- The Combined Anti-Tumor Efficacy of Bioactive Hydroxyapatite Nanoparticles Loaded with Altretamine. [Journal Article]
- In the current study, the combined anti-tumor efficacy of bioactive hydroxyapatite nano- particles (HA-NPs) loaded with altretamine (ALT) was evaluated. The well-known fact that HA has great biological compatibility was confirmed through the findings of the hemolytic experiments and a maximum IC50 value seen in the MTT testing. The preparation of HA-NPs was performed using the chemical precipitat…
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- Room-Temperature Dialkylamination of Chloroheteroarenes Using a Cu(II)/PTABS Catalytic System. [Journal Article]Chem Asian J. 2023 Jan 03; 18(1):e202201006.CA
- The dimethylamino functionality has significant importance in industrially relevant molecules and methodologies to install these efficiently are highly desirable. We report herein a highly efficient, room-temperature dimethylamination of chloroheteroarenes performed via the in-situ generation of dimethylamine using N,N-dimethylformamide (DMF) as precursor wiith a large substrate scope that includ…
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- Mode of interaction of altretamine with calf thymus DNA: biophysical insights. [Journal Article]J Biomol Struct Dyn. 2022 Mar 28 [Online ahead of print]JB
- Insights into drug-DNA interactions have importance in medicinal chemistry as it has a major role in the evolution of new therapeutic drugs. Therefore, binding studies of small molecules with DNA are of significant interest. Spectroscopy, coupled with measurements of viscosity and molecular docking studies were employed to obtain mechanistic insights into the binding of altretamine with calf thym…
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- The mechanisms and therapeutic targets of ferroptosis in cancer. [Journal Article]
- Ferroptosis, a form of programmed cell death, is mediated primarily by lipid peroxidation via a unique iron-dependent process. The mechanisms of ferroptosis involve the metabolisms of amino acids, irons, and lipids, and the regulation of antioxidant systems. Evidence supports the roles of ferroptosis in cancer, while metabolic reprogramming (a hallmark of cancer) renders tumor cells highly vulner…
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- Phytochemical, acute toxicity and renal protective appraisal of Ajuga parviflora hydromethanolic leaf extract against CCl4 induced renal injury in rats. [Journal Article]
- CONCLUSIONS: The restored urine and serum profile of various parameters to normal physiological levels suggests that the A. parviflora has potential antioxidant and repairing potential in renal disorders.
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- The effect of cation-π interactions on the stability and electronic properties of anticancer drug Altretamine: a theoretical study. [Journal Article]Acta Crystallogr C Struct Chem. 2020 10 01; 76(Pt 10):982-991.AC
- The present work utilizes density functional theory (DFT) calculations to study the influence of cation-π interactions on the electronic properties of the complexes formed by Altretamine [2,4,6-tris(dimethylamino)-1,3,5-triazine], an anticancer drug, with mono- and divalent (Li+, Na+, K+, Be2+, Mg2+ and Ca2+) metal cations. The structures were optimized with the M06-2X method and the 6-311++G(d,p…
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- Metabonomics analysis of Zi goose follicular granulosa cells using ENO1 gene expression interference. [Journal Article]
- The Zi goose is native to North-east China and is noted for its high egg production. Alpha enolase (ENO1) is a glycolytic enzyme which functions as a plasminogen receptor in follicular granulosa cells (FGCs), with several studies showing that FGCs can support follicular development. By transfecting the ENO1 interfering plasmid (shRNA) into FGCs, ENO1 expression in these cells was downregulated, s…
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- Anticancer altretamine recognition by bovine serum albumin and its role as inhibitor of fibril formation: Biophysical insights. [Journal Article]
- Binding of anticancer drug altretamine with bovine serum albumin (BSA) and its inhibitory effect on fibrillation of the protein has been studied by using a combination of spectroscopic and calorimetric methods. Altretamine is observed to bind with BSA with a moderate binding affinity of the order of 105, which is weakly temperature dependent. Circular dichroism, fluorescence spectroscopic and dyn…
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- The human gut chemical landscape predicts microbe-mediated biotransformation of foods and drugs. [Journal Article]
- Microbes are nature's chemists, capable of producing and metabolizing a diverse array of compounds. In the human gut, microbial biochemistry can be beneficial, for example vitamin production and complex carbohydrate breakdown; or detrimental, such as the reactivation of an inactive drug metabolite leading to patient toxicity. Identifying clinically relevant microbiome metabolism requires linking …
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- Pharmacokinetic study of solid-lipid-nanoparticles of altretamine complexed epichlorohydrin-β-cyclodextrin for enhanced solubility and oral bioavailability. [Journal Article]
- Altretamine is a synthetic drug approved for treatment of ovarian cancer. The only drawback with its formulation is poor aqueous solubility and low oral bioavailability. In the present work an attempt has been made to prepare inclusion complex of altretamine with epichlorohydrin beta cyclodextrin. The complexes were prepared by kneading, co-evaporation and freeze-drying method and were confirmed …
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- LiverTox: Clinical and Research Information on Drug-Induced Liver Injury: Altretamine [BOOK]LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. National Institute of Diabetes and Digestive and Kidney Diseases: Bethesda (MD)BOOK
- Altretamine is an orally administered alkylating agent, formerly known as hexamethylmelamine, which is currently used as a secondary therapy for advanced ovarian carcinoma. Altretamine therapy has been associated with low rates of serum enzyme elevations during therapy and with rare instances of acute, clinically apparent injury.
- Elucidating Compound Mechanism of Action by Network Perturbation Analysis. [Journal Article]
- Genome-wide identification of the mechanism of action (MoA) of small-molecule compounds characterizing their targets, effectors, and activity modulators represents a highly relevant yet elusive goal, with critical implications for assessment of compound efficacy and toxicity. Current approaches are labor intensive and mostly limited to elucidating high-affinity binding target proteins. We introdu…
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- Preparation, characterization, and optimization of altretamine-loaded solid lipid nanoparticles using Box-Behnken design and response surface methodology. [Journal Article]
- The objective of the present study was to prepare solid lipid nanoparticles (SLNs) of altretamine (ALT) by the hot homogenization and ultrasonication method. The study was conducted using the Box-Behnken design (BBD), with a 3(3) design and a total of 17 experimental runs, performed in combination with response surface methodology (RSM). The SLNs were evaluated for mean particle size, entrapment …
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- Liposomes incorporating sodium deoxycholate for hexamethylmelamine (HMM) oral delivery: development, characterization, and in vivo evaluation. [Journal Article]
- Liposomes incorporating sodium deoxycholate (NaDC) were prepared by the method of reverse phase evaporation and used for drug delivery by the oral route. Hexamethylmelamine (HMM), an anti-tumor agent, was chosen as a model drug and encapsulated into liposomes incorporating NaDC (NaDC-Lip). Several properties of NaDC-Lip containing HMM (HMM NaDC-Lip), such as particle size, entrapment efficiency, …
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- Hexamethylmelamine as consolidation treatment for patients with advanced epithelial ovarian cancer in complete response after first-line chemotherapy. [Journal Article]
- The aim of this study was to assess the efficacy of consolidation therapy with hexamethylmelamine (HMM) in patients with advanced epithelial ovarian cancer (EOC). Patients treated at our hospital between January 1997 and November 2006 and in documented clinical complete response from advanced ovarian cancer following front-line platinum-based therapy were retrospectively analyzed. The patients tr…
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- Relationship between frailty and cognitive decline in older Mexican Americans. [Journal Article]
- CONCLUSIONS: Frail status in older Mexican Americans with MMSE scores of 21 or higher at baseline is an independent predictor of MMSE score decline over a 10-year period. Future research is needed to establish pathophysiological components that can clarify the relationship between frailty and cognitive decline.
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- Atom efficient cyclotrimerization of dimethylcyanamide catalyzed by aluminium amide: a combined experimental and theoretical investigation. [Journal Article]
- A novel method for the cyclotrimerization of dimethylcyanamide to form hexamethylmelamine has been developed using an aluminium amide catalyst; detailed DFT modelling of the catalytic cycle supports a triple insertion, nucleophilic ring closure, deinsertion mechanism.
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- Lessons from a time capsule: evolution, not revolution, in therapy for advanced non-small-cell lung cancer. [Comment]
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- Synergy of irofulven in combination with other DNA damaging agents: synergistic interaction with altretamine, alkylating, and platinum-derived agents in the MV522 lung tumor model. [Journal Article]
- CONCLUSIONS: These results indicate that the antitumor activity of irofulven is enhanced when combined with platinum-derived agents, altretamine, and select alkylating agents such as melphalan or chlorambucil. A common factor between these agents appears to be the production of intrastrand DNA crosslinks. The synergistic interaction between irofulven and other agents may stem from the nucleotide excision repair system being selectively overwhelmed at two distinct points in the pathway, resulting in prolonged stalling of transcription forks, and subsequent initiation of apoptosis.
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- Pretreatment CA-125 and risk of relapse in advanced ovarian cancer. [Journal Article]
- CONCLUSIONS: The baseline CA-125 level before initiation of maintenance chemotherapy strongly predicts the risk of subsequent relapse. Patients with premaintenance baseline CA-125 values < or = 10 u/mL have a superior PFS compared with higher levels in the normal CA-125 range.
- Topotecan: weighing in when there are many options. [Comment]
- The manuscript by Armstrong et al. in this issue of The Oncologist, reviewing the toxicity and efficacy of full-dose topotecan delivered as second-line therapy in individuals with small cell lung cancer or ovarian cancer, will likely serve as both the most comprehensive and the final review of this active agent delivered at the U.S. Food and Drug Administration-approved dosage and schedule. The r…
- Better treatments improve survival of CHD patients. [Review]Nurse Pract. 2005 Sep; 30(9):57-63.NP
- Recurrent ovarian cancer: how important is it to treat to disease progression? [Review]
- Ovarian cancer is increasingly recognized as a chronic disease whose treatment is often characterized by administration of multiple, sequential active agents, each of which may or may not be accompanied by a tumor response. Despite the large proportion of patients who relapse and undergo longer-term treatment, the question of optimal treatment duration has not been fully addressed to date. For pa…
- Long-term follow-up of a phase II trial of oral altretamine for consolidation of clinical complete remission in women with stage III epithelial ovarian cancer in the Southwest Oncology Group. [Multicenter Study]
- CONCLUSIONS: Consolidation therapy with oral altretamine was generally well tolerated and associated with prolonged progression-free and overall survival in the Phase II setting.
- Oral altretamine used as salvage therapy in recurrent ovarian cancer. [Case Reports]
- CONCLUSIONS: Outpatient-administered oral altretamine can provide a prolonged disease-free interval with minimal toxicity.
- Medication sheets for patients. Oral chemotherapy. [Patient Education Handout]Clin J Oncol Nurs. 2003 Nov-Dec; 7(6 Suppl):40-72.CJ
- Comparative study on three chemotherapeutic regimens for the treatment of advanced epithelial ovarian cancer. [Journal Article]
- To investigate the best first-line chemotherapy regimen for the treatment of advanced epithelial ovarian cancer (AEOC), the efficacy of three chemotherapy regimens for treatment of the patients with AEOC in our hospital during Jan. 1992-Jan. 1999 was retrospectively analyzed. The therapeutic effects were compared with the supplement of Melphalan + Hexamethylme (PAM + HMM), cisplatin + adriamycin …
- Altretamine (hexamethylmelamine) in the treatment of platinum-resistant ovarian cancer: a phase II study. [Clinical Trial, Phase II]
- CONCLUSIONS: Altretamine should not be chosen as standard treatment in patients with platinum-resistant recurrent ovarian cancer. However, Altretamine represents a useful alternative in patients who prefer oral treatment or when socioeconomic considerations are an important issue.
- Part II: chemotherapy for epithelial ovarian cancer-treatment of recurrent disease. [Review]
- For women with advanced ovarian cancer, rates of response to first-line chemotherapy are high but most patients have relapses and become candidates for further chemotherapy. Chemotherapy for recurrence can palliate symptoms, and there is some evidence that it can also improve survival in this clinical situation. Patients who relapse quickly after first-line therapy should not be given the same dr…
- Solvent, emulsifier and drug concentration factors in poly(D,L-lactic acid) microspheres containing hexamethylmelamine. [Journal Article]
- Biodegradable poly(D,L-lactic acid) (PLA) microspheres containing hexamethylmelamine (HMM) were developed for potential use in chemoembolization and intraperitoneal implantation. The emulsion-solvent-evaporation/extraction method was used to prepare 15 formulations with different drug/polymer ratios, solvent compositions and emulsifer concentrations in the continuous aqueous phase. A central comp…
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