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Relugolix

Generic name: relugolix
Brand name: Orgovyx
Dosage form: oral tablet
Drug class: Gonadotropin-releasing hormone antagonists

Medically reviewed by N. France, BPharm. Last updated on Apr 28, 2022.

What is relugolix?

Relugolix is a prescription medicine used to treat adults with advanced prostate cancer, which comes as a tablet.

Relugolix belongs to a class of drugs called gonadotropin-releasing hormone (GnRH) receptor antagonists. In 2020, it was the first oral drug in its class to be approved by the US Food and Drug Administration (FDA) for prostate cancer patients.

Most prostate cancers need an androgen or sex hormone called testosterone to help them grow. Relugloix works by binding to GnRH receptors in your pituitary gland, which reduces how much luteinizing hormone (LH) and follicle-stimulating hormone (FSH) they release. This deceases the amount of testosterone produced and helps to slow or stop the spread of the cancer cells that rely on this hormone for their growth.

What is relugloix used for?

Relugolix is used in adults for the treatment of advanced prostate cancer.

It is not known if relugolix is safe or effective in females.

It is not known if relugolix is safe or effective in children.

What should I tell my doctor before taking relugolix?

Before taking relugolix, tell your healthcare provider about all of your medical conditions, including if you:

  • have any heart problems, including a condition called long QT syndrome.

How should I take relugolix?

  • Take relugolix exactly as your healthcare provider tells you.
  • Take 3 relugolix tablets on your first day of treatment. After that, take 1 relugolix tablet each day.
  • Take relugolix at about the same time each day.
  • Take relugolix with or without food.
  • Swallow relugolix tablets whole. Do not crush or chew tablets.
  • Your healthcare provider may change your dose if needed.
  • Do not change your dose or stop taking relugolix without talking with your healthcare provider first.

What happens if I miss a dose?

If you miss a dose of relugolix, take it as soon as you remember. If the dose was missed by more than 12 hours, the missed dose should not be taken. Take your next dose at your regular time the next day.

Dosing information

The recommended dose of relugolix is a loading dose of 360 mg on the first day of treatment followed by 120 mg taken orally once daily, at approximately the same time each day.

Relugolix can be taken with or without food. The tablets must be swallowed whole and not crushed or chewed.

See full prescribing information for further details about relugolix dosing.

What are the side effects of relugolix?

Relugolix may cause serious side effects, including:

  • Changes in the electrical activity of your heart (QT prolongation). Your healthcare provider may check your body salts (electrolytes) and the electrical activity of your heart during treatment with relugolix. Tell your healthcare provider right away if you get any signs or symptoms of QT prolongation, including:
    • dizziness
    • fainting
    • feeling that your heart is pounding or racing (palpitations)
    • chest pain

The most common side effects of relugolix include:

  • hot flushes
  • increased blood sugar levels
  • increased blood fat (triglyceride) levels
  • muscle and joint pain
  • decreased blood hemoglobin levels
  • increased liver enzymes
  • tiredness
  • constipation
  • diarrhea

Other side effects include weight gain, decreased sex drive, and erectile function problems.

Relugolix may cause fertility problems in males, which may affect your ability to father children. Talk to your healthcare provider if this is a concern for you.

These are not all the possible side effects of relugolix.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Interactions

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Taking relugolix with certain other medicines can affect how relugolix works or may cause side effects.

You should not start or stop any medicine before you talk with your healthcare provider who prescribed relugolix.

Know the medicines you take. Keep a list of them with you to show to your healthcare provider and pharmacist when you get a new medicine.

Pregnancy and breastfeeding

Tell your doctor if your are pregnant or plan to become pregnant. Relugolix can harm your unborn baby and cause loss of pregnancy (miscarriage).

Tell your doctor if you have a partner who is pregnant or may become pregnant. Males who have female partners who are able to become pregnant should use effective birth control (contraception) during treatment with relugolix and for 2 weeks after the last dose of relugolix.

Tell your doctor if you are breastfeeding or plan to breastfeed. It is not known if relugolix passes into your breast milk.

Storage

  • Store relugolix at room temperature. Do not store relugolix above 86°F (30°C).
  • Keep the bottle tightly closed after you first open it.
  • The relugolix bottle contains a desiccant to help keep your medicine dry (protect it from moisture). Do not remove the desiccant from the bottle.

Keep relugolix and all medicines out of the reach of children.

What are the ingredients in relugolix?

Active ingredient: relugolix

Inactive ingredients: mannitol, sodium starch glycolate, hydroxypropyl cellulose, magnesium stearate, hypromellose, titanium dioxide, ferric oxide red, and carnauba wax.

Relugolix is manufactured under the brand name Orgovyx by Bushu Pharmaceuticals, Ltd, Kawagoe, Saitama, Japan for Myovant Sciences, Inc., Brisbane, CA 94005.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.