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Chemical Compound Review

Aliette     aluminum(+3) cation; ethoxy-oxido-oxo...

Synonyms: Phosethyl, Valiant, Rhodax, Mikal, Epal, ...
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Disease relevance of Efosite-Al

  • PURPOSE: Because docetaxel (Taxotere, RP 56976; Rhone-Poulenc Rorer, Antony, France) appeared to be active against breast cancer in phase I trials, we performed this phase II study [1].
  • PURPOSE: We conducted a phase II study to determine the response and toxicity of docetaxel (Taxotere; Rhône-Poulenc Rorer Pharmaceuticals, Inc, Collegeville, PA) in chemotherapy-naive patients with advanced non-small-cell lung cancer [2].
  • PURPOSE: We conducted a phase II study to determine the response to and toxicity of docetaxel (Taxotere; Rhône-Poulenc Rorer Pharmaceuticals, Inc, Collegeville, PA) in patients with advanced non-small-cell lung cancer refractory to prior platinum-containing chemotherapy (PCC) regimens [3].
  • PURPOSE: We conducted a phase II study designed to evaluate the activity, safety, and tolerability of docetaxel (Taxotere: Rhône-Poulenc Rorer Pharmaceuticals Inc, Collegeville, PA) in patients with advanced, incurable, or recurrent squamous cell carcinoma of the head and neck (SCCHN) who had not received prior palliative chemotherapy [4].
  • [1(S)-Aminoethyl][(2RS)2-carboxy-1-octyl]phosphinic acid (I), previously shown to bind tightly to Enterococcus faecalis and Salmonella typhimurium D-alanine:D-alanine ligases following phosphorylation Parsons, Patchett, Bull, Schoen, Taub, Davidson, Combs, Springer, Gadebusch, Weissberger, Valiant, Mellin & Busch (1988) J [5].

High impact information on Efosite-Al


Chemical compound and disease context of Efosite-Al

  • In patients with advanced cancers, gemcitabine and docetaxel (Taxotere; Rhône-Poulenc Rorer, Antony, France) can be administered together at 80% to 100% of their single-agent doses on days 1 and 8 of an every-3-week cycle without undue toxicity [11].
  • Several groups have reported significant efficacy and minimal toxicity in patients with hormone-refractory disease receiving estramustine plus docetaxel (Taxotere; Rhône-Poulenc Rorer, Collegeville, PA) [12].
  • In a prospective multicenter trial, 279 patients with metastatic colorectal cancer who had failed 5-fluorouracil therapy were randomized 2:1 to receive either best supportive care (BSC) plus treatment with the topoisomerase I inhibitor, irinotecan (CPT-11; Rhône-Poulenc Rorer, Antony, France), at a dose of 350 mg/m2 every 3 weeks or BSC alone [13].
  • A low dose (1.25 mg) of indapamide (Lozol, Rhône-Poulenc Rorer Pharmaceuticals, Collegeville, PA) was evaluated in 222 elderly patients (> or = 50 years) with mild to moderate essential hypertension in a multicenter, randomized, double-blind, parallel-group clinical trial [14].
  • A double-blind safety and efficacy dose-ranging study was conducted with a new, once-daily, extended-release (XR) diltiazem hydrochloride formulation (Dilacor XR, Rhône-Poulenc Rorer, Collegeville, PA) in 189 patients with chronic stable angina pectoris [15].

Biological context of Efosite-Al

  • Docetaxel (Taxotere; Rhône-Poulenc Rorer, Antony, France) is a hemisynthetic derivative from European yew that inhibits tubulin depolymerization and enhances the formation of microtubule bundle aggregates, causing cell death [16].
  • Occupational exposure to fosetyl-Al fungicide during spraying of ornamentals in greenhouses [17].
  • A kinetic study of the chemical hydrolysis of isoxaflutole [5-cyclopropyl-4-(2-methanesulfonyl-4-trifluoromethylbenzoyl)is oxazol e (IFT)], a new herbicide recently developed by Rhône-Poulenc Agro, in buffered, sterile aqueous solutions was carried out in the dark at 295, 308, and 323 K and at nine pH values between 1.8 and 10 [18].
  • Our early experience of using Valiant in 28 patients with a range of pathologies is described [19].
  • Seattle Genetics is developing SGN-10 (BR96-SCIT), a single-chain immunotoxin (SCIT) under license from Bristol-Myers Squibb (BMS), as both a monotherapy and in combination with Taxotere (Rhône-Poulenc Rorer) for the potential treatment for cancer [308773] [20].

Anatomical context of Efosite-Al

  • Docetaxel (Taxotere; Rhône-Poulenc Rorer, Antony, France) is a semisynthetic taxoid that is an inhibitor of microtubule depolymerization [21].
  • In each group, the flat dentin surface was treated with the assigned adhesive cement with a Teflon mold, followed by condensation of amalgam (Valiant PhD) onto it [22].
  • These results suggest a metabolic activation of peroxidase isoenzyme B5 as a consequence of fosetyl-A1 treatment, probably due to an acidification of the vacuole [23].
  • An in-vitro study of marginal leakage around class V restorations, prepared in freshly extracted upper central incisors, tested two types of high copper amalgam: spherical high copper amalgam (Tytin) and spherical high copper amalgam containing palladium (Valiant) [24].

Associations of Efosite-Al with other chemical compounds

  • Patients received estramustine phosphate 280 mg orally every 6 hours for a total of five doses (24-hour exposure), docetaxel (Taxotere; Rhône-Poulenc Rorer, Collegeville, PA) 70 mg/m2 intravenously over 1 hour, coumadin 2 mg orally every day, and dexamethasone as premedication for docetaxel [25].
  • The levels of phosphorous acid residues in apples after foliar fertilization with P fertilizers and after treatment with a phosphonate fungicide (Fosetyl-Al) were determined and compared [26].
  • Ground occlusal dentin surfaces of 140 formaldehyde-treated human molars were used to study shear strengths of different adhesive bonds (40: Syntac/Variolink, 40: Amalgambond Plus (AP), 40: AP+microfibre, and 20: Amalcoden) to a spherical high-copper amalgam (Valiant, Ivoclar NA) [27].
  • Wear ranking from the least to the most volumetric wear was as follows: high copper unicompositional alloy, Tytin (T) < high copper admixed alloy, Valiant PhD (V) < microfilled composite resin, Silux Plus (S) < gallium alloy, Galloy (G) < heavily filled composite resin, Z100 (Z) < hybrid composite resin, P50 (P) [28].
  • RESULTS: Fracture toughness values obtained were as follows: Fluorocore (composite resin; Caulk, Milford, DE), 1.54 MN.m-1.5; Ti-Core (composite resin and titanium; Essential Dental Systems, New York, NY), 1.34 MN.m-1.5; Valiant Ph.D. (amalgam; Caulk), 1.29 MN.m-1.5; and Coreshade Glass Ionomer Base Cement (Shofu Inc, Kyota, Japan), 0.55 MN.m-1 [29].

Gene context of Efosite-Al

  • This impact has perhaps been greatest for treatment of severe chronic neutropenia (SCN) conditions for which there were no predictably effective treatment before the availability of these growth factors, particularly r-metHuG-CSF (Filgrastim, Amgen Inc, Thousand Oaks, CA; or Lenograstim, Rhone-Poulenc Rorer, Milan, Italy) [30].
  • Impact and sliding wear were simulated on the machine, with water as the lubricant, on three metal alloys (Tytin, Valiant Ph.D., Galloy) and three composite resins (Silux Plus, Z100, P50) [31].
  • Microbial HTS has been implemented at Rhône-Poulenc Rorer through the development of a dedicated robotic platform [32].
  • The three disposables considered here (Gambro Lundia Nova, Cordis HFAK 4 and Rhone Poulenc RP 5) all have clearance of small molecules close to or, for the HFAK 4, just above that of the multipoint though their middle molecular clearance is not quite as good as the multipoint [33].
  • MATERIALS AND METHODS: Inlay composites (EOS) were bonded with two different bonding systems (Geristore, All-Bond 2) to high- or low-copper amalgams (Valiant, Agestan) [34].

Analytical, diagnostic and therapeutic context of Efosite-Al


  1. Phase II and pharmacologic study of docetaxel as initial chemotherapy for metastatic breast cancer. Hudis, C.A., Seidman, A.D., Crown, J.P., Balmaceda, C., Freilich, R., Gilewski, T.A., Hakes, T.B., Currie, V., Lebwohl, D.E., Baselga, J., Raptis, G., Gollub, M., Robles, M., Bruno, R., Norton, L. J. Clin. Oncol. (1996) [Pubmed]
  2. Phase II study of docetaxel for recurrent or metastatic non-small-cell lung cancer. Fossella, F.V., Lee, J.S., Murphy, W.K., Lippman, S.M., Calayag, M., Pang, A., Chasen, M., Shin, D.M., Glisson, B., Benner, S. J. Clin. Oncol. (1994) [Pubmed]
  3. Phase II study of docetaxel for advanced or metastatic platinum-refractory non-small-cell lung cancer. Fossella, F.V., Lee, J.S., Shin, D.M., Calayag, M., Huber, M., Perez-Soler, R., Murphy, W.K., Lippman, S., Benner, S., Glisson, B. J. Clin. Oncol. (1995) [Pubmed]
  4. Docetaxel: an active drug for squamous cell carcinoma of the head and neck. Dreyfuss, A.I., Clark, J.R., Norris, C.M., Rossi, R.M., Lucarini, J.W., Busse, P.M., Poulin, M.D., Thornhill, L., Costello, R., Posner, M.R. J. Clin. Oncol. (1996) [Pubmed]
  5. D-alanine: D-alanine ligase of Escherichia coli. Expression, purification and inhibitory studies on the cloned enzyme. al-Bar, O.A., O'Connor, C.D., Giles, I.G., Akhtar, M. Biochem. J. (1992) [Pubmed]
  6. Combination versus sequential doxorubicin and docetaxel as primary chemotherapy for breast cancer: A randomized pilot trial of the Hoosier Oncology Group. Miller, K.D., McCaskill-Stevens, W., Sisk, J., Loesch, D.M., Monaco, F., Seshadri, R., Sledge, G.W. J. Clin. Oncol. (1999) [Pubmed]
  7. Phase II study of docetaxel and cisplatin in advanced non-small-cell lung cancer. Zalcberg, J., Millward, M., Bishop, J., McKeage, M., Zimet, A., Toner, G., Friedlander, M., Barter, C., Rischin, D., Loret, C., James, R., Bougan, N., Berille, J. J. Clin. Oncol. (1998) [Pubmed]
  8. Docetaxel and cisplatin in metastatic urothelial cancer: a phase II study. Sengeløv, L., Kamby, C., Lund, B., Engelholm, S.A. J. Clin. Oncol. (1998) [Pubmed]
  9. Phase I study of docetaxel administered as a 1-hour intravenous infusion on a weekly basis. Tomiak, E., Piccart, M.J., Kerger, J., Lips, S., Awada, A., de Valeriola, D., Ravoet, C., Lossignol, D., Sculier, J.P., Auzannet, V. J. Clin. Oncol. (1994) [Pubmed]
  10. Heparin and low-molecular-weight heparin (enoxaparin) significantly ameliorate experimental colitis in rats. Dotan, I., Hershkoviz, R., Karmeli, F., Brazowski, E., Peled, Y., Rachmilewitz, D., Halpern, Z. Aliment. Pharmacol. Ther. (2001) [Pubmed]
  11. Docetaxel (Taxotere) and gemcitabine in combination therapy. Rizvi, N.A. Semin. Oncol. (1999) [Pubmed]
  12. Docetaxel (Taxotere)-based chemotherapy for hormone-refractory and locally advanced prostate cancer. Oh, W.K., Kantoff, P.W. Semin. Oncol. (1999) [Pubmed]
  13. A phase III study of irinotecan (CPT-11) versus best supportive care in patients with metastatic colorectal cancer who have failed 5-fluorouracil therapy. V301 Study Group. Cunningham, D., Glimelius, B. Semin. Oncol. (1999) [Pubmed]
  14. Efficacious response with lower dose indapamide therapy in the treatment of elderly patients with mild to moderate hypertension. Weidler, D., Jallad, N.S., Curry, C., Ferdinand, K., Jain, A.K., Schnaper, H.W., Toth, P.D., Codispoti, J., Stokes, A., McNally, C. Journal of clinical pharmacology. (1995) [Pubmed]
  15. Dose-ranging study of a new, once-daily diltiazem formulation for patients with stable angina. Cutler, N.R., Eff, J., Fromell, G., Brass, E.P., Archer, S., Chrysant, S.G., Fiddes, R. Journal of clinical pharmacology. (1995) [Pubmed]
  16. Docetaxel (Taxotere) in combination: a step forward. Burris, H.A., Fields, S., Peacock, N. Semin. Oncol. (1995) [Pubmed]
  17. Occupational exposure to fosetyl-Al fungicide during spraying of ornamentals in greenhouses. Fenske, R.A., Hamburger, S.J., Guyton, C.L. Arch. Environ. Contam. Toxicol. (1987) [Pubmed]
  18. Kinetics of abiotic hydrolysis of isoxaflutole: influence of pH and temperature in aqueous mineral buffered solutions. Beltran, E., Fenet, H., Cooper, J.F., Coste, C.M. J. Agric. Food Chem. (2000) [Pubmed]
  19. The Valiant thoracic endograft. Brooks, M., Loftus, I., Morgan, R., Thompson, M. The Journal of cardiovascular surgery. (2006) [Pubmed]
  20. SGN-10. Seattle Genetics. Smith, S.V. Current opinion in investigational drugs (London, England : 2000) (2001) [Pubmed]
  21. Docetaxel (Taxotere): an effective agent in the management of second-line breast cancer. van Oosterom, A.T. Semin. Oncol. (1995) [Pubmed]
  22. Bonded amalgam restorations: using a glass-ionomer as an adhesive liner. Chen, R.S., Liu, C.C., Cheng, M.R., Lin, C.P. Operative dentistry. (2000) [Pubmed]
  23. Effect of fosetyl-A1 on peroxidase from grapevine (Vitis vinifera) cells. López-Serrano, M., Ferrer, M.A., Ros Barceló, A., Pedreño, M.A. European journal of histochemistry : EJH. (1995) [Pubmed]
  24. Marginal leakage of palladium-enriched amalgam restorations: an in-vitro study. Khalaf, M.A. Clinical materials. (1990) [Pubmed]
  25. Preliminary evaluation of a short course of estramustine phosphate and docetaxel (Taxotere) in the treatment of hormone-refractory prostate cancer. Sinibaldi, V.J., Carducci, M., Laufer, M., Eisenberger, M. Semin. Oncol. (1999) [Pubmed]
  26. Phosphorous acid residues in apples after foliar fertilization: results of field trials. Malusà, E., Tosi, L. Food additives and contaminants. (2005) [Pubmed]
  27. Strengths of modified amalgam-to-dentin interphases. Herda, E., Arianto, Y.K., Baier, R.E., Meyer, A.E. Journal of materials science. Materials in medicine. (1997) [Pubmed]
  28. Comparative wear ranking of dental restoratives with the BIOMAT wear simulator. Yap, A.U., Ong, L.F., Teoh, S.H., Hastings, G.W. Journal of oral rehabilitation. (1999) [Pubmed]
  29. The fracture toughness of various core materials. Ziebert, A.J., Dhuru, V.B. Journal of prosthodontics : official journal of the American College of Prosthodontists. (1995) [Pubmed]
  30. Severe chronic neutropenia: pathophysiology and therapy. Welte, K., Boxer, L.A. Semin. Hematol. (1997) [Pubmed]
  31. Bruxing-type dental wear simulator for ranking of dental restorative materials. Teoh, S.H., Ong, L.F., Yap, A.U., Hastings, G.W. J. Biomed. Mater. Res. (1998) [Pubmed]
  32. Microbiological high throughput screening: an opportunity for the lead discovery process. Beydon, M.H., Fournier, A., Drugeault, L., Becquart, J. Journal of biomolecular screening : the official journal of the Society for Biomolecular Screening. (2000) [Pubmed]
  33. A comparative evaluation of three high efficiency disposable dialyzers. Hoenich, N.A., Kerr, D.N. Clin. Nephrol. (1975) [Pubmed]
  34. Evaluation of interfacial bond strengths between amalgam and composite inlay. Abdel-Aziz, A.H., Alhadainy, H.A. American journal of dentistry. (1998) [Pubmed]
  35. Rhône-Poulenc to focus biotech work on gene therapy. Butler, D. Nature (1994) [Pubmed]
  36. Taxoids: effective agents in anthracycline-resistant breast cancer. Ravdin, P.M. Semin. Oncol. (1995) [Pubmed]
  37. Docetaxel (Taxotere) in combination with anthracyclines in the treatment of breast cancer. Nabholtz, J.M., North, S., Smylie, M., Mackey, J., Au, H.J., Au, R., Morrish, D., Salter, E., Tonkin, K. Semin. Oncol. (2000) [Pubmed]
  38. The role of docetaxel (Taxotere) as a single agent or in combination before local treatment of non-small cell lung cancer. Harper, P. Semin. Oncol. (1997) [Pubmed]
  39. The use of docetaxel (Taxotere) in patients with advanced non-small cell lung cancer previously treated with platinum-containing chemotherapy regimens. Fossella, F.V., Rigas, J. Semin. Oncol. (1999) [Pubmed]
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