Bicalutamide Information

Sourcing this medication can be found here.

Rare instances of liver toxicity/damage have been reported with this medication and it is therefore recommended to monitor your liver enzymes (ALT/AST) once a year.

Bicalutamide functions as an anti-androgen by competing with testosterone and blocking its activity at the androgen receptor. While it is commonly prescribed as an anti-androgen, its usage is less common within the United States.


Dose Amount Per Day Amount Every Other Day
Minimum 25mg daily 50mg bi-daily
Typical Starting 50mg daily 100mg bi-daily
Maximum Dose 50mg daily 100mg bi-daily
Maximum Safe 100mg daily 200mg bi-daily
  • There is no reason to go above the maximum dose when taken in conjunction with estrogen.
  • Some people use bicalutamide mono-therapy, information on the topic can be found here.


Adjusting bicalutamide dose from the starting dose is typically not needed, however there are some blood tests you should monitor.


Liver tests should be done at least six months after starting and once a year after, and it can be afforded three months in, six months in, and every six months after.

AST Normal Ranges: 8-33 U/L (Cleavland Clinic).
ALT Normal Range: 7-56 U/L (Cleavland Clnic).

Ranges on liver tests can vary significantly depending on demographics, however if out of range discontinue the medication and consult with a doctor (in these situations switching to injection monotherapy might be best).


Bicalutamide does not decrease blood levels of testosterone and may actually cause them to increase as the body tries to compensate for the reduction of androgen receptor activity. This is not a cause for concern. (Randolph John, 2018).

Safety and Effects

Bicalutamide and Liver Toxicity

These symptoms can be a major sign that you are experiencing a acute problem with your liver, if you are experiencing these please see a doctor:

  • Yellowing of the skin and eye whites (jaundice)
  • Abdominal pain in the upper right portion of the abdomen
  • Dark or tea-colored urine.

This list is not conclusive however these signs are serious indicators of liver issues (others are detailed in the source) Mayo Clinic.

The risk for liver toxicity in prostate cancer patients is small (one in four thousand); this risk of liver toxicity in transgender patients taking a much smaller dose as an anti-androgen is undoubtedly significantly lower, but this risk has not been studied. If possible, doing a liver panel after long-term use of bicalutamide is a good idea. (Aly 2020).