Bicalutamide
 |
This article is a rough draft! This means that although usable, the article may be missing citations, contain grammar errors, and likely still needs to be expanded upon. |
| 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 |
| 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.
- Common Packaging Designs of Bicalutamide
Casodex branded boxes.
Calutide branded box.
A generic branded box.
Various assorted brands.
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
- Bicalutamide (Casodex) as an Antiandrogen for Transgender Women Megathread (Reddit.com)
- Bicalutamide (Wikipedia.org)
- Bicalutamide (MedlinePlus.gov)
- Bicalutamide (Webmd.com)
- 9channel /hrt/ Spreadsheet of Hormones and Prices
- HRT.Cafe
References
- ↑ 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
- ↑ 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
- ↑ 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