Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0376358 (prostate cancer)
 59,338 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The efficacy of an association of cyclophosphamide (CPM) and 5-fluorouracil was studied in 15 patients with prostate cancer not responding to oestrogen therapy, and more particularly its effect on pain due to bone metastases. No objective improvement was noted with this association, but there was a definitite reduction in bone metastases pain in 5 of the patients, with an average remission time of 4 months. Half of the patients had nausea and vomiting, but in spite of this digestive intolerance those patients who obtained pain relief for 4 months considered the treatment to be of positive value. This therapy is recommended only fater the failure of castration, anti-androgens, and oestrogens, together with nitrogen mustard (Estracyt) and corticotherapy.
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PMID:[Palliative chemotherapy with 5 FU and CPM in cancer of the prostate with bone metastases resistant to oestrogens. A clinical trial (author's transl)]. 9 8

30 patients with oestrogen-escaped carcinoma of the prostate have been treated with estramustine phosphate (Estracyt). 27% showed a partial objective response and 33% had a subjective response. The terms used for defining a response are challenged and it is recommended that comparative controlled trials are necessary to judge the place of this drug in the management of advanced prostatic cancer.
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PMID:The treatment of oestrogen-escaped carcinoma of the prostate with estramustine phosphate. 33 86

The relationship of prior hormonal therapy to subsequent response on estramustine phosphate (Estracyt) was examined in 107 patients with advanced prostatic cancer treated in two different Phase II chemotherapy trials. In both trials patients with the longest prior hormonal treatment were the least likely to respond to estramustine phosphate. Patients in the series from the National Prostatic Cancer Project with a response classification to prior hormonal therapy had only a 26 per cent response to subsequent estramustine phosphate therapy, whereas 40 per cent of those with no prior response to hormonal therapy responded to estramustine phosphate. This latter group had the shortest average disease duration from diagnosis. The sample of prostate cancers studied appeared to include groups that were sensitive to both hormones and cytotoxic activity as well as to either of these two alone. These data support the contention that estramustine phosphate may act both as an estrogenic and a cytotoxic agent.
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PMID:Relationship of prior hormonal therapy to subsequent estramustine phosphate treatment in advanced prostatic cancer. 39 Aug 10

A transplantable, metastasizing prostatic adenocarcinoma (Tumor I) in Lobund Wistar rats was examined for activity and distribution of five hydrolytic enzymes and for ability to accumulate radioactive zinc. The results suggest that the tumor had arisen in the ventral lobe of the prostate and that its growth was not affected by orchiectomy, adrenalectomy, or replacement treatment with exogenous androgen or corticosteroids. The androgen independency of the tumor was further shown by the low uptake of 3H-testosterone, in contrast to the high uptake in the ventral prostate. Tumor growth was retarded by Cytoxan but not by 5-fluorouracil, Estracyt, or streptozotocin, three agents clinically effective in the treatment of some patients with prostatic cancer resistant to endocrine therapy. It is concluded that this tumor in Lobund Wistar rats may be an adequate model for human prostatic cancers resistant to the agents mentioned above.
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PMID:A rat prostatic adenocarcinoma as a model for the human disease. 44 85

40 patients with inoperable, histologically proved carcinoma of the prostate were treated with estramustine phosphate. 35 patients had progressive, symptomatic, metastatic disease unresponsive to conventional oestrogens and/or castration Estramustine phosphate was given intravenously initially at a dose of 150 mg/day increasing to 300 mg/day. After 3 weeks or more oral therapy was substituted in 23 patients at a dose of 560 mg/day. Of 23 evaluable patients given the drug by both routes, 17 died after a mean treatment period of 12.5 months and 6 are alive and well after a mean treatment period of 27.7 months. The cause of death in 2 patients was probably, and in a third certainly, due to myocardial infarction. The other 31 deaths were due to carcinoma of the prostate. 18 patients showed transient toxic side-effects. No haematological abnormalities were found during treatment. An attempt at active treatment with estramustine phosphate in patients with prostatic cancer is justified when the disease is resistant to treatment with conventional oestrogens.
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PMID:Treatment of advanced carcinoma of the prostate with estramustine phosphate. 83 52

We treated 21 patients with stage D prostatic adenocarcinoma who had had unsuccessful hormonal therapy with a combination of 600 mg. per M.2 per day estramustine phosphate (Estracyt) and 15 mg. per M.2 per day prednimustine (Stereocyt, Leo 1031) in daily oral doses. Estramustine is a combination of estradiol and nitrogen mustard, and alone has shown objective responses in advanced prostatic cancer. Prednimustine is an ester of chlorambucil and prednisone. The preliminary results (after 2 to 9 months of therapy) show 5 patients (24 per cent) did not benefit from the drug and 7 patients (33 per cent) are stable. These preliminary results indicate the possible advantage of adding an alkylating agent (prednimustine) to estramustine in advanced prostatic carcinoma. Currently, a national randomized trial by the National Prostatic Cancer Project is evaluating this therapeutic innovation.
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PMID:Combined therapy of advanced prostatic carcinoma with estramustine and prednimustine. 83 97

Estramustine phosphate is a nitrogen mustard derivative of estradiol that has been advocated for the treatment of prostatic cancer. The compound was designed with the hope that the estrogen moiety would direct the alkylating moiety to estrogen-dependent malignancies, where the alkylating moiety would be released specifically. Preclinical and clinical data are reviewed to determine to what extent that challenging concept is fulfilled. In addition, we have examined critically the efficacy of this drug for the treatment of prostatic cancer. From available data it appears that there is no evidence that the alkylating moiety of estramustine phosphate is specifically freed in estrogen-dependent tissues. Estramustine phosphate appears to be an active compound with acceptable toxicity in prostatic cancer. However, further clinical trials must be undertaken to clarify the future role of estramustine phosphate in the treatment of prostatic cancer.
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PMID:Estramustine phosphate: a specific chemotherapeutic agent?. 85 Mar 19

In a previous study, 50 patients with prostatic carcinoma were given continuous oral estramustine phosphate at a dose of 15 mg/kg/day. All patients had progressed on prior standard treatment. The objective and subjective response rates were 19% and 36% respectively. Seven of the 50 patients are still receiving treatment after 1-3 years. One patient who was given estramustine phosphate therapy for 1 year achieved a complete response, which included disappearance of osteoblastic metastasis. He still continues in unmaintained remission despite the fact that estramustine phosphate therapy was stopped because of gastrointestinal toxicity. No serious side effects related to the drug have been seen. Estramustine phosphate may be given safely for a prolonged period and has a place in the treatment of advanced prostatic cancer refractory to hormonal therapy. Twenty-one patients with stage D prostatic adenocarcinoma who failed hormonal therapy were treated with a combination of estramustine phosphate (600 mg/m2/day) plus prednimustine (Leo-1031) (15 mg/m2/day) in daily oral doses. Fifteen patients have been treated with prednimustine alone. The preliminary results of the combination therapy (after 2-9 months) are as follows: five patients (24%) had an objective response and nine patients (44%) had subjective improvement. Only five (24%) did not benefit from the drug and seven (33%) are stable. Of the 16 patients treated with prednimustine alone, one patient has had an unequivocal objective response and one experienced a considerable objective improvement. These preliminary results indicate the possible advantage of adding an alkylating agent (prednimustine) to estramustine phosphate in advanced prostatic carcinoma.
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PMID:New steroidal alkylating agents in advanced stage D carcinoma of the prostate. 87 34

Estracyt (estramustine phosphate) injected intraperitoneally, 100 mg, per Kg. three days a week for four weeks, retarded growth of the R-3327 tumor in intact rats and in orchiectomized rats given androgen. The growth inhibition was accomplished by reduction of tumor deoxyribonucleic acid concentration and of the activities of acid phosphatase, leucine aminopeptidase, and other hydrolases. Histologic examination revealed cellular necrosis particularly prominent in the orchiectomized, androgen-treated rats. Estracyt did not affect the uptake of 65-Zn in the tumors but markedly reduced the high uptake in the dorsolateral prostate. There was no accumulation of 3H or 14C in the tumors after intravenous administration of 3H, 14C-labeled Estracyt, but the isotope concentrations decreased much in the same way as they decreased in the dorsolateral prostate. The isotopes were retained in the ventral prostate, where their concentrations were approximately twenty times higher than those in the muscle four hours after injection. The results demonstrate the value of the R-3327 tumor in the evaluation of drugs of potential clinical use for the treatment of prostatic cancer. The results also show that Estracyt has an antitumor effect which is not dependent on the antigonadotropic action of the drug.
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PMID:Inhibitory effects of Estracyt on R-3327 rat prostatic carcinoma. 91 34

Estracyt, a compound of nitrogen-mustard linked to oestradiol phosphate, is used in the treatment of human prostatic cancer. The metabolism of this compound has been studied in different tissues of the rat both in vivo and in vitro. The phosphate group in position 17 of the oestradiol moiety is rapidly split off from the compound. An oestrone-cytostatic compound was extractable from the liver half an hour after the injection of Estracyt. In addition the in vitro results showed that only the liver was able to convert the oestradiol-cytostatic compound to an oestrone-cytostatic one. When animals were killed 24 h after a 3-day period of Estracyt treatment, the dominating metabolite in the ventral prostate was an oestronecytostatic compound, but traces of free oestrone could also be demonstrated. No such compound, however, was found in liver, diaphragm or blood at this time. It is concluded that in vivo an oestrone-cytostatic compound seems to be preferentially retained in the ventral prostate after Estracyt injection whilst the metabolic conversion of the oestradiol-cytostatic compound into an oestrone-cytostatic one possibly occurs in the liver.
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PMID:Studies on the conversion of oestradiol linked to a cytostatic agent (Estracyt) in various rat tissues. 94 35


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