Disease relevance of D00946

• Low-dose continuous oral fosfestrol is highly active in 'hormone-refractory' prostate cancer [1].
• Phase I trial of high-dose fosfestrol in hormone-refractory adenocarcinoma of the prostate [2].
• 6 dosages of diethylstilbestrol-diphosphate (DES-dp), ranging from 0.01 to 500 mg per kg of body weight were compared to saline and phosphate buffered saline (negative controls) and two dosages of cyclophosphamide (positive control) in the micronucleus test with 115 ICR mice [3].
• The usefulness of diethylstilbestrol-diphosphate for prostate cancer patients with lymph node metastasis is emphasized [4].
• Fosfestrol-induced porphyria cutanea tarda [5].

High impact information on D00946

• The median duration of prior treatment was 20 months and the median PSA at fosfestrol start was 126 ng/ml (range 8-12,800); symptoms (pain) were present in 73% of patients [1].
• Bioavailability, distribution and pharmacokinetics of diethystilbestrol produced from stilphostrol [6].
• The other modification separates stilphostrol and DES using a reversed-phase, ion-paired high-performance liquid chromatographic method followed by alkaline phosphatase hydrolysis followed by the GC-MS method [7].
• Cytogenetic effects of diethylstilbestrol-diphosphate (DES-dp) on mouse bone marrow monitored by the micronucleus test [3].
• Eleven patients with terminal metastatic prostatic carcinoma were selected for a pilot study to evaluate how effective diethylstilbestrol diphosphate (Stilphostrol) and cylcophosphamide (Cytoxan) are in this disease [8].

Chemical compound and disease context of D00946

• This study reports--for the first time--a capillary electrophoretic method for the determination of fosfestrol, a synthetic estrogen used in the treatment of metastatic prostate cancer [9].
• The pharmacokinetics of fosfestrol and diethylstilbestrol in chronic hemodialysis patients with prostate cancer [10].

Biological context of D00946

• Diethylstilbestrol-diphosphate induces chromosomal aberrations but not sister chromatid exchanges in murine bone marrow cells in vivo [11].

Anatomical context of D00946

• Up to 300 mg/kg of fosfestrol the induction of mutations occurs exclusively in spermatozoa [12].

Associations of D00946 with other chemical compounds

• Assay of the synthetic estrogen fosfestrol in pharmaceutical formulations using capillary electrophoresis [9].

Analytical, diagnostic and therapeutic context of D00946

• Half received daily subcutaneous injections of 10 mug diethylstilbestrol-diphosphate (DES-DP) in saline for up to 3 wk and half daily saline injections [13].
• RESULTS: Serum fosfestrol levels increased rapidly after the drip infusion was started and remained at high levels during infusion, but fell quickly after the treatment ended [10].
• Fosfestrol was quickly eliminated from the blood after hemodialysis was started, while DES remained in the blood during hemodialysis [10].

References