Kamil Dyrka, A. Czarnywojtek, M. Borowska, Jeremi Kościński, J. Moskal, N. Sawicka-Gutaj, A. Lewandowska, S. V. Van Gool, M. Fichna, P. Gut, K. Pietrończyk, Patryk Graczyk, M. Dworacka
{"title":"替莫唑胺:一种至今仍很重要的细胞抑制药物","authors":"Kamil Dyrka, A. Czarnywojtek, M. Borowska, Jeremi Kościński, J. Moskal, N. Sawicka-Gutaj, A. Lewandowska, S. V. Van Gool, M. Fichna, P. Gut, K. Pietrończyk, Patryk Graczyk, M. Dworacka","doi":"10.32383/appdr/159449","DOIUrl":null,"url":null,"abstract":"TMZ has an advantage over other traditional alkylating agents (carmustine, lomustine, procarbazine), which are highly toxic and have poor patient survival. TMZ circumvents these problems because cytochrome P450 enzymes and the kidneys are not involved in its metabolism, it has predictable side effects (nausea, vomiting, thrombocytopenia, neutropenia), which are usually reversible and only mild to moderate, have been widely described.\nAbout half of patients treated with TMZ have high drug resistance induced by activity of O6-methylguanine methyltransferase. Cancer stem cells (CSCs), which are found among the neoplastic cell population, have also been shown to be responsible for resistance to TMZ. Additionally, acquired immunity, induced by TMZ’s epigenetic and genetic alterations, may develop. Currently, there are new therapeutic strategies for GBM based on nanotechnology, which are aimed at improving TMZ treatment (e.g. the use of apolipoprotein), or other techniques (siRNA, which increases the oxygen level in the tumour).\nThus, although TMZ was discovered more than three decades ago, this drug will be used to treat not only GBM, but also a large number of neoplastic pathologies. Further research focused on understanding the mechanisms of action and resistance to TMZ is required to improve its clinical application today and in the future.\n\nKeywords: alkylating agents, drug resistance, chemotherapy, nanoparticles, cancer, glioblastoma multiforme","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4000,"publicationDate":"2023-03-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Temozolomide: a cytostatic drug that is still important today\",\"authors\":\"Kamil Dyrka, A. Czarnywojtek, M. Borowska, Jeremi Kościński, J. Moskal, N. Sawicka-Gutaj, A. Lewandowska, S. V. Van Gool, M. Fichna, P. Gut, K. Pietrończyk, Patryk Graczyk, M. Dworacka\",\"doi\":\"10.32383/appdr/159449\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"TMZ has an advantage over other traditional alkylating agents (carmustine, lomustine, procarbazine), which are highly toxic and have poor patient survival. TMZ circumvents these problems because cytochrome P450 enzymes and the kidneys are not involved in its metabolism, it has predictable side effects (nausea, vomiting, thrombocytopenia, neutropenia), which are usually reversible and only mild to moderate, have been widely described.\\nAbout half of patients treated with TMZ have high drug resistance induced by activity of O6-methylguanine methyltransferase. Cancer stem cells (CSCs), which are found among the neoplastic cell population, have also been shown to be responsible for resistance to TMZ. Additionally, acquired immunity, induced by TMZ’s epigenetic and genetic alterations, may develop. Currently, there are new therapeutic strategies for GBM based on nanotechnology, which are aimed at improving TMZ treatment (e.g. the use of apolipoprotein), or other techniques (siRNA, which increases the oxygen level in the tumour).\\nThus, although TMZ was discovered more than three decades ago, this drug will be used to treat not only GBM, but also a large number of neoplastic pathologies. Further research focused on understanding the mechanisms of action and resistance to TMZ is required to improve its clinical application today and in the future.\\n\\nKeywords: alkylating agents, drug resistance, chemotherapy, nanoparticles, cancer, glioblastoma multiforme\",\"PeriodicalId\":7147,\"journal\":{\"name\":\"Acta poloniae pharmaceutica\",\"volume\":\" \",\"pages\":\"\"},\"PeriodicalIF\":0.4000,\"publicationDate\":\"2023-03-03\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Acta poloniae pharmaceutica\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.32383/appdr/159449\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Acta poloniae pharmaceutica","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.32383/appdr/159449","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Temozolomide: a cytostatic drug that is still important today
TMZ has an advantage over other traditional alkylating agents (carmustine, lomustine, procarbazine), which are highly toxic and have poor patient survival. TMZ circumvents these problems because cytochrome P450 enzymes and the kidneys are not involved in its metabolism, it has predictable side effects (nausea, vomiting, thrombocytopenia, neutropenia), which are usually reversible and only mild to moderate, have been widely described.
About half of patients treated with TMZ have high drug resistance induced by activity of O6-methylguanine methyltransferase. Cancer stem cells (CSCs), which are found among the neoplastic cell population, have also been shown to be responsible for resistance to TMZ. Additionally, acquired immunity, induced by TMZ’s epigenetic and genetic alterations, may develop. Currently, there are new therapeutic strategies for GBM based on nanotechnology, which are aimed at improving TMZ treatment (e.g. the use of apolipoprotein), or other techniques (siRNA, which increases the oxygen level in the tumour).
Thus, although TMZ was discovered more than three decades ago, this drug will be used to treat not only GBM, but also a large number of neoplastic pathologies. Further research focused on understanding the mechanisms of action and resistance to TMZ is required to improve its clinical application today and in the future.
Keywords: alkylating agents, drug resistance, chemotherapy, nanoparticles, cancer, glioblastoma multiforme
期刊介绍:
The international journal of the Polish Pharmaceutical Society is published in 6 issues a year. The journal offers Open Access publication of original research papers, short communications and reviews written in English, in all areas of pharmaceutical sciences. The following areas of pharmaceutical sciences are covered: Analysis, Biopharmacy, Drug Biochemistry, Drug Synthesis, Natural Drugs, Pharmaceutical Technology, Pharmacology and General.
A bimonthly appearing in English since 1994, which continues “Acta Poloniae Pharmaceutica”, whose first issue appeared in December 1937. The war halted the activity of the journal’s creators. Issuance of “Acta Poloniae Pharmaceutica” was resumed in 1947. From 1947 the journal appeared irregularly, initially as a quarterly, then a bimonthly. In the years 1963 – 1973 alongside the Polish version appeared the English edition of the journal. Starting from 1974 only works in English are published in the journal. Since 1995 the journal has been appearing very regularly in two-month intervals (six books a year). The journal publishes original works from all fields of pharmacy, summaries of postdoctoral dissertations and laboratory notes.