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In spite of the fact that it is widely referred to as an antiandrogen in the literature, bifluranol is actually a pure estrogen and does not significantly bind to the androgen receptor or directly antagonize the action of androgens.[3] It exerts functional antiandrogen effects by binding to and activating the estrogen receptor in the pituitary gland, consequently suppressing the secretion of luteinizing hormone (and hence acting as an antigonadotropin) and thereby reducing gonadal androgen production and systemic androgen levels.[3] Bifluranol has also been found to act as a 17α-hydroxylase/17,20 lyaseinhibitor, though with less potency than ketoconazole, and this action may contribute to its efficacy in benign prostatic hyperplasia by further helping to lower androgen levels.[10][11][12]
^ abPope, D. J.; Gilbert, A. P.; Easter, D. J.; Chan, R. P.; Turner, J. C.; Gottfried, S.; Parke, D. V. (1981). "Bifluranol, a novel fluorinated bibenzyl anti-androgen, its chemistry and disposition in different animal species". Journal of Pharmacy and Pharmacology. 33 (1): 297–301. doi:10.1111/j.2042-7158.1981.tb13784.x. ISSN0022-3573. PMID6116777.
^Beacock, C. J. M.; Buck, A. C.; Roberts, E. E. (1985). "Bifluranol in the treatment of benign prostatic hyperplasia (BPH)". The Prostate. 7 (4): 357–361. doi:10.1002/pros.2990070403. ISSN0270-4137.
^Keane, P. F.; Timoney, A. G.; Kiely, E.; Williams, Gordon; Stamp, G. (1988). "Response of the Benign Hypertrophied Prostate to Treatment with an LHRH Analogue". British Journal of Urology. 62 (2): 163–165. doi:10.1111/j.1464-410X.1988.tb04299.x. ISSN0007-1331. PMID2457404.
^Barrie, S.E.; Rowlands, M.G.; Foster, A.B.; Jarman, M. (1989). "Inhibition of 17α-hydroxylase/C17-C20 lyase by bifluranol and its analogues". Journal of Steroid Biochemistry. 33 (6): 1191–1195. doi:10.1016/0022-4731(89)90429-9. ISSN0022-4731. PMID2559252.
^Jarman, Michael; John Smith, H.; J. Nicholls, Paul; Simons, Claire (1998). "Inhibitors of enzymes of androgen biosynthesis: cytochrome P45017α and 5α-steroid reductase". Natural Product Reports. 15 (5): 495. doi:10.1039/a815495y. ISSN0265-0568.
^Barrie, S.E.; Haynes, B.P.; Potter, G.A.; Chan, F.C.Y.; Goddard, P.M.; Dowsett, M.; Jarman, M. (1997). "Biochemistry and pharmacokinetics of potent non-steroidal cytochrome P45017α inhibitors". The Journal of Steroid Biochemistry and Molecular Biology. 60 (5–6): 347–351. doi:10.1016/S0960-0760(96)00225-7. ISSN0960-0760.
^Polska Akademia Nauk. Komitet Badania Polonii (1984). II Kongres Uczonych Polskiego Pochodzenia: zbiór materiałów. Zakład Narodowy im. Ossolińskich. ISBN978-83-04-01670-5. [This explains why the estrogenic activity is minimal in terms of pentafluranol or even bifluranol. Doses which shall apply from 1 to 6 days of pregnancy, are in micrograms per kg of body weight: bifluranol 80, 30 and terfluranol pentafluranol 280 ...]