Pharmacokinetics and testosterone suppression of a single dose of polyestradiol phosphate (Estradurin®) in prostatic cancer patients

  title={Pharmacokinetics and testosterone suppression of a single dose of polyestradiol phosphate (Estradurin{\textregistered}) in prostatic cancer patients},
  author={Reinhard Stege and Per Olov Gunnarsson and Carl J. Johansson and Per Olsson and {\AA}ke Pousette and Kjell Carlstr{\"o}m},
  journal={The Prostate},
The pharmacokinetics and endocrine effects of polyestradiol phosphate (PEP; Estradurin®) were studied by determination of the concentrations of estradiol (E2), unconjugated (E1) and total estrone (tE1; ≥85% estrone sulfate), and testosterone in serum from 11 prostatic cancer patients after administration of a single intramuscular injection (320 mg). 

Pharmacodynamic model of testosterone suppression after intramuscular depot estrogen therapy in prostate cancer

A model is described predicting the effect on testosterone flux achieved with this estrogen drug, PEP, which has been in clinical use for several years in combination therapy and pharmacokinetically and clinically as a single treatment.

Time for revival of estrogens in the treatment of advanced prostatic carcinoma? Pharmacokinetics, and endocrine and clinical effects, of a parenteral estrogen regimen

The present pilot study tested the clinical performance of a new pharmacokinetically guided dosing regimen of parenteral estrogen in patients with advanced prostatic carcinoma. The aim was to

Parenteral polyoestradiol phosphate vs orchidectomy in the treatment of advanced prostatic cancer. Efficacy and cardiovascular complications: a 2-year follow-up report of a national, prospective prostatic cancer study. Finnprostate Group.

Parenteral PEP (240 mg/month) seems to be as efficient as orchidectomy in inhibiting disease in patients with advanced prostatic cancer, and the difference was statistically significant during the first year of treatment.

Flip-flop pharmacokinetics--delivering a reversal of disposition: challenges and opportunities during drug development.

The purpose of this article is to analyze both the pharmacokinetic interpretation errors and opportunities underlying the presence of flip-flop pharmacokinetics during drug development.

Vastly extended drug release from poly(pro-17β-estradiol) materials facilitates in vitro neurotrophism and neuroprotection

First-generation poly(pro-E2) biomaterial scaffolds that release E2 at nanomolar concentrations over the course of 1–10 years via slow hydrolysis in vitro demonstrate the first step towards next-generation implantable biomaterials with prolonged release and excellent regenerative potential.

Application of Pharmacokinetic-Pharmacodynamic Modeling in Drug Delivery: Development and Challenges

The basic PK-PD modeling theory in drug delivery is summarized and it is demonstrated how it had been applied to help the development of new delivery systems and modified large molecules and the linkage between PK and PD was highlighted.



Clinical pharmacology of polyestradiol phosphate

The results of the present studies demonstrate that intramuscular injections of polyestradiol phosphate (PEP) produce not only considerably increased estrogen concentration in plasma but also

Cardiovascular follow‐up of patients with prostatic cancer treated with single‐drug polyestradiol phosphate

Patients with cancer of the prostate treated with strict parenteral estrogen in the form of monthly polyestradiol phosphate injections have responded to therapy and there have been no cardiovascular complications at a mean follow‐up of 12.9 ± 0.7 months.

A comparison of androgen status in patients with prostatic cancer treated with oral and/or parenteral estrogens or by orchidectomy

Both estrogen treatment regimens were as effective as orchidectomy in reducing circulating levels of T and A‐4 and the more pronounced effects of oral estrogens on circulating adrenal androgens may reflect an altered liver metabolism associated with this route of administration.

Single‐drug parenteral estrogen treatment in prostatic cancer: A study of two maintenance‐dose regimens

Treatment of 17 patients with prostatic cancer with 320 mg polyestradiol phosphate (PEP) as intramuscular injections every fourth week suppressed serum testosterone (T) values to orchidectomy levels

Effect of parenteral oestrogen on the coagulation system in patients with prostatic carcinoma.

Parenteral administration of oestrogen caused a less marked change in the coagulation system than oral administration and should be the treatment of choice for prostatic carcinoma.

Orchidectomy versus oestrogen for prostatic cancer: cardiovascular effects.

The substantially increased risk of cardiovascular complications in patients given oestrogen for prostatic cancer warrants careful consideration when choosing treatment for this disorder.

The metabolism of estrogens in normal women after pulse injections of 3H-estradiol and 3H-estrone.

ABSTRACT 3H-estradiol was administered as a single pulse to 7 normal women between days 5–7 of their menstrual cycle. The disappearance from the blood of 3H as free estradiol in all 7 subjects could

Testicular and adrenocortical function in healthy men and in men with benign prostatic hyperplasia