What is Orgovyx (relugolix)?

Reviewed by: HU Medical Review Board

Orgovyx (relugolix) is the first oral gonadotropin-releasing hormone (GnRH) receptor antagonist therapy approved by the U.S. Food and Drug Administration to treat advanced prostate cancer in adults. This is prostate cancer that has spread beyond the prostate into the lymph nodes or other organs within the body.1

Orgovyx is a form of androgen deprivation therapy that lowers the levels of the hormones that help prostate cancer grow.1

What are the ingredients of Orgovyx?

The active ingredient of Orgovyx is relugolix.2

How does it work?

Orgovyx belongs to a class of drugs called gonadotropin-releasing hormone (GnRH) receptor antagonists. It blocks the GnRH receptors in the pituitary gland and prevents it from carrying out its regular function.

Normally, the GnRH receptors play a role in a bigger pathway that regulates hormone production. Specifically, it is involved in making hormones called follicle-stimulating hormone (FSH) and luteinizing hormone (LH). Both of these are important for producing and controlling testosterone levels in the body.2

Some prostate cancers are sensitive to testosterone. Specifically, testosterone causes them to grow or spread. By blocking GnRH receptors and subsequently other related hormones from being released, the production of testosterone can be slowed or stopped. This is also referred to as medical castration. By blocking testosterone production, cancer growth may be slowed as well.1,2

What are possible side effects?

The most common side effects of Orgovyx are similar to other testosterone-lowering drugs. These include:2

  • Hot flashes
  • Increase in blood sugar (blood glucose)
  • Muscle or joint pain
  • Anemia (low levels of hemoglobin)
  • Fatigue
  • Elevated liver function tests
  • Constipation and/or diarrhea
  • Increased fat in the blood (also called triglycerides)

Orgovyx many cause serious side effects, including changes in the electrical activity of your heart (QT prolongation) that can cause chest pain, dizziness or passing out, and/or heart palpitations.2

These are not all the possible side effects of Orgovyx. Talk to your doctor about what to expect or if you experience any changes that worry you.

Things to know

Tell your doctor about all your health conditions, including if you have any history of heart problems before starting Orgovyx. Your doctor may monitor your heart’s rhythm while you are taking the drug.1,2

Orgovyx can also cause harm to an unborn baby. People taking Orgovyx who have a partner who may become pregnant or who is pregnant are advised to use birth control (contraception) during treatment and for a period of time after the last dose of Orgovyx. Talk to your doctor about the right birth control options and how long you need to use them.2

Orgovyx may also interact with other drugs. Specifically, it interacts with drugs called P-glycoprotein (P-gp) and CYP3A inducers, as well as P-gp (P-glycoprotein) inhibitors. If you are unsure if a drug you are taking belongs to one of these classes, ask your doctor.1,2

Before taking Orgovyx, tell your doctor about any other drugs, vitamins, or supplements you are taking. This includes over-the-counter drugs.

For more information, read the full prescribing information of Orgovyx.

Written by: Casey Hribar | Last reviewed: December 2020

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