Phase II evaluation of chlorozotocin (NSC-178248) in advanced human cancer.

  title={Phase II evaluation of chlorozotocin (NSC-178248) in advanced human cancer.},
  author={Robert W. Talley and Michael K. Samson and Robert W. Brownlee and A M Samhouri and R J Fraile and Laurence H. Baker},
  journal={European journal of cancer},
  volume={17 3},
Phase II trial with chlorozotocin in advanced colorectal cancer.
Evaluation of bleomycin, chlorozotocin, MGBG, and bruceantin in patients with advanced soft tissue sarcoma, bone sarcoma, or mesothelioma
None of the four drugs tested was active against previously treated sarcomas at these doses and schedules, but bleomycin, however, should be considered for further evaluation in mesothelioma patients.
Phase II New Drug Trials in Soft Tissue Sarcomas
Since the complete response rate to doxorubicin alone or in combination rarely exceeds 10%, with only an occasional patient having prolonged meaningful survival, efforts have continued to identify new drugs with activity against soft tissue sarcomas.
Hematological toxicity of repeated injections of (chloro-2-ethyl)-ribofuranosyl-3-nitrosourea.
The results demonstrate that (chloro-2-ethyl)ribofuranosyl-3-nitrosourea belongs to the class of new nitrosoureas with low cumulative hematotoxicity and contrasts with the absence of significant effect when the same treatment is used on peripheral white blood cell counts.
Nitrosoureas. Modes of action and perspectives in the use of hormone receptor affinity carrier molecules.
Mechanisms of DNA adduct formation by antineoplastic 2-chloroethyl-N-nitrosoureas (CNUs) and of DNA damage induced by these compounds are discussed. CNUs are alkylating agents that form DNA-DNA
Nitrosoureas-Still a Challenge for Developmental Cancer Chemotherapy
Although 2-chloroethyl-N-nitrosoureas (CNU’s) are highly active antineoplastic agents with a broad antitumour spectrum in experimental systems, in the clinic their usefulness is limited. The most
Synthesis and antineoplastic activity of CNC-cysteamine and related compounds
Preliminary testing of the newly synthesized CNC-derivatives against L 1210 leukemia in mice revealed that C NC-cysteamine, its disulfide bis(CNC)cystamine and CNC -cystamines carboxylazide were highly active against L1210 leukemia.
Systemische Chemotherapie maligner Melanome
Die Uberlebensprognose von Patienten mit metastasierendem malignem Melanom der fortgeschrittenen Stadien III und IV ist bis heute denkbar ungunstig, nur vereinzelt uberleben wenige von ihnen ohne
Chlorozotocin treatment of advanced gastrointestinal cancer.
At the dosage and schedule used, chlorozotocin does not seem to be an effective agent in the treatment of advanced gastrointestinal cancer.


Phase I trial of chlorozotocin.
Chlorozotocin was given to 37 patients with advanced malignant tumors in a daily X 5 schedule at 6-week intervals, with no major antitumor activity occurred; however, three patients with renal cell carcinoma and one patient each with lung cancer, ovarian carcinoma, and Hodgkin's disease had minor objective decreases in tumor size.
Phase I studies on chlorozotocin
Based on these studies, the recommended dose for phase II investigation of chlorozotocin is 120 mg/m2 every 6 wk, and there were objective signs of therapeutic activity in 5 patients, 3 of whom had melanoma.
Pharmacology of chlorozotocin Nsc-178248), a new nitrosourea antitumor agent.
If aminoglucose modification of nitrosourea bone marrow toxicity can be confirmed in man without significant loss of antitumor activity, the use of such a compound could facilitate treatment of patients with neoplastic disease who have pre-existing abnormal bone marrow function.
Chlorozotocin, 2-(3-(2-chloroethyl)-3-nitrosoureido)-D-glucopyranose, an antitumor agent with modified bone marrow toxicity.
If the antitumor activity and reduced bone marrow toxicity of chlorozotocin are confirmed in man the use of this compound would facilitate treatment of patients with neoplastic disease who have preexisting abnormal bone marrow function or would allow for the more effective use of a nitrosourea agent in combination with anticancer agents possessing more potent myelosuppressive properties.