Oxendolone was introduced for medical use in 1981.[8] It is used only in Japan.[8][11]
Medical uses
Oxendolone is used in the treatment of
benign prostatic hyperplasia (BPH) in
Japan.[8][11] It has been used at a dosage of 200 mg once every 2 weeks via
intramuscular injection.[17] Although it is approved for the treatment of BPH in Japan, concerns have been raised about its use for this condition due to poor efficacy seen in
clinical trials.[11]
The
acetateester of oxendolone is known as TSAA-328, while the
caproate ester of oxendolone is known as TSAA-330.[21] They were never marketed.[21]
History
Oxendolone has been marketed in
Japan by
Takeda since 1981.[8]
Society and culture
Generic names
Oxendolone is the
generic name of the drug and its
INNTooltip International Nonproprietary Name,
USANTooltip United States Adopted Name, and
JANTooltip Japanese Accepted Name.[7][22] It is also known by its developmental code name TSAA-291.[7][22]
Brand names
Oxendolone is or has been sold under the brand names Prostetin and Roxenone.[7][22]
^
abcHenkler G, Klotzbach M, Koch H, Müller W, Richter J (November 1982). "[Progress in the area of drug development. 15]". Die Pharmazie (in German). 37 (11): 753–765.
PMID6131442. [Oxendolone] has been clinically tested in Japan (weekly intramuscular injection of 200-400 mg) in prostatic hypertrophy.
^
abcHikichi Y, Yamaoka M, Kusaka M, Hara T (October 2015). "Selective androgen receptor modulator activity of a steroidal antiandrogen TSAA-291 and its cofactor recruitment profile". European Journal of Pharmacology. 765: 322–331.
doi:
10.1016/j.ejphar.2015.08.052.
PMID26335395. According to the clinical data of TSAA-291, the plasma level of TSAA-291 after weekly intramuscular administration at 400 mg/kg for 12 weeks is approximately 100 nM (Drug Information).
^
abcOstri P, Swartz R, Meyhoff HH, Petersen JH, Lindgård G, Frimodt-Møller C, et al. (1989). "Antiandrogenic treatment of benign prostatic hyperplasia: a placebo controlled trial". Urological Research. 17 (1): 29–33.
doi:
10.1007/bf00261046.
PMID2466359.
S2CID30551043. Thirty patients were treated with weekly injections of oxendolone 200 mg during a 3 months' period, and 30 patients were allocated to placebo treatment.
^
abcdeMidgley I, Fowkes AG, Darragh A, Lambe R, Chasseaud LF, Taylor T (April 1983). "The metabolic fate of the anti-androgenic agent, oxendolone, in man". Steroids. 41 (4): 521–536.
doi:
10.1016/0039-128x(83)90092-2.
PMID6419414.
S2CID41224726. After intramuscular administration of 16β-ethyl-17β-hydroxy-4-[4-14C] estren-3-one (14C-oxendolone; 300 mg) to 3 human subjects, [...]
^
abcKirby RS, Christmas T (1991). "The potential value of 5-alpha-reductase inhibition in the treatment of bladder outflow obstruction due to benign prostatic hyperplasia". World Journal of Urology. 9 (1).
doi:
10.1007/BF00184713.
ISSN0724-4983.
S2CID38790542.
^
abcBashirelahi N, Ganesan S, Ekiko DB, Young JD, Shida K, Yamanaka H, Takahashi E (September 1986). "Effect of 16 beta-ethyl-17 beta-hydroxy-4-estren-3-one (TSAA-291) on the binding of promegestone (R5020) and methyltrienolone (R1881) to hyperplastic and neoplastic human prostate". Journal of Steroid Biochemistry. 25 (3): 367–374.
doi:
10.1016/0022-4731(86)90249-9.
PMID2430141.
^
abSudo K, Yamazaki I, Masuoka M, Nakayama R (1979). "Anti-androgen TSAA-291. IV. Effects of the anti-androgen TSAA-291 (16 beta-ethyl-17 beta-hydroxy-4-oestren-3-one) on the secretion of gonadotrophins". Acta Endocrinologica. Supplementum. 229 (3 Supplb): 53–66.
doi:
10.1530/acta.0.092S053.
PMID294107.
^
abcKatayama T, Umeda K, Kazama T (November 1986). "[Hormonal environment and antiandrogenic treatment in benign prostatic hypertrophy]". Hinyokika Kiyo. Acta Urologica Japonica (in Japanese). 32 (11): 1584–1589.
PMID2435122.
^Dalton J, Gao W (2010). "Androgen Receptor". Nuclear Receptors: Current Concepts and Future Challenges. Proteins and Cell Regulation. Springer. pp. 143–182.
doi:
10.1007/978-90-481-3303-1_6.
ISBN978-90-481-3302-4.
^Wakeling AE, Furr BJ, Glen AT, Hughes LR (December 1981). "Receptor binding and biological activity of steroidal and nonsteroidal antiandrogens". Journal of Steroid Biochemistry. 15: 355–359.
doi:
10.1016/0022-4731(81)90297-1.
PMID7339263.
^Hikichi Y, Yamaoka M, Kusaka M, Hara T (October 2015). "Selective androgen receptor modulator activity of a steroidal antiandrogen TSAA-291 and its cofactor recruitment profile". European Journal of Pharmacology. 765: 322–331.
doi:
10.1016/j.ejphar.2015.08.052.
PMID26335395.
^
abMasuoka M, Masaki T, Yamazaki I, Hori T, Nakayama R (1979). "Anti-androgen TSAA-291. III. Hormonal spectra of anti-androgen TSAA-291 (16 beta-ethyl-17 beta-hydroxy-4-oestren-3-one) and its derivatives". Acta Endocrinologica. Supplementum. 229: 36–52.
doi:
10.1530/acta.0.092s036.
PMID294106.