In vitro Anti-proliferative Effects of ProLindac™, a Novel Dach-Platinum-Linked Polymer Compound, as a Single Agent and in Combination with Other Anti-cancer Drugs

Author(s):  
Maria Serova ◽  
Aïda Ghoul ◽  
Keyvan Rezaï ◽  
François Lokiec ◽  
Esteban Cvitkovic ◽  
...  
2013 ◽  
Vol 14 (7) ◽  
pp. 963-974 ◽  
Author(s):  
Vincent Jamier ◽  
Wioleta Marut ◽  
Sergio Valente ◽  
Christiane Chereau ◽  
Sandrine Chouzenoux ◽  
...  

2021 ◽  
Vol 12 ◽  
Author(s):  
Junjie Zeng ◽  
Wenying Zhao ◽  
Shuhua Yue

The high attrition rates of anti-cancer drugs during clinical development remains a bottleneck problem in pharmaceutical industry. This is partially due to the lack of quantitative, selective, and rapid readouts of anti-cancer drug activity in situ with high resolution. Although fluorescence microscopy has been commonly used in oncology pharmacological research, fluorescent labels are often too large in size for small drug molecules, and thus may disturb the function or metabolism of these molecules. Such challenge can be overcome by coherent Raman scattering microscopy, which is capable of chemically selective, highly sensitive, high spatial resolution, and high-speed imaging, without the need of any labeling. Coherent Raman scattering microscopy has tremendously improved the understanding of pharmaceutical materials in the solid state, pharmacokinetics of anti-cancer drugs and nanocarriers in vitro and in vivo. This review focuses on the latest applications of coherent Raman scattering microscopy as a new emerging platform to facilitate oncology pharmacokinetic research.


2002 ◽  
Vol 30 (2_suppl) ◽  
pp. 111-113 ◽  
Author(s):  
Laura Gribaldo

Haematopoietic tissues are the targets of numerous xenobiotics. The purpose of in vitro haematotoxicology is the prediction of adverse haematological effects from toxicants on human haematopoietic targets under controlled experimental conditions in the laboratory. Building on its foundations in experimental haematology and the wealth of haematotoxicological data found in experimental oncology, this field of alternatives toxicology has developed rapidly during the past decade. Preclinical and clinical drug development for anti-cancer drugs differs from that for other pharmaceuticals, because of the life-threatening nature of the disease. Treatment with anti-cancer drugs at clinically efficacious doses usually induces serious side-effects. The design of preclinical toxicology studies for anti-cancer drugs is intended to identify a safe clinical starting dose, characterise toxicities that could be encountered in human clinical trials, and determine whether these toxicities are reversible, manageable, and predictable. Although the myeloid colony-forming unit (CFU-GM) progenitor is most frequently evaluated, other defined progenitors and stem cells, as well as cell types found in the bone-marrow stroma, can now be evaluated in vitro. Genetic damage to haematopoietic cells can occur in the absence of any overt haematological signs. The development of tissue-specific screening systems that are able to give information about the toxic effects of chemicals, drugs and environmental hazards on target genes is needed, in order to make preliminary decisions or to set priorities for selection among large groups of chemicals and possible drugs.


Materials ◽  
2019 ◽  
Vol 12 (10) ◽  
pp. 1632
Author(s):  
Peisen Zhang ◽  
Junli Meng ◽  
Yingying Li ◽  
Zihua Wang ◽  
Yi Hou

Determining therapeutic efficacy is critical for tumor precision theranostics. In order to monitor the efficacy of anti-cancer drugs (e.g., Paclitaxel), a pH-sensitive ratiometric fluorescent imaging probe was constructed. The pH-sensitive ratiometric fluorescent dye ANNA was covalently coupled to the N-terminal of the cell-penetrating TAT peptide through an amidation reaction (TAT-ANNA). The in vitro cellular experiments determined that the TAT-ANNA probe could penetrate the cell membrane and image the intracellular pH in real time. The in vivo experiments were then carried out, and the ratiometric pH response to the state of the tumor was recorded immediately after medication. The TAT-ANNA probe was successfully used to monitor the pharmacodynamics of anti-cancer drugs in vivo.


2020 ◽  
Vol 46 (5) ◽  
pp. 846-851
Author(s):  
Mozhgan Aghajanzadeh ◽  
Ehsan Naderi ◽  
Mostafa Zamani ◽  
Ali Sharafi ◽  
Mahmoud Naseri ◽  
...  

Molecules ◽  
2019 ◽  
Vol 24 (2) ◽  
pp. 266 ◽  
Author(s):  
Adam Bohr ◽  
Thais Nascimento ◽  
Necati Harmankaya ◽  
Johan Weisser ◽  
Yingya Wang ◽  
...  

Many anti-cancer drugs are difficult to formulate into an oral dosage form because they are both poorly water-soluble and show poor permeability, the latter often as a result of being an intestinal efflux pump substrate. To obtain a more water-soluble formulation, one can take advantage of the higher solubility of the amorphous form of a given drug, whereas to increase permeability, one can make use of an efflux pump inhibitor. In this study, a combination of these two strategies was investigated using the co-amorphous approach, forming an amorphous mixture of two anti-cancer drugs, docetaxel (DTX) and bicalutamide (BIC). The efflux substrate, DTX, was combined with the efflux inhibitor, BIC, and prepared as a single phase co-amorphous mixture at a 1:1 molar ratio using vibrational ball milling. The co-amorphous formulation was tested in vitro and in vivo for its dissolution kinetics, supersaturation properties and pharmacokinetics in rats. The co-amorphous formulation showed a faster in vitro dissolution of both drugs compared to the control groups, but only DTX showed supersaturation (1.9 fold) compared to its equilibrium solubility. The findings for the co-amorphous formulation were in agreement with the pharmacokinetics data, showing a quicker onset in plasma concentration as well as a higher bioavailability for both DTX (15-fold) and BIC (3-fold) compared to the crystalline drugs alone. Furthermore, the co-amorphous formulation remained physically stable over 1.5 years at 4 °C under dry conditions.


Digestion ◽  
1996 ◽  
Vol 57 (1) ◽  
pp. 22-28 ◽  
Author(s):  
G. Weckbecker ◽  
F. Raulf ◽  
L. Tolcsvai ◽  
C. Bruns
Keyword(s):  

1998 ◽  
Vol 24 (5) ◽  
pp. 345-366 ◽  
Author(s):  
K.M.L. Crommentuyn ◽  
J.H.M. Schellens ◽  
J.D. van den Berg ◽  
J.H. Beijnen

1990 ◽  
Vol 25 (4) ◽  
pp. 252-256 ◽  
Author(s):  
B. Sundman-Engberg ◽  
U. Tidefelt ◽  
J. Liliemark ◽  
C. Paul

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