Update of carcinogenicity studies in animals and humans of 535 marketed pharmaceuticals

Brambilla, Giovanni; Mattioli, Francesca; Robbiano, Luigi; Martelli, Antonietta

doi:10.1016/j.mrrev.2011.09.002

Cited by 32 publications

(23 citation statements)

References 127 publications

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“…Fluoxetine, which is a popular antidepressant used for many years for the treatment of anxiety, depression and bulimia, was not cytotoxic or mutagenic in experiments with Wistar rats treated intraperitoneally for 24 h (acute form) (Figure 3), or via gavage for 24 h (acute form) or 7 days (subchronic form) (Figure 4). These results corroborate a compendium of reports of genotoxicity and carcinogenicity assays performed on marketed antidepressants, among them fluoxetine: a negative response in regard to genotoxicity assays (reverse mutation with Salmonella typhimurium, DNA repair synthesis with rat primary hepatocytes, gene mutation with mouse lymphoma L5178Y cells, and sister chromatid exchanges with bone marrow cells of Chinese hamster in vivo) and carcinogenicity assays in rodents (long-term carcinogenesis assays with B6C3F1 mice and Sprague-Dawley rats) and humans (breast cancer, ovarian cancer, colorectal cancer, cancer at other sites) (Brambilla et al, 2009(Brambilla et al, , 2010(Brambilla et al, , 2012. Lemos et al (2005) also showed that fluoxetine at concentrations of 0.2 and 1.0 mg/ mL was not genotoxic by the comet assay in Chinese hamster ovary (CHO) cultured cells.…”

Section: Discussionmentioning

confidence: 99%

Cytotoxicity and mutagenicity of fluoxetine hydrochloride (Prozac), with or without vitamins A and C, in plant and animal model systems

Düsman¹,

Almeida²,

Mariucci³

et al. 2014

Genet. Mol. Res.

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ABSTRACT. Fluoxetine, commonly known as Prozac, is the first representative of the so-called new generation of antidepressants that promise efficacy, with few side effects, against deep depression, nervous bulimia, and anxiety. As there is a growing number of people suffering from anxiety and depression; consequently, the use of fluoxetine is also increasing. Verifying absence of drug effects such as cytotoxicity or mutagenicity is of great importance. Certain vitamins, such as vitamin A (retinol, retinoids) and vitamin C (ascorbic acid) protect and are extremely active against mutagens. We evaluated the cytotoxic and mutagenic activity of fluoxetine, with and without concomitant administration of vitamin A or C, in Allium cepa meristem cells and Wistar rat bone marrow cells. The A. cepa meristem cells Cytotoxicity and mutagenicity of fluoxetine showed fluoxetine cytotoxicity; concomitant treatment with vitamin A or C proved non-protective. Treatment of Wistar rats with fluoxetine intraperitoneally or via gavage did not affect cell division or cause clastogenic effects. Vitamin A and C did not affect the cytotoxicity or mutagenicity of fluoxetine in the rat cells.

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Section: Discussionmentioning

confidence: 99%

Cytotoxicity and mutagenicity of fluoxetine hydrochloride (Prozac), with or without vitamins A and C, in plant and animal model systems

Düsman¹,

Almeida²,

Mariucci³

et al. 2014

Genet. Mol. Res.

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“…Son basamakta ise, bir in vivo genotoksisite testi, genellikle rodent hematopoietik hücreleri üzerinde kromozomal hasarı belirleyebilen bir test (ya mikronukleus testi ya da metafaz hücrelerinde kromozomal aberasyon testi) yapılması önerilmektedir. In vivo testlerle, organizmada metabolize edildikten sonra oluşabilen genotoksik ajanların belirlenmesi mümkün olmaktadır (ICH, 2011;Brambilla, Mattioli, Rbiano & Martelli, 2012).…”

Section: Ich Ve Oecd Kılavuzları Perspektifinden Preklinik Genotoksisunclassified

The importance of genotoxicity tests in new drug development process<p>Genotoksisite testlerinin yeni ilaç geliştirme sürecindeki önemi

2018

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In the preclinic investigation period at the beginning of the drug development process, it is an obligation to subject candidate drugs to genotoxicty investigations. Genotoxicty data of drugs that are developed with these tests are demanded as a part of the security evaluation process by regulatory authorities in various countries. The demand of these laboring and costly data by regulatory authorities of various countries in different standards prevents potential candidate drugs from being marketed, interrupts the drug development process and causes unnecessary utilization of experimental materials in researches. Therefore, nowadays, it is generally accepted that the researches aimed at achieving these data are implemented with standardized approaches in the guidelines of international harmonisation organizations such as ICH (International Council for Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use) and OECD (Organisation for Economic Cooperation and Development). In this review, it is aimed to provide current information about the various genotoxicity tests which are used commonly in the drug development process, in accordance with ICH, OECD guidelines and literature. Extended English summary is in the end of Full Text PDF (TURKISH) file.Özetİlaç geliştirme sürecinin başlangıcındaki preklinik araştırma döneminde, aday ilaçların genotoksisite testlerinden geçirilmesi bir zorunluluktur. Bu testlerle elde edilen genotoksisite verileri, çeşitli ülkelerdeki düzenleyici otoriteler tarafından güvenlilik değerlendirme sürecinin bir parçası olarak istenmektedir. Elde edilmesi oldukça zahmetli ve maliyetli olan bu bilgilerin, farklı ülkelerin düzenleyici otoriteleri tarafından değişik standartlarda istenmesi, potansiyel ilaç adaylarının pazarlamasını engellemekte, ilaç geliştirme sürecini kesintiye uğratmakta ve araştırmalarda gereksiz yere deney materyali kullanımına neden olmaktadır. Bu bakımdan, günümüzde bu bilgileri elde etmeyi amaçlayan araştırmaların, ICH (İnsanda Kullanılan İlaçların Ruhsatlandırılması İçin Teknik Gerekliliklerin Uyumlandırılması Uluslararası Birliği) ve OECD (Ekonomik Kalkınma ve İşbirliği Örgütü) gibi uluslararası harmonizasyon örgütlerinin kılavuzlarında standardize edilen yaklaşımlarla uygulanması genel kabul görmektedir. Bu derlemede, ilaç geliştirme sürecinde kullanılan genotoksisite testlerine ilişkin, ICH, OECD kılavuzları ve literatür ışığında güncel bilgiler verilmesi amaçlanmıştır.

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“…Note that silver ions can strongly attract the sulfhydryl group of bacterial proteinase, which causes resulting in the loss of enzyme activity of the original bacteria respiration and thus the bacterial apoptosis . Ag + is well used to prepare safe and non‐carcinogenic broad‐spectrum fungicides, however, difficult to cause damage to complex tissue cells …”

Section: Introductionmentioning

confidence: 99%

New 3D Supramolecular Ag(I) Coordination Polymer Crystal Containing 2‐Quinaldic Acid Radical Biological Ligand: Crystal Structure and Anticancer Activity

Wang

Jun

Lei

et al. 2018

Crystal Research and Technology

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A new coordination polymer of {[Ag(Qina)(Bpp)]·(H 2 O) 2 } n (Qina =2-quinolinecarboxylic-carboxylate, Bpp = 4,4'-trimethylenedipyridine) is successfully synthesized and the structure is determined using single crystal X-ray diffraction. The complex is crystallized in the monoclinic system with P2 1 /c space group: Each atom of Ag(I) is chelated by one Qina group, with each Bpp ligand bridging two Ag(I) atoms to form the 1D polymer chains. Furthermore, the 3D supramolecular architecture is a costructure directed via weak stacking interactions of C-H···π and hydrogen bond. The complex shows competitive binding affinities in calf thymus DNA (ct-DNA) interaction by fluorescence spectroscopy. In addition, the complexes' cytotoxic activity is explored for two kinds of cancer cell lines (Hela, MCF-7), indicating an anticancer activity and cytotoxicity. CCDC: 1553426 Experimental Section Materials and InstrumentsAll reagents and solvents used in experimental and tests are commercially available and directly used without any treatment. As for characterizations, a model Finnigan EA 1112 was employed for Elemental analyses (including C, H, and N); and a Thermo Nicolet 380 FT-IR spectrophotometer for IR analysis by KBr disks method; a Bruker SMART APEX2 CCD diffractometer (Mo Kα, λ = 0.71073Å) for polymorphism analysis by single-crystal X-ray diffraction; as well as a Perkin-Elmer LS55 fluorescence spectrofluorimeter for emission spectrum.

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Update of carcinogenicity studies in animals and humans of 535 marketed pharmaceuticals

Cited by 32 publications

References 127 publications

Cytotoxicity and mutagenicity of fluoxetine hydrochloride (Prozac), with or without vitamins A and C, in plant and animal model systems

Cytotoxicity and mutagenicity of fluoxetine hydrochloride (Prozac), with or without vitamins A and C, in plant and animal model systems

The importance of genotoxicity tests in new drug development process<p>Genotoksisite testlerinin yeni ilaç geliştirme sürecindeki önemi

New 3D Supramolecular Ag(I) Coordination Polymer Crystal Containing 2‐Quinaldic Acid Radical Biological Ligand: Crystal Structure and Anticancer Activity

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