Objective： We aimed to evaluate the efficiency of serum testosterone suppression as well as the potential for agonistic stimulation of serum testosterone during chronic treatment with monthly （3.75 mg） depot formul...Objective： We aimed to evaluate the efficiency of serum testosterone suppression as well as the potential for agonistic stimulation of serum testosterone during chronic treatment with monthly （3.75 mg） depot formulation of domestic substitute of leuprorelin acetate microspheres for patients with metastatic prostate cancer. Methods： A total of 23 patients with metastatic prostate cancer were enrolled in the prospective study and received 6 monthly intramuscular depot injections of domestic substitute of leuprorelin acetate microspheres. Their levels and patterns of serum testosterone suppression and the potential for agonistic stimulation of serum testosterone were monitored following injection monthly （3.75 rag） depot formulation of domestic substitute of leuprorelin acetate microspheres for 24 weeks. Results： Mean testosterone was 431.4 ng/dL, 119.3 ng/dL, 28.2 ng/dL by week 1, 2, 3 and decreased to less than 15.6 ng/dL by week 4 where it remained throughout the treatment period. Median time to suppression of serum testosterone was 20.7 days. No transient minor ＂escape＂ from suppression occurred in all patients which was defined as a single testosterone value greater than 50 ng/dL once suppression was achieved. Assessment of agonistic stimulation following the second depot injection revealed no pattern of stimulation. Conclusion： We concluded that monthly （3.75 mg） depot formulation of domestic substitute of leuprorelin acetate microspheres could provide persistent, stable suppression of serum testosterone throughout the dosing intervals, and that the initial depot injection of this formulation also could provide sufficient pituitary desensitization to prevent agnostic stimulation of serum testosterone during chronic treatment.展开更多
A major goal of research in biotechnology and nanotechnology is to develop assemblies of novel biomaterials that can be used in analytical, industrial, and therapeutic applications. The synthesis of DNA （oligodeoxyri...A major goal of research in biotechnology and nanotechnology is to develop assemblies of novel biomaterials that can be used in analytical, industrial, and therapeutic applications. The synthesis of DNA （oligodeoxyribonucleotide） has been described containing the biaryl-type nucleoside surrogates, 6-deamino-2＇-deoxy-6-（l-naphthyl） adenosine （AN） and 6-deamino-2＇-deoxy-6-（1-pyrenyl） adenosine （AP）. It is found that incorporation of multiple ATM or AP residues in the middle of DNA duplexes does not significantly destabilize the duplexes and that the fluorescence intensities of the oligonucleotides containing AN or Ap significantly increases in the duplexes formed.展开更多
基金Supported by a grant from the State Key Laboratory of Environmental Chemistry and Ecotoxicology,Chinese Academy of Sciences(No.KF2011-12)
文摘Objective： We aimed to evaluate the efficiency of serum testosterone suppression as well as the potential for agonistic stimulation of serum testosterone during chronic treatment with monthly （3.75 mg） depot formulation of domestic substitute of leuprorelin acetate microspheres for patients with metastatic prostate cancer. Methods： A total of 23 patients with metastatic prostate cancer were enrolled in the prospective study and received 6 monthly intramuscular depot injections of domestic substitute of leuprorelin acetate microspheres. Their levels and patterns of serum testosterone suppression and the potential for agonistic stimulation of serum testosterone were monitored following injection monthly （3.75 rag） depot formulation of domestic substitute of leuprorelin acetate microspheres for 24 weeks. Results： Mean testosterone was 431.4 ng/dL, 119.3 ng/dL, 28.2 ng/dL by week 1, 2, 3 and decreased to less than 15.6 ng/dL by week 4 where it remained throughout the treatment period. Median time to suppression of serum testosterone was 20.7 days. No transient minor ＂escape＂ from suppression occurred in all patients which was defined as a single testosterone value greater than 50 ng/dL once suppression was achieved. Assessment of agonistic stimulation following the second depot injection revealed no pattern of stimulation. Conclusion： We concluded that monthly （3.75 mg） depot formulation of domestic substitute of leuprorelin acetate microspheres could provide persistent, stable suppression of serum testosterone throughout the dosing intervals, and that the initial depot injection of this formulation also could provide sufficient pituitary desensitization to prevent agnostic stimulation of serum testosterone during chronic treatment.
文摘A major goal of research in biotechnology and nanotechnology is to develop assemblies of novel biomaterials that can be used in analytical, industrial, and therapeutic applications. The synthesis of DNA （oligodeoxyribonucleotide） has been described containing the biaryl-type nucleoside surrogates, 6-deamino-2＇-deoxy-6-（l-naphthyl） adenosine （AN） and 6-deamino-2＇-deoxy-6-（1-pyrenyl） adenosine （AP）. It is found that incorporation of multiple ATM or AP residues in the middle of DNA duplexes does not significantly destabilize the duplexes and that the fluorescence intensities of the oligonucleotides containing AN or Ap significantly increases in the duplexes formed.
