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Lomustine
Lomustine (INN); abbreviated as CCNU; original brand name CeeNU, now marketed as Gleostine) is an alkylating nitrosourea compound used in chemotherapy. It is closely related to semustine and is in the same family as streptozotocin. It is a highly lipid-soluble drug, thus it crosses the blood–brain barrier. This property makes it ideal for treating brain tumors, which is its primary use, although it is also used to treat Hodgkin lymphoma as a second-line option. Lomustine has a long time to nadir (the time when white blood cells reach their lowest number). Unlike carmustine, lomustine is administered orally. It is a bifunctional alkylating agent Alkylation is the transfer of an alkyl group from one molecule to another. The alkyl group may be transferred as an alkyl carbocation, a free radical, a carbanion, or a carbene (or their equivalents). Alkylating agents are reagents for effectin ..., alkylates both DNA and RNA, has the ability to created interstrand cross-links ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nitrosourea Compounds
Nitrosourea is both the name of a molecule, and a class of compounds that include a nitroso (R-NO) group and a urea. Examples Examples include: * Arabinopyranosyl-''N''-methyl-''N''-nitrosourea (Aranose) * Carmustine (BCNU, BiCNU) * Chlorozotocin * Ethylnitrosourea (ENU) * Fotemustine * Lomustine (CCNU) * Nimustine * ''N''-Nitroso-''N''-methylurea (NMU) * Ranimustine (MCNU) * Semustine * Streptozocin (Streptozotocin) Nitrosourea compounds are DNA alkylating agents and are often used in chemotherapy. They are lipophilic and thus can cross the blood–brain barrier, making them useful in the treatment of brain tumors such as glioblastoma multiforme. File:Aranose (Haworth).svg, Arabinopyranosyl-''N''-methyl-''N''-nitrosourea File:Carmustine.svg, Carmustine File:Chlorozotocin (Haworth).svg, Chlorozotocin File:ENU.svg, Ethylnitrosourea File:Fotemustine.svg, Fotemustine File:Lomustine.svg, Lomustine File:N-Nitroso-N-methylurea.svg, ''N''-Nitroso-''N''-methylurea File:Nimus ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nitrosoureas
Nitrosourea is both the name of a molecule, and a class of compounds that include a nitroso (R-NO) group and a urea. Examples Examples include: * Arabinopyranosyl-''N''-methyl-''N''-nitrosourea (Aranose) * Carmustine (BCNU, BiCNU) * Chlorozotocin * Ethylnitrosourea (ENU) * Fotemustine * Lomustine (CCNU) * Nimustine * ''N''-Nitroso-''N''-methylurea (NMU) * Ranimustine (MCNU) * Semustine * Streptozocin (Streptozotocin) Nitrosourea compounds are DNA alkylating agents and are often used in chemotherapy. They are lipophilic and thus can cross the blood–brain barrier, making them useful in the treatment of brain tumors such as glioblastoma multiforme. File:Aranose (Haworth).svg, Arabinopyranosyl-''N''-methyl-''N''-nitrosourea File:Carmustine.svg, Carmustine File:Chlorozotocin (Haworth).svg, Chlorozotocin File:ENU.svg, Ethylnitrosourea File:Fotemustine.svg, Fotemustine File:Lomustine.svg, Lomustine File:N-Nitroso-N-methylurea.svg, ''N''-Nitroso-''N''-methylurea ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Semustine
Semustine (1- (2-Chloroethyl)-3-(trans-4-methylcyclohexyl)- 1-nitrosourea, MeCCNU) is an alkylating nitrosourea compound used in chemotherapy treatment of various types of tumours. Due to its lipophilic property, semustine can cross the blood-brain barrier for the chemotherapy of brain tumours, where it interferes with the cellular DNA of the highly dividing cells. Semustine, just as lomustine, is administered orally. It has been reported that semustine can perform the main mechanism of action at molecular level via the alkylation of DNA nitrogenous bases in duplex by results of inhibition of DNA replication, transcription, and translation by way of alkylation of DNA, under pH-dependent conditions by hydrolysis, forming chloro-carbonium ions. Sufficient evidence was found that treatment with semustine can cause acute leukaemia as a delayed effect in very rare cases. History During the past two decades, massive developments of various categories of anti-cancer drugs have been obs ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Carmustine
Carmustine, sold under the brand name BiCNU among others, is a medication used mainly for chemotherapy. It is a nitrogen mustard β-chloro- nitrosourea compound used as an alkylating agent. Description Carmustine is an orange-yellow solid medication used mainly for chemotherapy. It is a nitrogen mustard β-chloro- nitrosourea compound. Mechanism of action As an alkylating agent, carmustine can form interstrand crosslinks in DNA, which prevents DNA replication and DNA transcription. Uses Carmustine is used as an alkylating agent to treat several types of brain cancer including glioma, glioblastoma multiforme, medulloblastoma and astrocytoma), multiple myeloma, and lymphoma ( Hodgkin's and non-Hodgkin). Carmustine is sometimes used in conjunction with alkyl guanine transferase (AGT) inhibitors, such as ''O''6-benzylguanine. The AGT-inhibitors increase the efficacy of carmustine by inhibiting the direct reversal pathway of DNA repair, which will prevent formation of the inter ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alkylating Antineoplastic Agent
An alkylating antineoplastic agent is an alkylating agent used in cancer treatment that attaches an alkyl group (CnH2n+1) to DNA. The alkyl group is attached to the guanine base of DNA, at the number 7 nitrogen atom of the purine ring. Since cancer cells, in general, proliferate faster and with less error-correcting than healthy cells, cancer cells are more sensitive to DNA damage—such as being alkylated. Alkylating agents are used to treat several cancers. However, they are also toxic to normal cells ( cytotoxic), particularly cells that divide frequently, such as those in the gastrointestinal tract, bone marrow, testicles and ovaries, which can cause loss of fertility. Most of the alkylating agents are also carcinogenic. History Before their use in chemotherapy, alkylating agents were better known for their use as sulfur mustard, ("mustard gas") and related chemical weapons in World War I. The nitrogen mustards were the first alkylating agents used medically, as well ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
IARC Group 2A Carcinogens
The agents in this list have been classified in group 2A (probable carcinogens) by the International Agency for Research on Cancer (IARC). The term "agent" encompasses both substances and exposure circumstances that pose a risk. This designation is applied when there is ''limited evidence'' of carcinogenicity in humans as well as ''sufficient evidence'' of carcinogenicity in experimental animals. In some cases, an agent may be classified in this group when there is ''inadequate evidence'' of carcinogenicity in humans along with ''sufficient evidence'' of carcinogenicity in experimental animals and ''strong evidence'' that the carcinogenesis is mediated by a mechanism that also operates in humans. Exceptionally, an agent may be classified in this group solely on the basis of ''limited evidence'' of carcinogenicity in humans. Agents Substances *Acrylamide * Adriamycin * Androgenic (anabolic) steroids * Azacitidine *BCNU (Bischloroethyl nitrosourea) *Captafol * Chloral *Chloral hyd ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cell-cycle Nonspecific Antineoplastic Agents
Cell-cycle nonspecific antineoplastic agents (CCNS) refer to a class of pharmaceuticals that act as antitumor agents at all or any phases of the cell cycle. Alkylating antineoplastic agent An alkylating antineoplastic agent is an alkylating agent used in cancer treatment that attaches an alkyl group (CnH2n+1) to DNA. The alkyl group is attached to the guanine base of DNA, at the number 7 nitrogen atom of the purine ring. Since ... and anthracyclins are two examples. References Further reading * * {{Intracellular chemotherapeutic agents Antineoplastic drugs ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cancer Treatments
Cancer can be treated by surgery, chemotherapy, radiation therapy, hormonal therapy, targeted therapy (including immunotherapy such as monoclonal antibody therapy) and synthetic lethality, most commonly as a series of separate treatments (e.g. chemotherapy before surgery). The choice of therapy depends upon the location and grade of the tumor and the stage of the disease, as well as the general state of the patient ( performance status). Cancer genome sequencing helps in determining which cancer the patient exactly has for determining the best therapy for the cancer. A number of experimental cancer treatments are also under development. Under current estimates, two in five people will have cancer at some point in their lifetime. Complete removal of the cancer without damage to the rest of the body (that is, achieving cure with near-zero adverse effects) is the ideal, if rarely achieved, goal of treatment and is often the goal in practice. Sometimes this can be accomplished ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Organochlorides
An organochloride, organochlorine compound, chlorocarbon, or chlorinated hydrocarbon is an organic compound containing at least one covalently bonded atom of chlorine. The chloroalkane class (alkanes with one or more hydrogens substituted by chlorine) provides common examples. The wide structural variety and divergent chemical properties of organochlorides lead to a broad range of names, applications, and properties. Organochlorine compounds have wide use in many applications, though some are of profound environmental concern, with TCDD being one of the most notorious. Physical and chemical properties Chlorination modifies the physical properties of hydrocarbons in several ways. These compounds are typically denser than water due to the higher atomic weight of chlorine versus hydrogen. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage. Natural occurrence Many organochlorine compounds have been iso ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nitrosamines
In organic chemistry, nitrosamines (or more formally ''N''-Nitrosamines) are organic compounds with the chemical structure , where R is usually an alkyl group. They feature a nitroso group () bonded to a deprotonated amine. Most nitrosamines are carcinogenic in nonhuman animals. A 2006 systematic review supports a "positive association between nitrite and nitrosamine intake and gastric cancer, between meat and processed meat intake and gastric cancer and oesophageal cancer, and between preserved fish, vegetable and smoked food intake and gastric cancer, but is not conclusive". Chemistry The organic chemistry of nitrosamines is well developed with regard to their syntheses, their structures, and their reactions. They usually are produced by the reaction of nitrous acid () and secondary amines. :HONO + R2NH -> R2N-NO + H2O The nitrous acid usually arises from protonation of a nitrite. This synthesis method is relevant to the generation of nitrosamines under some biological cond ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alkylating Antineoplastic Agents
Alkylation is the transfer of an alkyl group from one molecule to another. The alkyl group may be transferred as an alkyl carbocation, a free radical, a carbanion, or a carbene (or their equivalents). Alkylating agents are reagents for effecting alkylation. Alkyl groups can also be removed in a process known as dealkylation. Alkylating agents are often classified according to their nucleophilic or electrophilic character. In oil refining contexts, alkylation refers to a particular alkylation of isobutane with olefins. For upgrading of petroleum, alkylation produces a premium blending stock for gasoline. In medicine, alkylation of DNA is used in chemotherapy to damage the DNA of cancer cells. Alkylation is accomplished with the class of drugs called alkylating antineoplastic agents. Nucleophilic alkylating agents Nucleophilic alkylating agents deliver the equivalent of an alkyl anion (carbanion). The formal "alkyl anion" attacks an electrophile, forming a new covalent bond b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Food And Drug Administration
The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food safety, tobacco products, caffeine products, dietary supplements, Prescription drug, prescription and Over-the-counter drug, over-the-counter pharmaceutical drugs (medications), vaccines, biopharmaceuticals, blood transfusions, medical devices, electromagnetic radiation emitting devices (ERED), cosmetics, Animal feed, animal foods & feed and Veterinary medicine, veterinary products. The FDA's primary focus is enforcement of the Federal Food, Drug, and Cosmetic Act (FD&C), but the agency also enforces other laws, notably Section 361 of the Public Health Service Act, as well as associated regulations. Much of this regulatory-enforcement work is not d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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