• Busulfan is an example of a dialkylating agent: it is the methanesulfonate diester of 1,4-butanediol. (wikipedia.org)
  • Because of this, many centers have used conditioning with alkylating agents including busulfan or melphalan known to open marrow niches in attempts to achieve B cell reconstitution. (duke.edu)
  • Melphalan should be administered under the supervision of a qualified physician experienced in the use of cancer chemotherapeutic agents. (nih.gov)
  • Chemotherapy (often abbreviated to chemo and sometimes CTX or CTx ) is a type of cancer treatment that uses one or more anti-cancer drugs (chemotherapeutic agents or alkylating agents) as part of a standardized chemotherapy regimen. (worldsbest.rehab)
  • Traditional chemotherapeutic agents are cytotoxic by means of interfering with cell division (mitosis) but cancer cells vary widely in their susceptibility to these agents. (worldsbest.rehab)
  • 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 remainder of this review will focus on the different chemotherapeutic agents currently being used for the treatment of cancer and their mechanism of action. (savedelicious.com)
  • Toxicity of Anticancer Drugs The therapeutic index for cancer chemotherapeutic agents is usually low and the cells of the bone marrow and the gastrointestinal tract are usually the most sensitive normal cells. (present5.com)
  • Like other bifunctional alkylating agents, it is active against both resting and rapidly dividing tumor cells. (nih.gov)
  • There have been significant advancements in the development of new drugs for multiple myeloma in recent years, including immunomodulatory drugs and monoclonal antibodies, which are driving growth in the market. (insights10.com)
  • Combination therapies, which involve the use of multiple drugs to treat multiple myeloma, have become increasingly common in Germany, as they have been shown to be more effective than single-agent therapies. (insights10.com)
  • The German healthcare system provides favorable reimbursement policies for cancer treatments, including multiple myeloma therapeutics, which is helping to drive growth in the market. (insights10.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)
  • 2. Cancer Treatment: Multiple myeloma and ovarian cancer are two cancers that Melphalan Tablets are especially advised to treat. (veapharma.com)
  • 1. Effective Cancer Management: Melphalan has shown effectiveness in the treatment of multiple myeloma and ovarian cancer, perhaps providing advantages and better results for people with these particular cancers. (veapharma.com)
  • 8. Potential for Disease Control: Patients with ovarian cancer and multiple myeloma may see increased survival rates and disease control after receiving melphalan treatment. (veapharma.com)
  • 1. Melphalan is frequently employed in the management of multiple myeloma, a bone marrow-based malignancy that affects plasma cells. (veapharma.com)
  • Melphalan is a prescription medication used to treat multiple myeloma (a type of cancer of the bone marrow). (rxwiki.com)
  • A dose-escalation study of single-agent bendamustine up to 100 mg/m 2 showed an overall response rate (ORR) of 55%, including minor responses (MRs). 3 Pönisch et al performed a phase 1 clinical trial testing the combination of bendamustine, prednisolone, and thalidomide for relapsed or refractory multiple myeloma. (ashpublications.org)
  • 18 F-FDOPA PET/CT complemented 18 F-FDG PET/CT in imaging melphalan therapy response in preclinical extramedullary MM. 18 F-FDOPA uptake was linked to LAT1 expression and melphalan response, with longitudinal imaging suggesting stabilization of LAT1 levels and melphalan tumor cytotoxicity. (snmjournals.org)
  • In preclinical models of MM, synergy was observed in anti-tumor activity when poly (ADPribose) polymerase (PARP) inhibitors (olaparib, talazoparib) were used in combination with melphalan. (haematologica.org)
  • Such activity would result in increased cell death of tumor tissue where PKB is elevated, and in decreased resistance to chemotherapy agents. (justia.com)
  • Adverse prognostic or predictive factors include detectable primary metastases, axial or proximal extremity tumor site, large tumor size, elevated serum alkaline phosphatase or lactate dehydrogenase levels, and older age. (medscape.com)
  • Melflufen A first in class peptide-drug conjugate that targets aminopeptidases and releases alkylating agents into tumor cells. (oncopeptides.de)
  • Bioreductive agents, such as Tirapazamine (TPZ), are preferentially cytotoxic in hypoxia and show activity against a variety of tumor cell lines ( 1 - 4 ). (aacrjournals.org)
  • The product is a first-in-class aminopeptidase-targeting peptide-drug conjugate that rapidly delivers an alkylating payload into tumor cells. (oncopeptides.com)
  • Alkylating agents are used to treat several cancers. (wikipedia.org)
  • While the incidence and mortality of all cancers combined is decreasing, specific cancers, including cancers among children, are on the rise. (healthandenvironment.org)
  • 14 Cancers increasing in the US include lung cancer (especially in women), melanoma, non-Hodgkin lymphoma and myeloma. (healthandenvironment.org)
  • The L-type amino acid transporter 1 (LAT1) is a key mediator in uptake and intracellular accumulation of melphalan and correlates with melphalan sensitivity and response in MM and other cancers ( 8 - 10 ). (snmjournals.org)
  • Pharmaceutical compositions that include these protein kinase inhibitors, and methods of using such compositions for treatment of cancers and other diseases associated with protein kinase activity are also disclosed. (justia.com)
  • Although melphalan is used to treat cancer , it may rarely increase your risk of developing other cancers. (webmd.com)
  • Melphalan Hydrochloride for Injection is supplied as a sterile, nonpyrogenic, white to off-white lyophilized cake or powder. (nih.gov)
  • Melphalan Hydrochloride for Injection is reconstituted using the sterile diluent provided. (nih.gov)
  • Melphalan Hydrochloride for Injection is administered intravenously. (nih.gov)
  • Do not mix Evomela with other melphalan hydrochloride for injection drug products. (nicerx.com)
  • 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)
  • In the Anatomical Therapeutic Chemical Classification System, alkylating agents are classified under L01A. (wikipedia.org)
  • 1 Despite significant therapeutic advances for MM, autologous stem cell transplant (ASCT) following high-dose, single-agent melphalan conditioning remains a cornerstone of therapy. (haematologica.org)
  • Suitability of an antigen for therapy is dependent on various factors including but not limited to the nature of the antigen (e.g. accessibility, abundance, location of expression on cancerous cells etc.), therapeutic approach, antibody affinity and other pharmacokinetic properties. (justia.com)
  • They transport therapeutic agents to the target cell/tissue. (mdpi.com)
  • This indicates the intricate control of metabolism and redox balance for survival of cancer cells that can be targeted by therapeutic agents. (degruyter.com)
  • EDO-S101 is a novel therapeutic agent conceived as the fusion of a histone deacetylase inhibitor radical to bendamustine, with the aim of potentiating its alkylating activity. (m2cobalt.com)
  • Therefore, a combination of bendamustine with a less hematotoxic agent such as bortezomib provides a very promising approach that will allow the administration of adequate therapeutic doses. (ashpublications.org)
  • The results from the HORIZON study demonstrates that melflufen in combination with dexamethasone, has a potential to provide a therapeutic option for patients with RRMM that are hard to treat and have a poor prognosis, including patients with triple class refractory myeloma and patients with extramedullary disease (EMD). (oncopeptides.com)
  • Sensitization of cancer cells to conventional drugs using multi-target agents that block survival and oncogenic pathways, alone or in combination, is an emerging strategy to overcome drug resistance. (researchsquare.com)
  • There are a number of cost containment measures in place in Germany, including reference pricing, which sets a maximum reimbursement price for drugs in a particular class, and rebates, which require drug manufacturers to pay a portion of their revenues back to health insurers. (insights10.com)
  • It can increase the anxiety and depression a person experiences, and it can interact with certain other drugs including chemotherapy. (worldsbest.rehab)
  • Melphalan belongs to a group of drugs called alkylating agents. (rxwiki.com)
  • As a result, there are numerous regimens that use two or more of these drugs available for the treatment of newly diagnosed and refractory/relapsed MM. The major classes include alkylating agents (melphalan andcyclophosphamide), corticosteroids (dexamethasone andprednisone), immunomodulatory drugs (thalidomide, lenalidomide, and pomalidomide), and proteasome inhibitors (bortezomib, carfilzomib, andixazomib) [ 1 ] . (encyclopedia.pub)
  • One type of alkylating agent -- platinum drugs like carboplatin , cisplatin , or oxaliplatin -- has a lower risk of causing leukemia. (webmd.com)
  • Conclusion These findings provide rationale for the clinical investigation of EDO-S101 in MM, either as a single agent or in combination with other anti-MM drugs, particularly proteasome inhibitors. (m2cobalt.com)
  • and miscellaneous agents, which include a number of recently developed drugs such as monoclonal antibodies. (savedelicious.com)
  • Compared with other frequently used alkylating agents, bendamustine induces higher rates of DNA double-strand breaks and is not cross-resistant with melphalan and several other cytotoxic drugs. (ashpublications.org)
  • The objectives in combination chemotherapy have been to limit the toxicity of individual agents and to evade drug resistance by exposing the cancer cell to drugs with different modes of action simultaneously. (present5.com)
  • Melphalan belongs to a class of drugs known as alkylating agents. (webmd.com)
  • Results EDO-S101 displayed potent activity in vitro in MM cell lines (IC50 1.6C4.8?M) and ex vivo in cells isolated from MM patients, which was higher than that of bendamustine and independent of the p53 status and previous melphalan resistance. (m2cobalt.com)
  • 4 Fixed doses of bendamustine (60 mg/m 2 ) and prednisolone (100 mg) with escalating doses of thalidomide (50, 100, and 200 mg) achieved a high response rate of 86%, including 14% complete responses. (ashpublications.org)
  • Ifosfamide must be given with the bladder-sparing agent Mesna, to avoid severe urothelial injury). (vin.com)
  • 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)
  • 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)
  • Combination therapies involving melphalan, a small-molecule DNA alkylating agent, are commonly prescribed to patients with relapsed or refractory MM, necessitating the stratification of responding patients to minimize toxicities and improve quality of life. (snmjournals.org)
  • Thus, stratification of melphalan-responsive patients in the MM patient population is critical for reducing therapy-induced toxicities. (snmjournals.org)
  • Hypersensitivity reactions, including anaphylaxis, have occurred in approximately 2% of patients who received the intravenous formulation. (nih.gov)
  • Mean (±SD) peak melphalan plasma concentrations in myeloma patients given intravenous melphalan at doses of 10 or 20 mg/m 2 were 1.2 ± 0.4 and 2.8 ± 1.9 mcg/mL, respectively. (nih.gov)
  • Although the contribution of renal elimination to melphalan clearance appears to be low, one study noted an increase in the occurrence of severe leukopenia in patients with elevated BUN after 10 weeks of therapy. (nih.gov)
  • Induced leukemia-differences in the ages of patients and differences in the accumulative doses of alkylating agents explain the wide variations in risk from study to study. (standardofcare.com)
  • The negative prognosis associated with PARP1 and POLD2 expression along with the apparent melphalan-sensitizing effect of PARP inhibition may suggest this pathway as a potential biomarker in patients with MM in the setting of ASCT. (haematologica.org)
  • METHODS: This retrospective longitudinal cohort study using IQVIA PharMetrics Plus adjudicated claims US data (January 1, 2015, to September 30, 2020) included adult patients with all available data who initiated IRd, VRd, or KRd in second line of therapy or later (LOT2+) on or after September 1, 2015. (bvsalud.org)
  • 4. Melphalan is a drug that can be used in palliative care to treat advanced cancer patients' symptoms of the disease and enhance their quality of life. (veapharma.com)
  • 5. Weakness and weariness are potential side effects of the treatment with Melphalan for patients. (veapharma.com)
  • Salvage therapy for patients with resistant disease or relapse includes reuse or alternative use of front-line agent, combination therapy, thalidomide (with or without steroids), autologous transplantation, and monoclonal antibody (alemtuzumab). (medscape.com)
  • 30% in patients with multiple previous lines of therapy, including those who do not respond to PIs, IMiDs, and mAbs. (encyclopedia.pub)
  • In patients with limited disease, radiotherapy (RT) including new techniques (eg, proton and carbon ion beam RT) should be considered, particularly for unresectable primary tumors. (medscape.com)
  • IWMF, volunteers from the IWMF Affiliates, and WM researchers develop publications including Booklets, Treatment Guides, and Facts Sheets to provide the newly diagnosed and veteran patients, as well as their caregivers, with up-to-date information about Waldenstrom's macroglobulinemia and how to treat it. (iwmf.com)
  • This booklet is designed to help patients with WM understand the basic functions of the bone marrow and how those are affected by our disease, including the bone marrow biopsy procedure and medical tests. (iwmf.com)
  • The patients were suffering with relapsed or refractory acute lymphoblastic leukaemia (ALL) (An additional 9 patients suffering with acute myelogenous leukaemia (AML) had similar pharmacokinetics but are not included in the figure below. (bionity.com)
  • While MDS are most commonly found in older patients (median age at diagnosis, 71 years), MDS can be diagnosed at any age, including childhood. (dermatologyadvisor.com)
  • National Comprehensive Cancer Network (NCCN) guidelines recommend that all patients younger than 40 years of age with abnormal radiographs be referred to an orthopedic oncologist for further workup that includes biopsy, which if indicated should be performed at the treating institution. (medscape.com)
  • Including only patients who received ≥2 cycles of therapy (71 patients), the ORR increased to 67.7% or 84.6% (with MRs). As expected, the response rates were lower in patients pretreated with bortezomib, lenalidomide, or both, in patients exposed to ≥2 prior lines of lenalidomide-based therapy, and in those with relapsed and/or refractory disease to the last treatment regimen. (ashpublications.org)
  • In the dexamethasone treatment group, the most commonly reported serious adverse reactions were pneumonia (4%), hyperglycemia (3%), pyrexia, and psychotic disorder (2% each).A total of 145 patients, including 84 (25%) of 331 patients in the bortezomib treatment group and 61 (18%) of 332 patients in the dexamethasone treatment group were discontinued from treatment due to adverse reactions. (drugcentral.org)
  • The HORIZON study population includes subgroups of patients who were triple ‑ class refractory and/or had extramedullary disease and/or had cytogenetic high ‑ risk features. (oncopeptides.com)
  • Alkylating agents and topoisomerase II inhibitors induce therapy related leukemia. (standardofcare.com)
  • Bortezomib is the first drug approved in the group of anticancer agents known as proteasome inhibitors. (medscape.com)
  • This Guide includes proteasome inhibitors, such as bortezomib (Velcade), carfilzomib (Kyprolis), and ixazomib (Ninlaro). (iwmf.com)
  • Differentiation agent: all-trans retinoic acid, HDAC inhibitors (Vorinostat) 11. (present5.com)
  • Agents that inhibit DNA repair: PARP inhibitors 15. (present5.com)
  • However, melphalan efficacy is variable in the clinical population, especially in relapsed and refractory MM, and is also implicated in various toxicities, including severe mucositis and myelosuppression. (snmjournals.org)
  • 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)
  • Controlled trials comparing intravenous (IV) to oral melphalan have shown more myelosuppression with the intravenous formulation. (nih.gov)
  • Melphalan produces chromosomal aberrations in vitro and in vivo and, therefore, should be considered potentially mutagenic in humans. (nih.gov)
  • The drug is now being studied in combination with other agents in both upfront and relapsed settings. (encyclopedia.pub)
  • Methods The efficacy of EDO-S101 was evaluated in vitroex vivo and in vivoalone, and in combination with standard anti-myeloma agents. (m2cobalt.com)
  • The risk of secondary leukemia is associated with the type of cytotoxic agents, cumulative dose, intensity of such agents and cumulative ionizing radiation doses. (standardofcare.com)
  • More than 85% of MDS cases are idiopathic or "de novo", while 10-15% are secondary to a recognized prior exposure to a DNA damaging agent such as alkylating agent / topoisomerase inhibitor chemotherapy, or ionizing radiation. (dermatologyadvisor.com)
  • In addition to the above immunotherapeutic agents, conjugation of cytotoxic agents with monoclonal antibodies is an evolving field with the development of multiple targeted cytotoxic agents called antibody-drug conjugates (ADC) [ 45 ]. (biomedcentral.com)
  • 4. Mucositis: Melphalan may result in ulcers and inflammation in the mouth and gastrointestinal tract. (veapharma.com)
  • Melphalan is a bifunctional alkylating agent that is active against selected human neoplastic diseases. (nih.gov)
  • They are bifunctional, which means they have two alkylating groups, and can cause intra- or inter-chain cross-linking between DNA strands. (savedelicious.com)
  • They may be related to traditional pharmaceutical agents, biologic agents and targeted immunotherapeutic agents, food additives, and dyes. (medscape.com)
  • Melphalan has demonstrated effectiveness in treating several particular malignancies, potentially providing advantages and bettering patient outcomes. (veapharma.com)
  • 4. Melphalan is occasionally used as part of conditioning regimens prior to stem cell transplantation in various malignancies. (veapharma.com)
  • It includes the treatment of blood disorders and malignancies, including hemophilia, leukemia, lymphoma and sickle-cell anemia. (oncopeptides.de)
  • During the seventies and eighties Peptichemio, a cocktail of six alkylating oligopeptides carrying m-L-sarcolysin, was investigated in a wide variety of human malignancies. (dissertations.se)
  • PKB has emerged as a crucial regulator of widely divergent cellular processes including apoptosis, proliferation, differentiation and metabolism. (justia.com)
  • Immunotherapeutic agents including antibodies and chimeric antigen receptor T cells are widely studied in clinical trials. (biomedcentral.com)
  • General staging should be carried out to assess the extent of distant disease, including bone scintigraphy, chest radiographs and computed tomography (CT), whole-body magnetic resonance imaging (MRI), and positron emission tomography (PET)-CT or PET-MRI. (medscape.com)
  • Serious side effects that can happen because of bone marrow suppression include severe infection ( sepsis ), bleeding, and anemia . (bionity.com)
  • The myelodysplastic syndromes (MDS) include a heterogeneous group of clonal bone marrow failure syndromes characterized by cytopenias, clonally restricted hematopoiesis (associated with an abnormal G-banded metaphase karyotype in about 50% of cases), genomic instability, and a risk of progression to acute myeloid leukemia (AML). (dermatologyadvisor.com)
  • Tell us about any medications that you are taking, including Evomela, your healthcare provider, your insurance plan, and your household income. (nicerx.com)
  • As an alkylating agent, the mechanism of action of the active metabolites may involve cross-linking of DNA, which may interfere with the growth of normal and neoplastic cells. (medscape.com)
  • Melphalan therapy induced a statistically significant reduction in lesion avidity and uptake for both 18 F-FDG and 18 F-FDOPA. (snmjournals.org)
  • Future work will explore additional MM cell lines with heterogeneous LAT1 expression and response to melphalan therapy. (snmjournals.org)
  • Therapy related leukemia this is complication of treatment that can develop months to years or even decades after exposure to cytotoxic agents or radiotherapy or both. (standardofcare.com)
  • 3. Melphalan may be used as an adjuvant therapy to assist lower the risk of cancer progression or recurrence following first therapy. (veapharma.com)
  • 7. Melphalan Tablets provide an outpatient therapy option in some circumstances, minimising the requirement for hospital stays and improving patient comfort. (veapharma.com)
  • The choice of chemotherapy depends on several factors, including the patient's performance status, age, renal function, desire for inpatient or outpatient therapy, and likelihood of receiving future autologous stem cell transplantation. (medscape.com)
  • Also, melphalan may cause a severe decrease in your blood cells , which lowers your ability to fight infections and increases the risk of anemia /bleeding problems. (webmd.com)
  • Renal & Urology News publishes timely news coverage of scientific developments of interest to nephrologists and urologists, including in-depth coverage of all relevant medical conferences. (renalandurologynews.com)
  • Oligopeptides can be used to carry cytotoxic agents in cancer chemotherapy, using tumour-associated proteins as the molecular target for selectivity. (dissertations.se)
  • One study has reported that on repeat dosing of 0.5 mg/kg every 6 weeks, the clearance of melphalan decreased from 8.1 mL/min/kg after the first course, to 5.5 mL/min/kg after the third course, but did not decrease appreciably after the third course. (nih.gov)
  • 6. Predictable Dosing: Melphalan is administered orally, which offers predictable dosing and promotes patient convenience and treatment adherence. (veapharma.com)
  • Mechanisms of action include intercalation of DNA and interference with topoisomerase enzyme function. (vin.com)
  • Arm 1: Oral melphalan 0.15 mg/kg/day x 7 followed by 0.05 mg/kg/day when WBC began to rise. (nih.gov)
  • These tumors of dogs and, rarely, cats are most frequently identified on the head (including ears, lips, and oral cavity) and extremities of mature adult to senior animals. (merckvetmanual.com)
  • An alkylating antineoplastic agent is an alkylating agent used in cancer treatment that attaches an alkyl group (CnH2n+1) to DNA. (wikipedia.org)
  • Related to alkylating agents typically develop 5-7 years after initial cancer treatment. (standardofcare.com)
  • The index date was the treatment initiation date for each LOT (multiple LOTs per patient were included) and the baseline was 6 months pre-index. (bvsalud.org)
  • 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)
  • 2. Vomiting and Nausea: Treatment with Melphalan frequently causes gastrointestinal adverse effects, such as nausea and vomiting. (veapharma.com)
  • 3. Hair Loss: Treatment with Melphalan may result in temporary hair loss or thinning (alopecia). (veapharma.com)
  • Its mechanism of action is complex and includes depolymerization of microtubules. (medscape.com)
  • These data further define the mechanism of action of TPZ and suggest that as a single agent, TPZ would only have clinical activity against p53-functional neuroblastomas. (aacrjournals.org)