Bicalutamide

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Bicalutamide
Skeletal formula for Bicalutamide; a commonly prescribed antiandrogen.
Drug class: Antiandrogen
Dosage range: Oral: 25–100 mg/day
Brand names: Casodex, Calutide
Elimination half-life: Single-dose: 5.8 days

Continuous: 7–10 days

Bicalutamide is an antiandrogen medication that is primarily used to treat prostate cancer. However, it is also commonly prescribed to transgender women as a means of reducing the influence of testosterone and dihydrotestosterone by acting as an antagonist of the androgen receptors and assisting them in their transition.

Method of action

Bicalutamide acts as a highly selective competitive silent antagonist of androgen receptors, the major biological target of the sex hormones testosterone and DHT, and hence is an antiandrogen.[1] In laymen's terms, this means that bicalutamide fits into a hormone receptor and essentially does nothing while simultaneously blocking testosterone and DHT from fitting into said receptor and exerting their effects.

Due to its selectivity for testosterone-related androgen receptors, bicalutamide does not interact importantly with other hormone receptors and hence has no clinically relevant off-target hormonal activity (e.g., progestogenic, estrogenic, etc).[2]

Unlike many other common antiandrogens such as spironolactone, bicalutamide neither suppresses nor inhibits testosterone production in the body. It therefore exclusively mediates its antiandrogenic effects by simply blocking testosterone, not from being produced, but from being able to exert any effects upon its relevant receptors. Bicalutamide is generally well tolerated and has substantially fewer side effects when compared to other more commonly used antiandrogens.

When taking bicalutamide, testosterone levels are elevated because it also blocks testosterone in the hypothalamus, which then senses the lack of hormones and up-regulates production. This has the added benefit of raising estrogen levels, as its inability to halt the production results in an excess amount of testosterone which is then converted to estrogen in a process called aromatization.[3]

Consequently, we here at DIY HRT Wiki thus recommend the use of bicalutamide over other blockers whenever possible.

Potential side effects

Frequency Class Side effect
Very common
(≥10%)
Reproductive system
and breast disorders
Breast tenderness
Gynecomastia
Common
(≥1% and <10%)
General and psychiatric
disorders
Asthenia
Decreased libido
Erectile dysfunction
Hot flashes
Skin and subcutaneous
tissue disorders
Decreased body hair
Hepato-biliary disorders Elevated liver enzymes
Uncommon
(≥0.1% and <1%)
Immune system disorders Hypersensitivity reactions,
(angioedema and hives)
Rare (<0.1%)
and unknown
Respiratory, thoracic, and
mediastinal disorders
Interstitial lung disease
Skin and subcutaneous
tissue disorders
Sensitivity to light
Hepato-biliary disorders Liver toxicity

Dosage

The standard starting dosage for bicalutamide is 50 mg, but this may have to be adjusted based on the results of blood tests. Because bicalutamide increases the production of testosterone, blood tests may not correctly reflect the amount of testosterone that is actually exerting an effect on your endocrine system. The up-regulation of the HPG axis can be mitigated in most people by making sure your estradiol levels stay at 200 pg/mL or higher. Once testosterone levels reach >100 ng/dL, bicalutamide dosage can be halved from the standard of 50 mg/day to 25 mg/day. In some rare cases, higher dosages may be required to completely block the uptake of dihydrotestosterone and testosterone. Users have been taking upwards of 100 mg/day in these cases.

Brand names

Bicalutamide is marketed by a company known as "AstraZeneca" in oral tablet form under the brand names Casodex, Cosudex, Calutide, Calumid, and Kalumid in many countries. It is also marketed under the brand names Bicadex, Bical, Bicalox, Bicamide, Bicatlon, Bicusan, Binabic, Bypro, Calutol, and Ormandyl among others in various countries. The drug is sold under a large number of generic trade names such as Apo-Bicalutamide, Bicalutamide Accord, Bicalutamide Actavis, Bicalutamide Bluefish, Bicalutamide Kabi, Bicalutamide Sandoz, and Bicalutamide Teva as well. A combination formulation of bicalutamide and goserelin is marketed by AstraZeneca in Australia and New Zealand under the brand name ZolaCos-CP.

Sources

Online pharmacies

Product Price Bulk Website Shipping
Bicalutamide 150mg x 28 67.85$ Pilloid Ships from russia
Bicalutamide 150mg x 30 60.00€ EU-Aibolit Ships from Germany/EU
Bicalutamide 50mg x 28 25.15$ Pilloid Ships from Russia
Bicalutamide 50mg x 30 35.00€ EU-Aibolit Ships from Germany/EU
Binarex 50mg x 28 66.00$ 47.67$ InHousePharmacy Ships from Vanuatu (Oceania)
Calutide 50mg x 10 20.93$ 19.47$ UnitedPharmacies (US-Centric)
Calutide 50mg x 10 17.21£ 16.01£ UnitedPharmacies-UK (UK-Centric)
Calutide 50mg x 10 18.95€ 17.63€ UnitedPharmacies-NL (NL-Centric)
Calutide 50mg x 30 59.63$ 53.90$ AllDayChemist Various worldwide centers
Calutide 50mg x 30 82.50$ 67.50$ InHousePharmacy Ships from Vanuatu (Oceania)
Calutide 50mg x 30 35.06€ InHome-Health Ships from UK/NL/Thailand
Casodex 150mg x 28 100.00€ 90.00€ Shape Shifter Ships from Turkey
Casodex 50mg x 28 50.00€ 43.34€ Shape Shifter Ships from Turkey
Casodex 50mg x 28 31.30€ Aphrodite's Ships from Portugal
Prolacut 50mg x 28 30.38$ 28.25$ UnitedPharmacies (US-Centric)
Prolacut 50mg x 28 24.98£ 23.23£ UnitedPharmacies-UK (UK-Centric)

Alibaba

Bicalutamide 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

References

  1. Shankar M. Singh, Sylvain Gauthier and Fernand Labrie, “ Androgen Receptor Antagonists (Antiandrogens) Structure-Activity Relationships”, Current Medicinal Chemistry (2000) 7: 211. https://doi.org/10.2174/0929867003375371
  2. B.J.A. Furr, Ph.D., H. Tucker, Ph.D. (JANUARY 01, 1996) "The preclinical development of bicalutamide: pharmacodynamics and mechanism of action" DOI: https://doi.org/10.1016/S0090-4295(96)80003-3
  3. Testosterone and Aromatization: How To Avoid Excess Estrogen Production (Blaineywellness.com) | https://www.blaineywellness.com/wp-content/uploads/2016/08/testosterone-and-aromatization-how-to-avoid-excess-estrogrogen-production.pdf