Bicalutamide

Casodex

Anti-Androgen HRT Oral FDA/EMA Label

Half-life

5.8 days

Time to Peak

31 hr

Steady State

~29 days

Dose Range

25–50 mg

Frequency

Daily

Overview

Non-steroidal anti-androgen (NSAA). Increasingly popular for transfem HRT as an alternative to CPA and spironolactone. Very long half-life (5.8 days) makes it forgiving of missed doses. Pure AR antagonist -- does NOT suppress testosterone production (actually increases T and E2 via feedback). Rare but serious hepatotoxicity risk -- monitor LFTs regularly, especially first 6 months.

Mechanism of Action

Pure androgen receptor antagonist. Blocks testosterone and DHT at the receptor without suppressing production. The R-enantiomer is the pharmacologically active form.

Dosing Information

Route	Dose Range	Half-life	Tmax	Frequency
Oral	25–50 mg	5.8 days	31 hr	Daily

Used in Regimens

1 regimen

EV + Bicalutamide Pathway

Estradiol valerate with bicalutamide non-steroidal anti-androgen. Bicalutamide blocks androgen receptors without affecting LH/FSH or testosterone production — testosterone remains high but its effects are blocked. Liver monitoring required. Growing in popularity as a spironolactone and CPA alternative.

Bicalutamide 25–50mg/day. Monitor liver function.

hrt_fem

Ancillary

Data Sources

FDA Label Casodex (bicalutamide) FDA Prescribing Information
Peer-reviewed Transfeminine Science: Bicalutamide in Transfeminine HRT

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