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At least 19 recordsLinked to original sources

PubMed1989

Combination chemotherapy of advanced breast cancer. Comparison of dibromodulcitol, doxorubicin, vincristine, and fluoxymesterone to thiotepa, doxorubicin, vinblastine, and fluoxymesterone: an Eastern Cooperative Oncology Group Study.

Two Adriamycin (doxorubicin)-based chemotherapy regimens were investigated in patients with carcinoma of the breast who had failed prior systemic therapy. The two chemotherapy programs, dibromodulcitol, Adriamycin, vincristine, and Halotestin (fluoxymesterone) (DAVH), and thiotepa, Adriamycin, vinblastine, and Halotestin (TAVH), were chosen for comparison on the basis of reported response rates of 40% to 50% with remission durations of 11 months in patients refractory to other cytotoxic chemotherapy. Cycles of DAVH were repeated every 4 weeks. Cycles of TAVH were repeated every 3 weeks. Of 184 patients evaluable for response, 32% of patients treated with DAVH and 38% of patients treated with TAVH had a complete response (CR) or partial response (PR). An additional 5% of patients had nonmeasurable improvement in osseous disease for an overall rate of response (CR + PR + improvement) of 40%. Patients who had previously received cytotoxic chemotherapy for metastatic disease or had early failure after adjuvant therapy had a lower response rate to DAVH, but not to TAVH than those who did not fail prior chemotherapy. Duration of response and survival were similar with the two treatments. There were seven treatment-related deaths, five among patients receiving DAVH and two among patients receiving TAVH. Patients receiving DAVH had significantly more thrombocytopenia and neurologic toxicity than those receiving TAVH. These treatments appear to be reasonable second-line regimens and are good candidates to be used in initial therapy of metastatic disease or adjuvant therapy studies that explore the use of alternating non-cross-resistant combinations with cyclophosphamide, methotrexate, and 5-fluorouracil.

Adenocarcinoma↗

PubMed1977

The effects of fluoxymesterone administration on testicular function.

Long term daily administration of fluoxymesterone (9alpha-fluoro-17alpha-methyl-11beta, 17beta-dihydroxyandrost-4-en-3-one) was associated with a modest suppression of sperm production and a profound suppression of testosterone levels in the absence of significant effects on plasma gonadotropin levels. Nine normal male volunteers took either 10, 20, or 30 mg of fluoxymesterone daily for twelve weeks. Plasma samples were obtained for testosterone, estrogen, LH and FSH levels at biweekly intervals before, during and for up to 12 weeks after fluoxymesterone treatment. Samples were obtained for dehydroepiandrosterone sulfate, testosterone binding globulin and free testosterone assays at representative times before, during and after treatment. Although lower sperm counts were observed at several points during both the treatment and follow up periods, significant consistent suppression of spermatogenesis could not be demonstrated. Reduced plasma testosterone levels were seen within 24 h after beginning fluoxymesterone, and further reductions were noted throughout the treatment period. Changes in plasma estrogen levels did not correlate with fluoxymesterone administration. Neither plasma LH nor plasma FSH levels were significantly altered by fluoxymesterone. A short term study utilizing a single dose of fluoxymesterone yielded similar findings. It is proposed that fluoxymesterone has a local effect on the Leydig cell which is not mediated by gonadotropins.

Adult↗

PubMed1983

Evaluation of tamoxifen doses with and without fluoxymesterone in advanced breast cancer.

From a group of 108 female patients with measurable and/or evaluable metastatic breast carcinoma, 52 were randomized to receive tamoxifen and 56 to receive tamoxifen and fluoxymesterone. The fluoxymesterone dose, given orally twice a day, was 7 mg/m2 body surface area. The tamoxifen dose per patient, also given orally twice a day, ranged from 2 to 100 mg/m2 body surface area. Eighty-five percent of the patients had received previous chemotherapy and 60% previous hormone therapy. The complete and partial remission rate was better with the tamoxifen and fluoxymesterone regimen (p = 0.016), with remission rates of 15% for tamoxifen alone and 38% for the combination. The tamoxifen and fluoxymesterone regimen appeared to have higher remission rates in all subsets of pretreatment variables. Duration of remission with each regimen was similar, but the overall time to treatment failure for tamoxifen and fluoxymesterone was longer than for tamoxifen alone (180 versus 64 days, p = 0.01). Median survival with the combination was 380 days compared to 330 days for tamoxifen. No significant dose-response relationships emerged. Side effects were not different between dose levels or regimens except for the androgen effects in the tamoxifen and fluoxymesterone combination. These results suggest that there is no major dose-response effect for doses ranging from 2 to 100 mg/m2 body surface area given twice daily in this largely (94%) postmenopausal pretreated patient group, and that the tamoxifen and fluoxymesterone regimen is superior to tamoxifen alone.

Adult↗

PubMed1985

Liquid chromatographic assay for fluoxymesterone in human serum with application to a preliminary bioavailability study.

Fluoxymesterone was extracted from serum with a liquid-liquid extraction procedure. Serum containing both drug and internal standard, 6 alpha-methylprednisolone, was extracted with methylene chloride. The extract was washed with 0.1 M NaOH and water, evaporated, and reconstituted with mobile phase. Chromatography was performed on a Zorbax Sil column, preceded by a guard column, with a mobile phase composed of 50% water-saturated butyl chloride:tetrahydrofuran:methanol:phosphoric acid (880:100:15:0.5). Fluoxymesterone and methylprednisolone were detected by UV absorption at 236 nm. Overall recovery was 80%. Calibration curves were linear for fluoxymesterone concentrations from 5 to 100 ng/mL. The assay is accurate and precise (RSD values less than or equal to 7%); endogenous steroids did not interfere with the assay. Assay suitability was assessed in a bioavailability study in which six subjects each received two treatments of 10-mg fluoxymesterone tablets in a Latin-square crossover study. The two treatments were a tablet administered either buccally or orally. Cmax values ranged from 40 to 150 ng/mL with tmax values of 1-2 h. The harmonic mean half-life of fluoxymesterone was 2.0 h. Less than 8% of the AUC was extrapolated. Mean Cmax and AUC values from the oral treatment were 80 and 76%, respectively, of the mean values from the buccal treatment.

Adult↗

PubMed1988

Tamoxifen and fluoxymesterone versus tamoxifen and danazol in metastatic breast cancer--a randomized study.

A prospective randomized trial of tamoxifen and fluoxymesterone versus tamoxifen and danazol in metastatic breast cancer was conducted from December 1980 to September 1985. Patients were eligible regardless of site of disease, estrogen receptor status, or age. Sixty-two of sixty-three randomized patients were evaluable for response. Overall response for tamoxifen and fluoxymesterone was 11% with 61% stabilization of disease, versus 12% response rate for tamoxifen and danazol with 59% stabilization. Toxicities with tamoxifen and fluoxymesterone were greater with an increase in masculinization. We conclude that the response rates to the combinations of tamoxifen and fluoxymesterone or tamoxifen and danazol reported are equivalent in this study but that the increased toxicity with tamoxifen and fluoxymesterone would make tamoxifen and danazol the treatment of choice if a combination were to be used.

Adult↗

PubMed1981

Fluoxymesterone and the development of sexual behavior in the golden hamster.

Male hamsters castrated at birth and female hamsters were treated on postnatal Days 2-4 with 100 microgram of testosterone. 100 microgram of fluoxymesterone, or the hormone vehicle. As adults, mounting behavior and lordosis were measured following exogenous hormone treatment. Although the degree of penile or clitoral virilization did not appear to differ between testosterone- and fluoxymesterone-treated animals, behavioral differences occurred. Neonatal treatment with fluoxymesterone failed to "masculinize" or defeminize" behavior; neonatal testosterone treatment induced mounting in males and females and intromission in males. These results, along with those of others, indicate that fluoxymesterone has little or no central neural effect on sexual behavior in the hamster.

Animals↗

PubMed1976

Effect of fluoxymesterone on the pituitary-gonadal axis: the role of testosterone-estradiol-binding globulin.

Four normal men and two agonadal men were given the oral synthetic androgen, fluoxymesterone (9alpha-fluoro-11beta, 17beta-dihydroxy-17alpha-methyl-4-androstene-3-one) for three days. Plasma testosterone (T), 17 alpha-hydroxyprogesterone (17-OHP), and LH were measured every 30 minutes on a control day and on the first day of treatment. Testosterone and LH were measured every six hours on the last day of treatment. During the first 24 hours of treatment the number of LH secretory episodes per day decreased from 10.5+/-2.5 (SD) to 6.2+/-2.9 (SD) (P less than 0.01), mean 24 hour LH decreased from 12.6+/-3.5 (SD) mlU/ml to 9.3+/-3.7 (SD) mlU/ml (P less than 0.01), and mean 17-OHP decreased from 2.33+/-1.4 (SD) ng/ml to 1.18+/-0.39 (SD) ng/ml (P less than 0.01) in all normal subjects. T was significantly decreased (P less than 0.01) from 464.5+/-76.4 (SD) ng/100 ml to 294.2+/-99.5 (SD) ng/100 ml. By the third day of treatment, LH had decreased further in four, and T in three of four normals. The number of LH spikes and the mean LH levels did not decrease in the agonadal patients. In vitro, using equilibrium dialysis, fluoxymesterone displaced T from plasma binding proteins with an apparent K=1.0 x 10(8) and 1.9 x 10(7) in female and male plasma, respectively, at 22 C; and 5.2 x 10(7) and 8.0 x 10(6) at 37 C. In polyacrylamide gel electrophoresis, a 500-fold molar excess of fluoxymesterone decreased the peak of TeBG-bound T by 45% (P less than 0.01). The in vitro data are consistent with the possibility that, in vivo, the displacement of T from TeBG by fluoxymesterone may play a role in the suppression of the pituitary-gonadal axis by synthetic oral androgens in vivo.

Adult↗

PubMed1995

Metabolism of anabolic steroids in humans: synthesis of 6 beta-hydroxy metabolites of 4-chloro-1,2-dehydro-17 alpha-methyltestosterone, fluoxymesterone, and metandienone.

Hydroxylation at position 6 beta testosterone I (17 beta-hydroxyandrost-4-en-3-one) and the anabolic steroids 17 alpha-methyltestosterone II (17 beta-hydroxy-17 alpha-methylandrost-4-en-3-one), metandienone III (17 beta-hydroxy-17 alpha-methylandrosta-1,4-dien-3-one), 4-chloro-1,2-dehydro-17 alpha-methyltestosterone IV (4-chloro-17 beta-hydroxy-17 alpha-methylandrosta-1,4-dien-3-one), and fluoxymesterone V (9-fluoro-11 beta, 17 beta-dihydroxy-17 alpha-methylandrost-4-en-3-one) was achieved via light-induced autooxidation of the corresponding trimethysilyl 3,5-dienol ethers dissolved in isopropanol or ethanol. The reaction further yielded the 6 alpha-hydroxy isomer in low amounts. The 6 beta-hydroxy isomer of I-V and the 6 alpha-hydroxy isomers of I, III, and IV were isolated and characterized by 1H and 13C NMR, high-performance liquid chromatography, gas chromatography, and mass spectrometry. Human excretion studies with single administered doses of boldenone (17 beta-hydroxyandrosta-1,4-dien-3-one), 4-chloro-1,2-dehydro-17 alpha-methyltestosterone, fluoxymesterone, metandienone, 17 alpha-methyltestosterone, and [16,16,17-2H3] testosterone showed that 6 beta-hydroxylation is the major metabolic pathway in the metabolism of 4-chloro-1,2-dehydro-17 alpha-methyltestosterone, fluoxymesterone, and metandienone, whereas for boldenone, 17 alpha-methyltestosterone, and testosterone, 6 beta-hydroxylation is negligible.

Adult↗

PubMed1995

In vitro and in vivo genotoxicity of hormonal drugs. VI. Fluoxymesterone.

Genotoxic evaluation of a commonly used synthetic steroidal androgen, fluoxymesterone, was undertaken using a combination of in vitro and in vivo assays. The clastogenic potential of fluoxymesterone was evident from the chromosome aberrations and sister chromatid exchanges induced by it in the cultured human lymphocytes and also from the increased frequencies of micronuclei and sister chromatid exchanges in bone marrow cells of mice. However, in Ames Salmonella assay both with and without S9 mix and in host-mediated assay using bacterial strains of S. typhimurium as indicator organism, fluoxymesterone did not cause any significant increase/decrease in His+ revertants.

Animals↗

PubMed1975

Radioimmunoassay for fluoxymesterone (Halotestin).

A specific, sensitive, precise and accurate radioimmunoassay has been developed for fluoxymesterone, 9alpha-fluoro-11beta,17beta-dihydroxy-17-methyl-4-androsten-3-one (Halotestin). The method is capable of detecting 25 picograms of drug in 0.1 ml of unextracted serum. The primary antibody was prepared against fluoxymesterone 3-(0-(carboxy-methoxime)) (CMO) bovine serum albumin. The specificity of the assay is greatly influenced by the hydroxyl group at position 11 and the methyl group at position 17. Physiological levels of endogenous steroids did not cross-react significantly with the primary antibody. Blood levels of fluoxymesterone were determined in both human subjects and male beagle dogs after oral administration of Halotestin.

Animals↗

PubMed1979

Growth in Turner's syndrome: spontaneous and fluoxymesterone stimulated.

Spontaneous growth was analysed in a group of 55 girls with Turner's syndrome and various karyotypes. Their variation in height and its dependence on parental height were similar to that of normal girls. At all ages, the 45,X karyotype was associated with slightly greater mean stature than the other karyotypes together. The bone ages lagged progressively behind from 10 years onwards. Twenty-five patients aged between 9.1 and 17.2 years were given fluoxymesterone, 0.06-0.17 mg/kg daily, for at least 1 year. Their height velocities increased significantly. This brought about a clear psychological benefit. Their final heights were predicted before and after therapy, with a new method based on the spontaneous growth and bone maturation of our patients. The response was individually variable but, on average, the patients gained in predicted height from the therapy. This effect was not lost during a posttreatment year. Abnormal lowering of the voice occurred in patients receiving greater than or equal to 0.15 mg/kg fluoxymesterone daily, but never with less than 0.13 mg/kg. No other adverse effects appeared. Thus, fluoxymesterone is useful for promoting growth in girls with Turner's syndrome.

Adolescent↗

PubMed1999

Randomized comparison of megestrol acetate versus dexamethasone versus fluoxymesterone for the treatment of cancer anorexia/cachexia.

PURPOSE: Previous double-blind, placebo-controlled, randomized clinical trials have demonstrated that both corticosteroids and progestational agents do partially alleviate cancer anorexia/cachexia. Pilot information suggested that an anabolic corticosteroid might also improve appetite in patients with cancer anorexia/cachexia. The current trial was developed to compare and contrast a progestational agent, a corticosteroid, and an anabolic corticosteroid for the treatment of cancer anorexia/cachexia. PATIENTS AND METHODS: Patients suffering from cancer anorexia/cachexia were randomized to receive either dexamethasone 0. 75 mg qid, megestrol acetate 800 mg orally every day, or fluoxymesterone 10 mg orally bid. Patients were observed at monthly intervals to evaluate weight changes and drug toxicity. Patients also completed questionnaires at baseline and at monthly intervals to evaluate appetite and drug toxicities. RESULTS: Fluoxymesterone resulted in significantly less appetite enhancement and did not have a favorable toxicity profile. Megestrol acetate and dexamethasone caused a similar degree of appetite enhancement and similar changes in nonfluid weight status, with nonsignificant trends favoring megestrol acetate for both of these parameters. Dexamethasone was observed to have more corticosteroid-type toxicity and a higher rate of drug discontinuation because of toxicity and/or patient refusal than megestrol acetate (36% v 25%; P =.03). Megestrol acetate had a higher rate of deep venous thrombosis than dexamethasone (5% v 1%; P =.06). CONCLUSION: Whereas fluoxymesterone clearly seems to be an inferior choice for treating cancer anorexia/cachexia, megestrol acetate and dexamethasone have similar appetite stimulating efficacy but differing toxicity profiles.

Administration, Oral↗

PubMed1980

Tamoxifen and fluoxymesterone in advanced breast cancer: a controlled clinical trial.

Seventy-nine postmenopausal women with stage IV breast cancer and no previous endocrine therapy or chemotherapy received tamoxifen or fluoxymesterone in an open, randomized, cross-over trial. The overall remission rate was 30% with tamoxifen as the first course of treatment and 19% with fluoxymesterone as the first course of treatment. Bone metastases were seen in 21 patients receiving tamoxifen and in 20 patients receiving fluoxymesterone. There were six and five remissions in these two groups respectively. The time to the first change in therapy was significantly longer for the tamoxifen group (P = 0.003). The survival of the patients who received tamoxifen as the first course of endocrine treatment was better (P = 0.05).

Bone Neoplasms↗

PubMed1982

Treatment of anemia in myeloproliferative disorders: a randomized study of fluoxymesterone v transfusions only.

Previously untreated patients who had anemia (hemoglobin level, less than or equal to 10 g/dL) caused by myelofibrosis (MF) (16 patients) or other myeloproliferative disorders (13 patients) were given the opportunity to participate in a prospective randomized study-to be treated either with 30 mg/day of oral fluoxymesterone and necessary transfusions or by transfusions alone. Of the 24 patients whose data could be evaluated, four (29%) of 14 responded well to fluoxymesterone therapy (hemoglobin level rise, of greater than 2 to greater than 10 g/dL and relief of symptoms of anemia), whereas, in the transfusion arm, there were no good "responders"; one of ten patients was a partial "remitter" (responder), with a rise in the hemoglobin level of 1 to 2 g/dL. All responders to fluoxymesterone therapy showed a 50% or more maximum uptake of injected ferrous citrate Fe 59 into RBC hemoglobin, whereas no nonresponder met this criterion. All responders had MF (marrow more than one third replaced by collagen). There was no significant difference in survival of patients in the two arms of the study.

Aged↗

PubMed1993

Long-term results of treatment with low-dose fluoxymesterone in constitutional delay of growth and puberty and in genetic short stature.

This prospective study was designed to assess growth response, side effects, other possible long-term effects, and final adult height in boys treated with the oral androgen, fluoxymesterone. From 1973 to 1984, eighty-two short boys (71 with constitutional delay of growth and puberty [CDGP] and 11 with genetic short stature [GSS]) were treated with daily oral doses of 2.5 mg of fluoxymesterone from 6 to 60 months. Final height assessment was made from 1989 to 1991. A group of 34 untreated boys (26 with CDGP and 8 with GSS) were also followed to assess the accuracy of the Greulich-Pyle and Bayley-Pinneau (GP-BP) and sexual maturity index height prediction methods. During treatment, each patient had a 1.7- to 2.5-fold increase in linear growth velocity. Accelerated velocity (over baseline) continued as long as the bone age was less than 14 years. No adverse androgenic effects (or undue acceleration of puberty) were observed. Final height exceeded pretreatment predictions for CDGP + GSS by 6.1 +/- 3.5 (SD) cm (GP-BP) and 5.4 +/- 3.2 cm (sexual maturity index). It is concluded that a daily oral dose of 2.5 mg of fluoxymesterone can be used to accelerate linear growth in boys with CDGP and GSS when needed to alleviate emotional problems secondary to slow growth and short stature without fear of compromising final adult height.

Adolescent↗

PubMed1992

Fluoxymesterone as third line endocrine therapy for advanced breast cancer. A phase II trial of the Piedmont Oncology Association.

The Piedmont Oncology Association conducted a Phase II trial of fluoxymesterone (Halotestin) in 28 patients who failed to respond to prior hormonal therapy with tamoxifen and a progestational agent. Of nine patients who had responded to prior endocrine therapy, one had a partial response (PR) as defined by strict criteria and remains on study at 17 + months for an 11% response rate [95% confidence interval (CI), complete response (CR) + PR, 0-48%]. None of 19 previously unresponsive patients achieved remission (95% CI, CR + PR, 0-18%). Eleven patients' performance status deteriorated during therapy. Five of them had not received prior chemotherapy, and their response to subsequent chemotherapy may have been adversely affected. Third-line hormonal therapy with fluoxymesterone can be recommended only as a temporizing measure in patients with indolent disease who have responded to prior hormonal therapy.

Adult↗

PubMed1985

Constitutional delay of growth and puberty in boys: the effect of a short course of treatment with fluoxymesterone.

17 boys with delayed growth spurt, 9 of whom also had late puberty, were treated with 2.5 to 5.0 mg of fluoxymesterone daily for 0.23-0.58 years. Mean increment of growth velocity was 4.5 cm/year during treatment and this was maintained at 3.8 cm/year over a post-treatment observation period of 0.22-1.3 years. Mean testicular volume at the end of the treatment period was 9.9 ml. Mean height for bone age standard deviation score remained unchanged at -1.2 to -1.4 (not significant). We conclude that a low dose of fluoxymesterone may be used in safety for a short time to induce a growth acceleration in adolescent boys with constitutional delay of growth and puberty.

Adolescent↗

PubMed1982

Combination hormonotherapy with tamoxifen and fluoxymesterone in patients with advanced breast cancer relapsing on hormonotherapy.

33 patients were treated with a combination of tamoxifen and fluoxymesterone (10 mg t.i.d. each) after progression on prior hormonotherapy (HT). 6 of 22 patients (27%) exhibiting a partial response (PR) or stable disease (NC) on previous HT responded to the combination (median time to relapse 7 months, range 3.5 to 17+ months). 11 (50%) maintained NC (median duration 5 months, range 2% to 9.5 months). No response has been seen in 11 patients who experienced progressive disease during prior hormonal manipulation or who were not evaluable for response to prior HT. The overall response rate was 18% for the patient population as a whole (responders and nonresponders to previous HT), which most probably would be similar to the response rate if these patients received only fluoxymesterone.

Adult↗