Structure–activity considerations and in vitro approaches to assess the genotoxicity of 19 methane-, benzene- and toluenesulfonic acid esters

Glowienke, Susanne; Frieauff, Wilfried; Allmendinger, Thomas; Martus, Hans-Joerg; Suter, Willi; Mueller, Lutz

doi:10.1016/j.mrgentox.2004.10.004

Cited by 51 publications

(38 citation statements)

References 10 publications

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“…PEDOT oxidation is performed in the presence of alcohol polymerization or post implantation may induce the formation of sulphonic acid esters. In particular, methyl and ethyl methanesulphonate esters are known genotoxins and carcinogens in rats and mice (IARC 2004), whereas the toxicity of p-toluene sulphonate esters has been generally established (Glowienke et al 2005). Unfortunately, these materials are not selective enough for neurons and over time the neural signal decreases.…”

Section: Tissue Engineering Applicationsmentioning

confidence: 99%

Applications of conducting polymers and their issues in biomedical engineering

Ravichandran

Sundarrajan

Venugopal

et al. 2010

J. R. Soc. Interface.

366

253

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Conducting polymers (CPs) have attracted much interest as suitable matrices of biomolecules and have been used to enhance the stability, speed and sensitivity of various biomedical devices. Moreover, CPs are inexpensive, easy to synthesize and versatile because their properties can be readily modulated by (i) surface functionalization techniques and (ii) the use of a wide range of molecules that can be entrapped or used as dopants. This paper discusses the various surface modifications of the CP that can be employed in order to impart physico-chemical and biological guidance cues that promote cell adhesion/proliferation at the polymer-tissue interface. This ability of the CP to induce various cellular mechanisms widens its applications in medical fields and bioengineering.

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Section: Tissue Engineering Applicationsmentioning

confidence: 99%

Applications of conducting polymers and their issues in biomedical engineering

Ravichandran

Sundarrajan

Venugopal

et al. 2010

J. R. Soc. Interface.

366

253

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“…Acceptable (maximum) daily intake (ADI) and duration of exposure Acceptable (maximum) daily intake (ADI) and duration of exposure 64 weeks ADI = 120 lg While this is a general guidance, some classes of bacterial mutagens (e.g., many sulfonic acid esters) may be missed by this approach since they require higher concentrations to be detected in the bacterial reverse mutation test (Glowienke et al, 2005) and they are considered to be trans-species rodent carcinogens (Ashby and Paton, 1993;Matthews et al, 2005). Hence, an evaluation of the available literature data on compounds with similar structures must be made when judging the adequacy of evaluating impurities as part of the API.…”

Section: Concentration Of Impurity (%) Concentration Of Impurity (Ppm)mentioning

confidence: 99%

A rationale for determining, testing, and controlling specific impurities in pharmaceuticals that possess potential for genotoxicity

Müller

Mauthe

Riley³

et al. 2006

Regulatory Toxicology and Pharmacology

402

193

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“…When choosing between pharmacologically active and tested and other forms of biologic agents that are not bioequivalent such as Imatib, consideration must also be given to patient safety, which may be impacted by product degradation and the associated generation of impurities. This is of particular concern with imatinib as the active ingredient is a mesylate salt [5,8], and degradation byproducts such as mesylate esters of methanesulfonic acid are known to be highly genotoxic [9]. This case report suggests that switching from the pharmacologically active and tested form of imatinib (Glivec Ò ) to a copy product may compromise efficacy and could have multiple negative impacts on long-term patient outcomes.…”

mentioning

confidence: 99%

Failure of copy Imatib (CIPLA, India) to maintain hematologic and cytogenetic responses in chronic myeloid leukemia in chronic phase

Mattar

2010

Int J Hematol

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A 50-year-old woman presented with CML-CP and was initially treated with branded imatinib (Glivec) 400 mg/day. She rapidly achieved a complete hematologic response (CHR), at which point she switched therapy to a copy version of imatinib (Imatib). She received 400 mg/day of Imatib for 3 months, during which time her platelet count decreased from 250 x 10(9) to 105 x 10(9)/L and her hemoglobin count fell from 12.8 to 11 g/dL. The patient's total leukocyte count rose rapidly from 4 x 10(9) to 70 x 10(9)/L, and the CHR was lost. At this point, therapy was switched back to Glivec at 400 mg/day, and the CHR was rapidly regained. Furthermore, the patient achieved a major cytogenetic response by 6 months after reintroduction of Glivec. This case report suggests a difference in clinical efficacy between the authorized form of imatinib (Glivec) and the copy version of the drug (Imatib). The exact reasons for the observed difference in clinical efficacy are unknown, but likely relate to the use of alternative polymorphic forms of the drug. Glivec can be obtained directly from the manufacturer (Novartis Pharmaceuticals) through a variety of patient access programs that should be fully explored when needed.

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Structure–activity considerations and in vitro approaches to assess the genotoxicity of 19 methane-, benzene- and toluenesulfonic acid esters

Cited by 51 publications

References 10 publications

Applications of conducting polymers and their issues in biomedical engineering

Applications of conducting polymers and their issues in biomedical engineering

A rationale for determining, testing, and controlling specific impurities in pharmaceuticals that possess potential for genotoxicity

Failure of copy Imatib (CIPLA, India) to maintain hematologic and cytogenetic responses in chronic myeloid leukemia in chronic phase

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