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Panomifene (PAN) /E/-1,2,-diphenyl-1-[4-[2-(2-hydroxyethylamino)-ethoxy]-phenyl]-3, 3,3-trifluoropropene is a new original Hungarian compound and is a tamoxifen (TMX) analog. In the phase I/a study presented here the human tolerance, pharmacokinetics and endocrine effects of a single oral dose of panomifene were evaluated in healthy, post-menopausal, female volunteers. As to the dose escalation, pharmacokinetic studies were carried out at doses of 24, 48 and 96 mg in two volunteers, and 120 mg in one volunteer. To find a suitable dose or dose range, for further evaluation of the drug detailed pharmacokinetics were performed at a selected dose level (24 mg) in 10 volunteers. The pharmacokinetic study showed considerable interindividual variability of the parameters, and only a medium correlation between dose and AUC (r=0.876). At the selected dose level (24 mg p.o.) the peak concentration of the plasma was 67.7 +/- 17.4 ng/ml (Cmax(meas)), the time to peak was 3.6 +/- 1.8 h (t[max(meas)]). The mean of the terminal half-life was 70.0 +/- 23.1 h (t(1/2beta)). The area under the plasma concentration time curve (AUC) calculated by the kinetic equation (AUCcalc) was 4814 +/- 1172 and by the trapezoidal rule (AUCtrap) was 4612 +/- 1357 (ng/ml) h.
V Erdélyi-Tóth, and
F Gyergyay, and
I Számel, and
E Pap, and
J Kralovánszky, and
E Bojti, and
M Csörgo, and
S Drabant, and
I Klebovich
May 2006,
Cancer chemotherapy and pharmacology,
V Erdélyi-Tóth, and
F Gyergyay, and
I Számel, and
E Pap, and
J Kralovánszky, and
E Bojti, and
M Csörgo, and
S Drabant, and
I Klebovich
November 2011,
International journal of clinical pharmacology and therapeutics,
V Erdélyi-Tóth, and
F Gyergyay, and
I Számel, and
E Pap, and
J Kralovánszky, and
E Bojti, and
M Csörgo, and
S Drabant, and
I Klebovich
April 2016,
Cancer chemotherapy and pharmacology,
V Erdélyi-Tóth, and
F Gyergyay, and
I Számel, and
E Pap, and
J Kralovánszky, and
E Bojti, and
M Csörgo, and
S Drabant, and
I Klebovich
May 2022,
The Journal of clinical endocrinology and metabolism,
V Erdélyi-Tóth, and
F Gyergyay, and
I Számel, and
E Pap, and
J Kralovánszky, and
E Bojti, and
M Csörgo, and
S Drabant, and
I Klebovich
January 1997,
Drugs under experimental and clinical research,
V Erdélyi-Tóth, and
F Gyergyay, and
I Számel, and
E Pap, and
J Kralovánszky, and
E Bojti, and
M Csörgo, and
S Drabant, and
I Klebovich
June 2002,
Journal of molecular neuroscience : MN,
V Erdélyi-Tóth, and
F Gyergyay, and
I Számel, and
E Pap, and
J Kralovánszky, and
E Bojti, and
M Csörgo, and
S Drabant, and
I Klebovich
May 2007,
Phytomedicine : international journal of phytotherapy and phytopharmacology,
V Erdélyi-Tóth, and
F Gyergyay, and
I Számel, and
E Pap, and
J Kralovánszky, and
E Bojti, and
M Csörgo, and
S Drabant, and
I Klebovich
January 2023,
Skin pharmacology and physiology,
V Erdélyi-Tóth, and
F Gyergyay, and
I Számel, and
E Pap, and
J Kralovánszky, and
E Bojti, and
M Csörgo, and
S Drabant, and
I Klebovich
January 1985,
Arzneimittel-Forschung,
V Erdélyi-Tóth, and
F Gyergyay, and
I Számel, and
E Pap, and
J Kralovánszky, and
E Bojti, and
M Csörgo, and
S Drabant, and
I Klebovich
January 2023,
Drug design, development and therapy,
