• 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 as the first modern cancer chemotherapies. (wikipedia.org)
  • These publications spurred rapid advancement in the previously non-existent field of cancer chemotherapy, and a wealth of new alkylating agents with therapeutic effect were discovered over the following two decades. (wikipedia.org)
  • What is the best protocol of single-agent methotrexate chemotherapy in nonmetastatic or low-risk metastatic gestational trophoblastic tumors? (medscape.com)
  • Roberts JP, Lurain JR. Treatment of low-risk metastatic gestational trophoblastic tumors with single-agent chemotherapy. (medscape.com)
  • Relapse rate of patients with low-risk gestational trophoblastic tumor initially treated with single-agent chemotherapy. (medscape.com)
  • Is lack of response to single-agent chemotherapy in gestational trophoblastic disease associated with dose scheduling or chemotherapy resistance? (medscape.com)
  • Several alkylating agents are commonly used in chemotherapy but may induce DNA damage to cancer cells as well as normal cells. (frontiersin.org)
  • Fludara is a type of chemotherapy and is the first of a new class of drugs (purine analogs) active in the treatment of CLL. (broomeoncology.com)
  • The mainstay of treatment for indolent non-Hodgkin's lymphoma is an anti-CD20 antibody rituximab in combination with chemotherapy consisting of alkylating agents, anthracyclines, antimitotic agents, or purine analogues. (esmo.org)
  • Patients on treatment with rituximab (R) either alone or in combination with chemotherapy, including an alkylating agent (e.g. bendamustine [R-B] or cyclophosphamide, hydroxydoxorubicin, vincristine, prednisone [R-CHOP]) for relapsed indolent non-Hodgkin's lymphoma (iNHL). (who.int)
  • [ 2 ] Options for second-line therapy in patients with relapsed/refractory disease include chemotherapy-free regimens with biologic targeted agents such as covalent Bruton tyrosine kinase (BTK) inhibitors, lenalidomide,venetoclax, and chimeric antigen receptor (CAR) T-cell therapy. (medscape.com)
  • Melphalan should be administered under the supervision of a qualified physician experienced in the use of cancer chemotherapeutic agents. (nih.gov)
  • Melphalan is a bifunctional alkylating agent that is active against selected human neoplastic diseases. (nih.gov)
  • Melphalan is an alkylating agent of the bischloroethylamine type. (nih.gov)
  • Melphalan is an alkylating agent and a derivative of mechlorethamine that inhibits mitosis by cross-linking DNA strands. (medscape.com)
  • Melphalan, an alkylating agent used in the treatment of several cancers, especially multiple myeloma and ovarian cancer, is the active component of Melphalan Tablets. (veapharma.com)
  • 1. Melphalan, an alkylating agent with a reputation for being beneficial in the treatment of cancer, is the active ingredient in the pills. (veapharma.com)
  • 3. Melphalan is an alkylating agent that kills cancer cells by interfering with DNA synthesis and harming cancer cells. (veapharma.com)
  • It may also be called a nitrogen mustard derivative or a cytotoxic agent. (drugs.com)
  • Precursor of an alkylating nitrogen mustard antineoplastic and immunosuppressive agent that must be activated in the LIVER to form the active aldophosphamide. (nih.gov)
  • Sulfur mustard and nitrogen mustard alkylate many cellular components, including DNA, and also release inflammatory cytokines. (msdmanuals.com)
  • As alkylating agent, mechanism of action of active metabolites may involve cross-linking of DNA, which may interfere with growth of normal and neoplastic cells. (medscape.com)
  • Transformed primarily in the liver to active alkylating metabolites. (medscape.com)
  • Apaziquone is converted to active metabolites in hypoxic cells by intracellular reductases, which are present in greater amounts in hypoxic tumor cells. (medicalterminologydb.com)
  • The active metabolites alkylate DNA, resulting in apoptotic cell death. (medicalterminologydb.com)
  • Common among these 10 interactions of organic compounds, their power to detect excess cancer agents is the electrophilic nature of or their metabolites, with DNA and R 1 risk at particular sites. (who.int)
  • Gestational trophoblastic tumors are sensitive to many antineoplastic agents, especially those that act in the S phase or the M phase of the cell cycle. (medscape.com)
  • The most recent chemotherapeutic agent that has been approved for use in patients with rituximab-refractory indolent non-Hodgkin's lymphoma is the alkylating agent bendamustine, but it is not currative. (esmo.org)
  • Through this function as an alkylating agent, bendamustine causes intra- and inter-strand crosslinks between DNA bases resulting in cell death. (rassopharma.ch)
  • Active treatment with high-dose corticosteroids (i.e., ≥20mg prednisone or equivalent per day), alkylating agents, antimetabolites, transplant-related immunosuppressive drugs, cancer chemotherapeutic agents classified as severely immunosuppressive, tumor-necrosis (TNF) blockers, and other biologic agents that are immunosuppressive or immunomodulatory. (yatescounty.org)
  • Goodman, Gilman, and others began studying nitrogen mustards at Yale in 1942, and, following the sometimes dramatic but highly variable responses of experimental tumors in mice to treatment, these agents were first tested in humans late that year. (wikipedia.org)
  • the D-isomer, known as medphalan, is less active against certain animal tumors, and the dose needed to produce effects on chromosomes is larger than that required with the L-isomer. (nih.gov)
  • These drugs are cell cycle non-specific and work by damaging DNA Altretamine has been shown to work on tumors resistant to other alkylating agents. (oncology-drugs.net)
  • This agent displays activity towards both hypoxic solid tumors, which exhibits higher expression of cytochrome P450 reductase, and well-oxygenated malignant cells that overexpress the bioreductive enzyme NQO1 (NAD(P)H: quinone oxidoreductase). (medicalterminologydb.com)
  • These include true alkyl groups, and have been known for a longer time than some of the other alkylating agents. (wikipedia.org)
  • Alkylating agents may substitute alkyl groups for hydrogen atoms on DNA, resulting in the formation of cross links within the DNA chain and thereby resulting in cytotoxic, mutagenic, and carcinogenic effects. (aopwiki.org)
  • Chemotherapeutic agents, corticosteroids, and monoclonal antibodies are used to reduce the disease burden, and bisphosphonates are used to promote bone healing and to provide secondary prophylaxis against skeletal-related events (eg, hypercalcemia, bone fracture, spinal cord compression, need for radiation, and need for surgery). (medscape.com)
  • The extremely low 5-year overall survival of patients is, in part, due to pancreatic cancer cells having several mechanisms of resistance to different chemotherapeutic treatments, one of which is their capacity to efficiently repair alkylating agent-induced DNA damage. (frontiersin.org)
  • a class of chemotherapeutic agents which reversibly inhibit glutathione reductase. (mysite.com)
  • The overall response rate was impressive 57%, with a median progression-free survival of 11 months, values suggesting that the efficacy of idelalisib is similar or superior to those of other active treatment options in relapsed or refractory indolent non-Hodgkin's lymphoma. (esmo.org)
  • They are chemically active substances that provide the therapeutic effect of a medication. (getonlinemedicine.com)
  • A cell cycle goes through three phases: resting, active growing, and mitosis (division). (drugs.com)
  • To improve tumor cells selectivity and/or photodynamic therapy (PDT) anti-tumor efficiency, active molecules (peptides, pseudopeptides, alkylating agents) have been conjugated to the photo-activable molecule. (univ-lorraine.fr)
  • Alkylating agents are highly reactive chemicals that introduce alkyl radicals into biologically active molecules and thereby prevent their proper functioning. (aopwiki.org)
  • It is active against both active and quiescent cells, although the exact mechanism of action is unknown. (rassopharma.ch)
  • Dialkylating agents can react with two different 7-N-guanine residues, and, if these are in different strands of DNA, the result is cross-linkage of the DNA strands, which prevents uncoiling of the DNA double helix. (wikipedia.org)
  • Monoalkylating agents can react only with one 7-N of guanine. (wikipedia.org)
  • The protein methyl guanine methyl transferase (MGMT) can restore the original guanine by transferring the methylation product to its active site. (news-medical.net)
  • These agents also form covalent cross-links in DNA, more typically at the 0-6 position of guanine as the most important DNA adduct site, and have the primary adverse effects of myelosuppression and GI toxicity. (vin.com)
  • It may be nonspecific as in the administration of immunosuppressive agents (drugs or radiation) or by lymphocyte depletion or may be specific as in desensitization or the simultaneous administration of antigen and immunosuppressive drugs. (lookformedical.com)
  • Treosulfan is an alkylating agent that has centralized marketing authorization by the European Medicines Agency (EMA) for use in the European Union (EU) for the treatment of ovarian cancer. (affygility.com)
  • In the Anatomical Therapeutic Chemical Classification System, alkylating agents are classified under L01A. (wikipedia.org)
  • They transport therapeutic agents to the target cell/tissue. (mdpi.com)
  • They are the active components responsible for the intended therapeutic effect. (getonlinemedicine.com)
  • Examples: Bulk drugs encompass a wide range of active ingredients used in various therapeutic areas. (getonlinemedicine.com)
  • Alkylating agents are used to treat several cancers. (wikipedia.org)
  • Based on alkylating mechanisms, these agents can be divided as SN1 and SN2. (frontiersin.org)
  • Agents that suppress immune function by one of several mechanisms of action. (lookformedical.com)
  • Bulk drugs, also known as active pharmaceutical ingredients (APIs) or drug substances, are the key components used in the production of medicines. (getonlinemedicine.com)
  • Affygility Solutions has an occupational exposure limit (OEL) and control band assignment for this active pharmaceutical ingredient (API). (affygility.com)
  • WINVOL Injection contains the active ingredient stanozolol, which is a synthetic anabolic steroid. (getonlinemedicine.com)
  • The effects of alterations to key residues in the active site of AGT were studied using AGTs with point mutations. (psu.edu)
  • The complete inhibition of the enzyme by 2-nitro-5-thiocyanatobenzoate, 5,5'-dithio-bis(2-nitrobenzoic acid) and 1,2-benzisothiazolidine-3-one at nanomolar concentrations suggested that these sulphydryl alkylating agents modify functionally significant cysteine residues at or near the active site of the epimerase. (birmingham.ac.uk)
  • Most of the alkylating agents are also carcinogenic. (wikipedia.org)
  • Drinking-water, or water used for agricultural or recreational activities, can be polluted by naturally occurring carcinogenic contaminants, such as arsenic, or by anthropogenic pollutants, including chlorinated agents, perfluorinated alkylated substances, and metals. (who.int)
  • An alkylating antineoplastic agent is an alkylating agent used in cancer treatment that attaches an alkyl group (CnH2n+1) to DNA. (wikipedia.org)
  • 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. (wikipedia.org)
  • Carmustine, the active substance in this medicine, is a type of cancer medicine known as an alkylating agent. (europa.eu)
  • Studies on the benefits and risks of the active substance carmustine in the authorised uses as a cancer medicine have already been carried out with the reference medicine, Carmubris, and do not need to be repeated for Carmustine Obvius. (europa.eu)
  • Here, we tested whether ALKBH6 plays a significant role in preventing alkylating DNA damage and decreasing genomic instability in pancreatic cancer cells. (frontiersin.org)
  • In particular, the loss of ALKBH6 in human pancreatic cancer cells increases alkylating agent-induced DNA damage and significantly decreases cell survival. (frontiersin.org)
  • Several new agents have recently been approved or are soon to be approved by the FDA for the treatment of cancer. (worthingtoncaron.com)
  • [1] These agents are very interesting compounds, and further research is needed to determine their precise role in the treatment of cancer. (worthingtoncaron.com)
  • Therefore, we recommend that STZ, which is the only cytotoxic agent available against NET, should be used in daily practice in Japan. (cancerindex.org)
  • Bortezomib is the first drug approved in the group of anticancer agents known as proteasome inhibitors. (medscape.com)
  • The predominant regimen was the weekly/bi-weekly intravenous administration of STZ combined with other oral anticancer agents. (cancerindex.org)
  • Developing new chemistry or a new drug delivery system that would keep DFX active in hypoxic cells may be the next step toward their application. (biomedcentral.com)
  • This cytostatic effect demonstrates the dependency of proliferating cells on reducing agents, and thiols in particular. (mysite.com)
  • These results show that even slight alterations in the active site pocket of AGT that do not prevent its ability to protect cells from alkylating agents can block the paradoxical enhancement of the genotoxicity of the larger α,ω-dihaloalkanes by reducing the reaction with Cys 145 . (psu.edu)
  • Along with ibrutinib, which targets Bruton's tyrosine kinase (BTK), idelalisib represents a new class of agents that target signal transduction downstream of the B-cell receptor (BCR) in malignant B cells. (esmo.org)
  • Used both as single agent and in multiagent regimens for the treatment of malignant GTN. (medscape.com)
  • Use as single agent or as part of multiagent regimen for treatment of malignant GTN. (medscape.com)
  • For use a conditioning treatment, for which Carmubris is not authorised, the Agency noted that the active substance in Carmustine Obvius has been used for decades as a part of different conditioning regimens, and that its effectiveness has been established. (europa.eu)
  • Using an E. coli strain deficient with ALKB, we found that ALKBH6 complements ALKB deficiency and increases resistance after alkylating agent treatment. (frontiersin.org)
  • Treatment generally consists of surgical resection when possible, followed by a combination of external beam radiotherapy with concomitant administration of the orally active alkylating agent temozolomide (TMZ). (biomedcentral.com)
  • Tenvir EM Tablets is indicated in combination with other antiretroviral agents (such as non-nucleoside reverse transcriptase inhibitors or protease inhibitors) for the treatment of HIV-1 infection in adults. (itradeeximm.com)
  • Leukeran, an oral alkylating agent, was the primary initial treatment of for CLL for 40 years, before the development of newer agents such as Fludara and Rituxan. (broomeoncology.com)
  • This drug, has in general, been replaced with newer agents for initial treatment but many patients will receive this drug during some course of their palliative therapy. (broomeoncology.com)
  • The primary strategy for preventing and controlling TB in the United States is to minimize the risk for transmission by the early identification and treatment of patients who have active infectious TB. (cdc.gov)
  • these also are the typical signs and symptoms of exposure to type 1 pulmonary agents and, like skin injuries, occur after a latent period that is inversely correlated with dose but is usually at least a few hours. (msdmanuals.com)
  • Women of childbearing potential and men must agree to use effective contraception when sexually active due to potential embryo-fetal toxicity for 1 month after the last dose. (who.int)
  • Radioimmunotherapies can be active, but owing to the potential for haematologic toxic effects, their use has been limited to patients with adequate marrow function and limited marrow involvement by tumour. (esmo.org)
  • In several instances, tumour sites cytotoxic agents. (who.int)
  • Blister fluid does not contain active sulfur mustard. (msdmanuals.com)
  • In this chapter, electrophilic agents nogenicity from studies of exposed (benzene, 1,3-butadiene, and eth- include direct-acting electrophilic humans. (who.int)
  • All of the chemicals discussed of this chemical was raised to carci- lung and the nasal cavity were iden- here are IARC Group 1 agents and nogenic to humans (Group 1) based tified as target organs in humans as such can be characterized as on strong mechanistic evidence and rats, respectively. (who.int)
  • or each of these agents, carcinogenicity in rats and/or mice, els, differences in exposure con- there was sufficient evidence of car- for example for the liver (aflatoxins, ditions between studies in animals cinogenicity from studies in rats and/ trichloroethylene [TCE], and vinyl and in humans, or limitations in Part 1 · Chapter 1. (who.int)
  • The newest agent in this class to be used in veterinary medicine is the fluorinated cytidine analog gemcitabine. (vin.com)
  • The use of the newer agents in the taxane class (paclitaxel and docetaxel) is being explored in veterinary medicine as these agents are highly effective in human medicine. (vin.com)
  • Overview of Chemical-Warfare Agents Chemical-warfare (CW) agents are chemical mass-casualty weapons (MCWs) developed by governments for wartime use and include Toxic agents (intended to cause serious injury or death) Incapacitating. (msdmanuals.com)
  • It is used as an antineoplastic agent and to induce diabetes in experimental animals. (cancerindex.org)
  • However, Rituxan is more commonly used in combination therapy than as single agent therapy. (broomeoncology.com)
  • In the present study, the effect of sulphydryl alkylating agents on the in vitro activity of M. tuberculosis DapF was tested. (birmingham.ac.uk)
  • The second most important strategy is the identification of persons who have latent M. tuberculosis infection and, if indicated, the use of preventive therapy with isoniazid to prevent the latent infection from progressing to active TB disease. (cdc.gov)
  • This means that Carmustine Obvius contains the same active substance and works in the same way as a 'reference medicine' already authorised in the EU called Carmubris. (europa.eu)
  • There was no need for ' bioequivalence ' studies to investigate whether Carmustine Obvius is absorbed similarly to the reference medicine to produce the same level of the active substance in the blood. (europa.eu)
  • This is because Carmustine Obvius is given by infusion into a vein, so the active substance is delivered straight into the bloodstream. (europa.eu)
  • In a second part, we have studied the in vivo interest of coupling an alkylating agent with porphyrine and chlorine-type photosensitizers. (univ-lorraine.fr)
  • Un photosensibilisateur de type chlorine a été couplé à un peptide ligand de neuropiline-1 (NRP-1) et a montré son efficacité anti-tumorale in vitro et in vivo en PDT. (univ-lorraine.fr)
  • Dans une 2ème partie, nous avons appréhendé l'intérêt in vivo de coupler cet agent alkylant à des photosensibilisateurs de type porphyrine et chlorine. (univ-lorraine.fr)
  • Les études d'efficacité in vivo sur un modèle de souris nude xénogreffées en ectopique avec des cellules de carcinome oral humain KB, ont été menées par une méthodologie de plans d'expérience. (univ-lorraine.fr)
  • Treosulfan is a bifunctional alkylating agent with antineoplastic activity derived from its nonenzymatic conversion to epoxide compounds that react with nucleophilic centers of DNA. (affygility.com)
  • Single-agent therapy is given to palliate the disease (relieve symptoms) and improve the quality of life because toxicities are generally less severe than with combination therapy. (broomeoncology.com)
  • Ifosfamide must be given with the bladder-sparing agent Mesna, to avoid severe urothelial injury). (vin.com)
  • Because people with HIV-associated immunocompromise are at risk for severe manifestations of monkeypox, the HIV status of all sexually active adults and adolescents with suspected or confirmed monkeypox should be determined. (cdc.gov)
  • Its activity is induced by certain physiologic triggers which call for vasodilation, *NO being an agent of this signal. (mysite.com)
  • Because of the spontaneous hydrolysis of the compound, temozolamide has less variability in its conversion to MTIC than does dacarbazine, and therefore there are differences in activity, spectrum, and potency between the 2 agents. (worthingtoncaron.com)