Bicalutamide has no established safety guidelines.

When I asked my first HRT (Hormone Replacement Therapy) doctor about trying Bicalutamide 50mg they simply said no. That first doctor was Plume in case you are trying to use Plume to get your hands on Bicalutamide – they will flatly decline for safety concerns.

The thing about Bicalutamide is that there are not a lot of formal cases of liver failure or mortality directly caused by it. The heart failure cases are tossed into the “Androgen Deprivation” pile. The liver failure cases are few and far between and thrown in the “They survived” or “It was probably from previous antiandrogen medications, not Bicalutamide”. It’s a bit up in the air, but it’s important to note that the known cases are only the known cases – they do not encapsulate every mortality that has happened from Bicalutamide.

I understand why Plume said no… but that didn’t stop me. I just switched to another doctor and got my hands on a prescription. I don’t think that was the wrong call, even though Bicalutamide ended up being incompatible for me. Here is my write up about what happened to me:

I want to be totally clear, I am not trying to argue for or against Bicalutamide safety. I am only writing this article to help people be informed about the evidence that is known.

Let’s dive into some details about the worst known cases:

By day 8 of bicalutamide therapy, AST was 2510 IU/L (9-37 IU/L), ALT 2379 IU/L (5-38 IU/L), total bilirubin 6.2 mg/dl (0.2-1.1 mg/dl) and INR 2.5 (0.9-1.1). Serum calcium was within normal limits, toxicology and viral serologies were negative, and iron studies excluded hemochromatosis. Ultrasound of the liver did not reveal any significant changes. Given the recent initiation of bicalutamide, it was discontinued. Total score using The Council for International Organizations of Medical Sciences/Roussel Uclaf Causality Assessment Method (CIOMS/RUCAM scale) for evaluating likelihood of drug induced liver injury (DILI) was 6 implying a probable link between the liver injury and bicalutamide therapy. His liver function and mental status continued to deteriorate and he subsequently died of fulminant hepatic failure 5 days after cessation of bicalutamide.

A total of 7 case reports of bicalutamide-associated hepatotoxicity or liver failure, two of which were fatal, have been published in the literature as of 2018.[114][103][115] One of these cases occurred after two doses of bicalutamide, and has been said to more likely to have been caused by prolonged prior exposure of the patient to flutamide and CPA.[103][105][116][117][118] In the reported cases of bicalutamide-associated hepatotoxicity, the dosages of the drug were 50 mg/day (three), 80 mg/day (one), 100 mg/day (one), and 150 mg/day (two).[114][115]

Details from the mention in Wikipedia:

A 60 year old man with prostate cancer developed acute liver failure following two doses of bicalutamide and a few days after stopping a 3 month course of flutamide. Liver test results were reported to be normal at the time of diagnosis of prostate cancer. Following an initial month of therapy with cyproterone acetate, flutamide and monthly subcutaneous goserelin acetate was started. Although flutamide was well tolerated, it was discontinued after 3 months and bicalutamide was substituted. After the second dose of bicalutamide, the patient developed jaundice and confusion. All medications were stopped and he was admitted for evaluation and therapy.

I brought up these citations in the Dr. Will Powers subreddit, but no one seemed to care even a little:

It was pointed out by one person that Tylenol has far more cases of liver failure/mortality than Bicalutamide. That is again not what I’m trying to accomplish by bringing this up, I’m not interested in a “what about” rebuttal, which is frankly not productive or the point.

The thing that rubs me the wrong way is that there are no established guidelines for introduction and monitoring for Bicalutamide in any literature. The closest mention in research is a retrospective note that monitoring the liver might have prevented some of the cases of liver failure. OK, so how do we monitor the liver?

Here are the fairly arbitrary guidelines I came up with for myself:

My doctor who prescribed the Bicalutamide decided a 1 month lab would make sense. My elaboration would be:

  • Labs should include ALT, AST, Albumin
  • Signs of Androgen Deprivation might be found in Cholesterol panel as well; which correspond with overall heart failure/mortality
  • Perform labs every 30 days for the first 3 months, then every 90 days afterward

What am I basing this on? Common sense and a little feedback from my doctor… so mostly nothing in particular, because there are no guidelines!

Here is what Wikipedia has to say about monitoring:

Bicalutamide monotherapy has been associated with abnormal liver function tests such as elevated liver enzymes in 3.4% of men relative to 1.9% for standard care.[20][107] Hepatic changes such as marked increases in liver enzymes or hepatitis that necessitated discontinuation of bicalutamide have occurred in approximately 0.3 to 1% of men in clinical trials.[19][26] Monitoring of liver function during treatment is recommended, particularly in the first few months.[20][92] In men of advanced age with prostate cancer, bicalutamide monotherapy has been associated with an increase in non-prostate cancer mortality, in part due to an increase in the rate of heart failure.[108][20] These mortality-related effects are thought to be a consequence of androgen deprivation, rather than a specific drug-related toxicity of bicalutamide.[109]

I hope if a patient or doctor stumbles on this post, it might be helpful to inform therapy and monitoring, at least slightly better than the totally unspecific literature I could find.

Note: I am not a medical professional, doctor, nurse, etc. I’m just a person who decided to try Bicalutamide with high hopes and a little apprehension. As cited near the beginning of this article, Bicalutamide did not work out well for me personally, but I don’t think that should deter anyone looking for a typically low adverse reaction antiandrogen from trying it.

Leave a Reply

Your email address will not be published. Required fields are marked *