Episode 310: Pharmacology 101: Androgen Receptor Inhibitors and Antiandrogens

“The things that I think creep up are things that unfortunately are quite common, and that’s hot flashes. I’ve had patients say that those are just overwhelming, and they want to go off therapy because of it. So I think talking about pharmacologic management, as well as lifestyle management, of hot flashes, are equally as important,” Rowena “Moe” Schwartz, PharmD, BCOP, FHOPA, professor of pharmacy practice at James L. Winkle College of Pharmacy at the University of Cincinnati in Ohio, told Jaime Weimer, MSN, RN, AGCNS-BS, AOCNS®, manager of oncology nursing practice at ONS, during a conversation about androgen receptor inhibitor and antiandrogen drug classes.

Music Credit: “Fireflies and Stardust” by Kevin MacLeod

Licensed under Creative Commons by Attribution 3.0 

Earn 0.5 contact hours of nursing continuing professional development (NCPD) by listening to the full recording and completing an evaluation at myoutcomes.ons.org by May 3, 2026. The planners and faculty for this episode have no relevant financial relationships with ineligible companies to disclose. ONS is accredited as a provider of NCPD by the American Nurses Credentialing Center’s Commission on Accreditation.

Learning outcome: Learners will report an increase in knowledge related to androgen receptor inhibitors and antiandrogens.

Episode Notes 

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Highlights From This Episode

“The androgen deprivation therapy is either orchiectomy, which we tend not to use as much anymore; LHRH agonists, meaning that they act like LHRH…and then now LHRH antagonists are taking an increased role because we now have an oral drug that is an LHRH antagonist.” TS 3:44

“When you give an LHRH agonist, you initially have an increase in testosterone, but over time you cause a decrease in the ability of the pituitary to produce luteinizing hormone. Therefore, you get decreased stimulation in the testes to produce androgens. So when you think of an LHRH agonist, by continual use, what you do—you get an initial surge and then a decrease overall if patients stay on the drug. And so LHRH agonists—leuprolide, goserelin, triptorelin—those are agents that are agonist. LHRH antagonists have a direct effect to block the receptor and decrease release of luteinizing hormone and follicle-stimulating hormone, ultimately decreasing testosterone. LHRH antagonists don't have that surge of testosterone. They have an immediate effect of decreasing testosterone.” TS 4:41

“In terms of the LHRH antagonists, we’ve only had one drug for a while that’s an antagonist. That’s degarelix. Recently there was the approval of relugolix, which is an oral LHRH antagonist. And that has shown to have great effect in a noninferiority trial in terms to the LHRH agonists. And also there’s some benefit with decreased cardiovascular risk with that drug. So I think this is the drug we’re starting to see more and more.” TS 7:01

“The other thing with abiraterone acetate, it is recommended by labeling to take on an empty stomach at least an hour before two hours after a meal. But there is data that you can use a lower dose with a low-fat meal, and so you will see many providers providing a lower dose, often to get around the cost issue sometime around the pill burden. And that needs to be taken with a low-fat meal. So I have patients who are on the lower dose. We’ve talked about taking it with a low-fat meal. Now specialty pharmacy has talked about it. And then they read stuff that’s online or in the literature and they’re like, ‘Oh, I shouldn’t be taking this with any food at all.’ So it’s really important to make sure that you educate patients how to take the medication and warn them if there’s different instruction out there than what you’re giving.” TS 16:47

“Adherence to the schedule—a lot of times people are getting LHRH agonists every three months. … Maybe you’re going to miss it this month. You miss one dose—that’s six months. So it’s really important that if people are going to not be able to get their injection, that they call, and it’s rescheduled, and they have a mechanism to make sure that you don’t lose people to follow up. So adherence to all therapy—essential.” TS 21:27

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