Cyproterone Acetate

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Cyproterone acetate (CPA) is an antiandrogen and progestin medication that is primarily used to treat androgen-dependent conditions and as a component of hormone replacement therapy for transgender women. CPA is not approved for use in the United States, but is commonly available and prescribed in most other parts of the country.[1] It's commonly taken orally once every 3 days or up to three times daily and may also be administered by intramuscular injection. One speculation of CPA is that it may hinder breast growth due to early exposure to progestins, however this has not been proven and is purely speculation.

Cyproterone Acetate
Skeletal formula for Cyproterone Acetate; an antiandrogen and mild progestin.
Drug class: Antiandrogen, Progestogen, Progestin
Dosage range:
10 - 100 mg/day
300 mg once every 4 weeks
Brand names: Androcur, Androcur Depot, Cyprostat, Siterone
Elimination half-life:
1.6–4.3 days
3–4.3 days

Method of Action

Antiandrogen effects

Cyproterone acetate functions as a potent antiandrogen by reducing the production of testosterone and working as a weak competitive antagonist of the androgen receptor.[2] This means it binds to the androgen receptors and does nothing, preventing androgens like testosterone and dihydrotestosterone from binding and exerting their effects on the body. The strength of the antiandrogenic activity depends on how much is taken. Relatively high doses of CPA are required for clinically important AR antagonism.[3] It's generally not recommended that you take large dosages of CPA as the high progestogenic activity can cause adverse side effects. [4]

Despite the fact that higher doses of CPA are necessary for considerable systemic AR antagonistic activity, it's worth noting that even low doses of CPA are able to antagonize AR signaling in the liver.[5] This is believed to be because the first-pass metabolism of oral CPA raises SHBG levels by 300 to 400%, whereas birth control pills containing various other progestins, with either androgenic or antiandrogenic activity, only increase SHBG levels by 50 to 300%.[5]

Side Effects

The use of CPA may result in the following side effects:

  • Hypogonadism (low sex-hormone levels)
    • Sexual dysfunction
    • Infertility
    • Osteoporosis
  • Breast tenderness and enlargement
  • Fatigue
  • Depression
  • Vitamin B12 deficiency
  • Elevated liver enzymes
  • Glucocorticoid effects
  • Weight gain at high doses

Although rare, CPA may cause the following at very high doses:

  • Blood clots
  • Liver toxicity
  • High prolactin levels
  • Benign brain tumors
  • Prolactinomas

Many of these side effects can be mitigated by taking CPA with an estrogen, as most trans women will. Be advised that CPA may cause adrenal insufficiency when use of it is halted.


The usual starting dose is 12.5 mg to 25 mg daily between one to two doses. This is usually enough for most people to reach female ranges of testosterone. Hormone levels should be monitored through blood tests to ensure you are receiving the appropriate dosages. Be very careful when administering CPA yourself and make sure to supplement vitamin B12 if you plan to take this medication.

Brand Names

Cyproterone acetate is marketed under the brand name Androcur. There is also a brand of CPA with ethinylestradiol that is sold under the names Diane or Diane-35. Some of the other brand names for CPA include: Androcur Depot, Androstat, Asoteron, Cyprone, Cyprostat, and Siterone. There are combinations of CPA with estradiol valerate that are marketed under the names Climen, Climene, Elamax, and Femilar.


Product Price Bulk Website Shipping
Aldactone 100mg x 20 27.00$ 21.60$ AllRealMedications Ships from Turkey
Aldactone 100mg x 30 16.80£ Aphrodite's Ships from Portugal
Aldactone 100mg x 30 14.04$ 11.60$ AllDayChemist Various worldwide centers
Aldactone 100mg x 96 60.00€ 52.50€ ShapeShifter Ships from Turkey
Aldactone 25mg x 15 3.16$ 2.85$ UnitedPharmacies (US-Centric)
Aldactone 50mg x 90 29.50$ 21.63$ InHousePharmacy Ships from Vanuatu (Oceania)
Hyles 100mg x 10 15.90€ 12.72€ ThailandPharmacy Ships from Thailand
Hyles 100mg x 10 4.45$ 4.05$ FabSkinHouse Ships from Thailand
Hyles 100mg x 100 49.99$ Request Amazon4Health Ships from Thailand
Hyles 25mg x 10 6.00€ 4.80€ ThailandPharmacy Ships from Thailand


Spironolactone can be purchased in tablet form through a variety of sources such as online pharmacies. However, it can also be purchased in bulk powdered form through vendors on websites such as Alibaba. From personal experience, Alibaba is substantially cheaper and some vendors will often go to great lengths to get your product to you by deliberately mislabelling packages in order to more easily get them through customs. We have personally had good luck with this particular vendor. It is also worth noting that in order to purchase products from these sites, you will need to personally contact the vendor and negotiate a price with them.

See also

External links


  1. Barradell, L.B., Faulds, D. Cyproterone. Drugs & Aging 5, 59–80 (1994).
  2. Figg W, Chau CH, Small EJ (14 September 2010). Drug Management of Prostate Cancer. Springer. p. 71. ISBN 978-1-60327-829-4.
  3. E. Pucci & F. Petraglia (1997) Treatment of androgen excess in females: Yesterday, today and tomorrow, Gynecological Endocrinology, 11:6, 411-433, DOI: 10.3109/09513599709152569
  4. | Cyproterone acetate dosage: low doses are maximally effective for testosterone suppression while higher doses are unnecessary and have greater risks and side effects by u/Alyw234237 |
  5. 5.0 5.1 Sitruk-Ware R (April 2004). "Pharmacological profile of progestins". Maturitas. 47 (4): 277–83. doi:10.1016/j.maturitas.2004.01.001. PMID 15063480.