生物活性

• 描述Chlorambucil, a chemotherapeutic agent, is usually administered orally to treat chronic lymphocytic leukemia and some other types of cancers in regimens of conventional and metronomic chemotherapies. Furthermore, the mesoporous polymeric microspheres as carriers greatly stabilized chlorambucil against its hydrolysis. The hydrolyzation percentage of chlorambucil that was adsorbed on the microspheres after incubation for 36 h in media simulating gastrointestinal fluids was less than 10%, while more than 90% of free chlorambucil hydrolyzed after incubation in the same media for 4 h. The chlorambucil-loaded mesoporous polymeric microspheres may be used as oral sustained release formulations, especially as oral formulations for the application in metronomic chemotherapy^[3]. Metronomic administration of chlorambucil was well tolerated, and 70% of dogs had partial remission or stable disease. Metronomic administration of chlorambucil may be a treatment option for dogs with TCC(transitional cell carcinoma) ^[4]. Chlorambucil compares favorably with fludarabine and bendamustine with respect to myelotoxicity, neutropenia, and fever, even at 70 mg/m(2) per cycle and in the elderly^[5]. The induction of apoptosis by CLB (Chlorambucil) is paralleled by an increase in P53 and Mdm-2 but this increase in not observed in patients with p53 mutations indicating that with high drug concentrations CLB can produce cell death through P53 independent pathways^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01664117	-	-	Completed	-	Spain ... more >> Vitoria, Alava, Spain, 01009 Elche, Alicante, Spain, 03203 Oviedo, Asturias, Spain, 33006 Zafra, Badajoz, Spain, 06300 Sabadell, Barcelona, Spain, 08208 Viladecans, Barcelona, Spain, 08840 Jerez de la Frontera, Cadiz, Spain, 11407 Vinaroz, Castellon, Spain, 12500 Cenes de la vega, Granada, Spain, 18190 Granda, Granada, Spain, 18190 San Sebastian, Guipuzcoa, Spain, 20080 Ibiza, Islas Baleares, Spain, 07800 Inca, Islas Baleares, Spain, 07300 Manacor (Islas Baleares), Islas Baleares, Spain, 07500 Jaén, Jaen, Spain, 23007 La Coruna, La Coruña, Spain, 15006 Alcala de Henares, Madrid, Spain, 28805 Benalmadena, Malaga, Spain, 29630 Vigo, Pontevedra, Spain, 36214 Gandia, Valencia, Spain, 46700 Alicante, Spain, 03010 Burgos, Spain, 06006 Caceres, Spain, 10310 Cordoba, Spain, 14001 Girona, Spain, 17007 Madrid, Spain, 28006 Madrid, Spain, 28007 Madrid, Spain, 28034 Madrid, Spain, 28222 Madrid, Spain, 28905 Malaga, Spain, 29005 Murcia, Spain, 30008 Palencia, Spain, 34005 Sevilla, Spain, 41013 Sevilla, Spain, 41018 Tenerife, Spain, 38010 Toledo, Spain, 45004 Valencia, Spain, 46015 Valladolid, Spain, 47005 Zamora, Spain, 49022 Zaragoza, Spain, 50009 Collapse <<
  NCT01664117	-	-	Completed	-	-
  NCT02987127	-	-	Recruiting	December 2019	Taiwan ... more >> National Taiwan University Hospital Recruiting Taipei, Taiwan, 100 Contact: Sung-Hsin Kuo, M.D.,Ph.D    +886-2-23123456 ext 67144    shkuo101@ntu.edu.tw    Contact: Shu-Ling Wu, MS    +886-2-23123456 ext 67573    shulingwu.ntuh@gmail.com Collapse <<

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• 参考文献

• [1] Guo JX, Zhou YH, et al. Synergistic effects of chlorambucil and TRAIL on apoptosis and proliferation of Raji cells. Eur Rev Med Pharmacol Sci. 2017 Oct;21(20):4703-4710.

  [2] Miksa B, Sierant M, et al. Chlorambucil labelled with the phenosafranin scaffold as a new chemotherapeutic for imaging and cancer treatment. Colloids Surf B Biointerfaces. 2017 Sep 1;159:820-828.

  [3] Wang X, Cao Y, Yan H. Chlorambucil loaded in mesoporous polymeric microspheres as oral sustained release formulations with enhanced hydrolytic stability. Mater Sci Eng C Mater Biol Appl. 2018 Oct 1;91:564-569

  [4] Schrempp DR, Childress MO, Stewart JC, Leach TN, Tan KM, Abbo AH, de Gortari AE, Bonney PL, Knapp DW. Metronomic administration of chlorambucil for treatment of dogs with urinary bladder transitional cell carcinoma. J Am Vet Med Assoc. 2013 Jun 1;242(11):1534-8

  [5] Catovsky D, Else M, Richards S. Chlorambucil--still not bad: a reappraisal. Clin Lymphoma Myeloma Leuk. 2011 Jun;11 Suppl 1:S2-6

  [6] Begleiter A, Mowat M, Israels LG, Johnston JB. Chlorambucil in chronic lymphocytic leukemia: mechanism of action. Leuk Lymphoma. 1996 Oct;23(3-4):187-201

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