioactivated by the L. donovani type
1 nitroreductase (NTR1). Importantly, molecule 5 was
neither mutagenic (negative Ames test), nor genotoxic (negative comet
assay), in contrast to many other nitroaromatics. Molecule 5 showed poor microsomal stability; however, its main metabolite (sulfoxide)
remained both active and nonmutagenic, making 5 a good
candidate for further in vivo studies.
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