|Trade names||Depostat, Primostat|
G03DA01 (WHO) |
|Synonyms||SH-582, SH-80582, NSC-84054; Gestonorone hexanoate, Gestronol hexanoate, Gestronol caproate, Norhydroxyprogesterone caproate; 17α-Hydroxy-19-norpregn-4-ene-3,20-dione hexanoate; 17α-hydroxy-19-norprogesterone hexanoate|
|Chemical and physical data|
|Molar mass||414.57752 g/mol|
|3D model (Jmol)||Interactive image|
Gestonorone caproate (INN, USAN, JAN) (brand names Depostat, Primostat), also known as gestronol hexanoate (BANM), as well as 17α-hydroxy-19-norprogesterone hexanoate or norhydroxyprogesterone caproate, is a synthetic, steroidal progestin of the 19-norprogesterone and 17α-hydroxyprogesterone groups. It is used in the treatment of sex hormone-dependent conditions such as benign prostatic hypertrophy and endometrial cancer. The drug was developed by Schering and has been marketed since at least 1973, and is available widely throughout Europe, including the United Kingdom, and is also marketed in Japan, China, Mexico, and other countries.
Gestonorone caproate is a strong, long-acting, and pure progestogen, possessing no androgenic, anabolic, antiandrogenic, estrogenic, antiestrogenic, corticosteroid, or teratogenic effects. In animals, it is approximately 25 times more potent than progesterone or hydroxyprogesterone caproate. In humans, 100 or 200 mg intramuscular gestonorone caproate is said to be equivalent to 1000 mg intramuscular hydroxyprogesterone caproate. Like other potent progestins, gestonorone caproate possesses potent antigonadotropic activity and is capable of markedly suppressing the gonadal production and circulating levels of sex hormones such as testosterone and estradiol. A clinical study found that 400 mg/week intramuscular gestonorone caproate suppressed testosterone levels by 75% in men. The drug is administered once weekly by intramuscular injection, via which it acts as a depot. Like the closely related progestins hydroxyprogesterone caproate and 19-norprogesterone, gestonorone caproate shows poor activity orally.
SH-834 was a combination of 90 mg estradiol valerate and 300 mg gestonorone caproate for weekly intramuscular injection that was developed by Schering in the 1970s. It was investigated clinically as a treatment for breast cancer and was found to be effective, but does not seem to have been marketed.
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The preparations used were Proluton Depot (17a-hydroxy-progesterone caproate) and in 3 patients SH 5132 (17a-hydroxy-19-norprogesterone caproate); 100 mg of the latter corresponds to 1000 mg of Proluton Depot.
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Thirteen patients with primary adenocarcinoma of the uterine corpus were treated for 21 days with l7alphahydroxy-progesterone-caproate (Primolut Depot@, Schering), 1000 mg daily, or 17alpha-hydroxy-19-nor-progesterone-caproate (DepostatB, Schering), 200 mg daily. These doses can be considered as equivalent.
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Another synthetic gestogen, 17-hydroxy-19-norprogesterone caproate (Depostat-Schering), 400 mg by i.m. weekly injections suppressed T levels to 25% of pretreatment values (Sander er al., 1978).
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Gestonorone caproate, another progestational agent, was investigated at our institution. Eighteen patients with painful metastatic [prostate cancer] with objective relapse after orchiectomy were treated with 400 mg/week i.m.
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Gestonorone [caproate] 100 or 200 mg/week i.m.
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A study was carried out in 30 male patients with benign prostate hyperplasia to assess the effectiveness of treatment with a progestational agent, gestonorone caproate (200 mg), given intramuscularly every 7 days over a period of 2 to 3 months.
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- Notter, G.; Berndt, G. (2009). "Hormonal Treatment of Mammary Carcinoma with Progynon-Depot and Depostat". Acta Radiologica: Therapy, Physics, Biology. 14 (5): 433–442. doi:10.3109/02841867509132684. ISSN 0567-8064.
- Ward, H. W. C. (1972). "PROGESTOGEN THERAPY FOR OVARIAN CARCINOMA". BJOG: An International Journal of Obstetrics and Gynaecology. 79 (6): 555–559. doi:10.1111/j.1471-0528.1972.tb14200.x. ISSN 1470-0328.
- Berndt, G.; Stender, H.-St. (2009). "[The combined estrogen-gestagen treatment of metastasizing mammary carcinoma using with SH 834]". 95 (48): 2399–2404. doi:10.1055/s-0028-1108843. ISSN 0012-0472.