Orgovyx

Orgovyx (relugolix) is a prescription hormone therapy used for advanced prostate cancer to help slow or stop the spread of prostate cancer in adult men. Orgovyx is an androgen deprivation therapy (ADT) that lowers levels of testosterone which prostate cancer cells usually depend on to grow, which slows growth of the prostate cancer cells.

Orgovyx belongs to a class of medications called gonadotropin-releasing hormone (GnRH) receptor antagonists.

Orgovyx is a once-daily tablet taken with or without food.

The most common side effects include tiredness, hot flashes, muscle or joint pain, diarrhea, and constipation

Orgovyx works (mechanism of action) by binding and blocking GnRH receptors in the pituitary gland. Blocking GnRH receptors reduces the production of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which in turn lowers testosterone levels in the body. Since most prostate cancer cells depend on testosterone to grow, Orgovyx helps slow or stop cancer cell growth by effectively reducing testosterone production.

Orgovyx was fast and effective at suppressing testosterone in advanced prostate cancer in the Orgovyx HERO clinical trial (NCT03085095) results demonstrated:

• 96.7% of Orgovyx patients maintained castrate levels (<50 ng/dL) from day 29 through to 48 weeks vs. 88.8% with leuprolide.

• Day 4: 56% of Orgovyx patients reached castrate levels vs. 0% with leuprolide.
• Day 15: 99% of Orgovyx patients achieved suppression vs. 12% with leuprolide.

Take Orgovyx exactly as prescribed by your doctor. Follow all directions on your prescription label and read all medication guides or instruction sheets. Your doctor may occasionally change your dose.

Orgovyx's usual dose for the first dose is 3 tablets (loading dose), then 1 tablet daily as a maintenance dose. Take the medicine at the same time each day, with or without food.

Orgovyx tablet should be swallowed whole; do not crush, chew, or break the tablet.

You will need frequent medical tests. Your heart function may need to be routinely monitored using an electrocardiogram or ECG (sometimes called an EKG).

Your doctor will determine how long to treat you with Orgovyx. Do not change your dose or stop using this medicine without your doctor's advice.

Store tightly closed at room temperature, away from moisture and heat. Keep the tablets in their original container, along with the packet or canister of moisture-absorbing preservative.

Do not keep leftover medicine. Ask your pharmacist about a drug take-back program. You may also mix the leftover medicine with cat litter or coffee grounds in a sealed plastic bag and throw the bag in the trash. Do not flush down the toilet.

Heart problems: Tell your doctor if you or anyone in your family has or has ever had long QT syndrome (a rare heart problem that may cause irregular heartbeat, fainting, or sudden death). Also, tell your doctor if you have or have ever had an electrolyte imbalance in your blood, heart failure, diabetes, high triglycerides (fatty substances in the blood), anemia, or liver problems.

Hypersensitivity: Tell your doctor and pharmacist if you are allergic to the active ingredient relugolix, any other medications, or any of the inactive ingredients in the tablets. This medicine can cause hypersensitivity reactions, including angioedema.

Orgovyx can cause fetal harm. If you are a male and your female partner can become pregnant, you should use effective contraception during treatment and for 2 weeks after the last dose.

Orgovyx may decrease fertility in men. Discuss the risks with your doctor.

You should not use Orgovyx if you are allergic to the active ingredient relugolix, or inactive ingredients, or if you have:

• heart problems; or
• long QT syndrome (in you or a family member).

Pregnancy

Orgovyx can harm an unborn baby and cause loss of pregnancy (miscarriage).

• If you are a man, use birth control if your sex partner is able to get pregnant. Keep using birth control for at least 2 weeks after your last dose.
• Tell your doctor if your partner is pregnant or plans to get pregnant.

It may be harder for you to get a woman pregnant while you are using Orgovyx. You should still use birth control to prevent pregnancy because the medicine can harm an unborn baby.

Breastfeeding

Tell your healthcare provider if you are breastfeeding or plan to breastfeed. It is not known if this medicine passes into your breast milk.

Common Orgovyx side effects

Common Orgovyx side effects may include:

• Hot flush (54%)
• High blood sugar (44%)
• Triglycerides increased (35%)
• Muscle or joint pain (30%)
• Feeling tired, fatigue (26%)
• Alanine aminotransferase increased - ALT (27%)
• Aspartate aminotransferase increased - AST (18%)
• Diarrhea (12%)
• Constipation (12%)

The most common Orgovyx side effects occurred in 10% or more of patients, and laboratory changes occurred in 15% or more patients in the HERO clinical trial.

Serious Orgovyx side effects

Get emergency medical help if you have signs of an allergic reaction to Orgovyx: Hives, difficulty breathing, swelling of your face, lips, tongue, or throat, trouble swallowing.

Orgovyx may cause serious side effects. Call your doctor at once if you have:

• fast or pounding heartbeats, fluttering in your chest, shortness of breath, and sudden dizziness (like you might pass out);
• chest pain or pressure;
• sudden numbness or weakness on one side of the body;
• little or no urination, pain or burning when you urinate; or
• unusual bleeding.

Serious side effects occurred in 0.5% or more of patients taking Orgovyx in the HERO clinical trial, included:

• Myocardial infarction (0.8%)
• Acute kidney injury (0.6%)
• Abnormal heart rhythm - Arrhythmia (0.6%)
• Bleeding: 0.6%
• Urinary tract infection (0.5%)

This is not a complete list of side effects, and others may occur. Call your doctor for medical advice about side effects. You may report side effects tothe FDA at 1-800-FDA-1088.

Usual Adult Orgovyx Dose for Prostate Cancer:

Loading Dose: 360 mg orally once on the first dayMaintenance Dose: 120 mg orally once a dayTreatment interruption: If treatment is interrupted for greater than 7 days, restart Orgovyx with a loading dose of 360 mg on the first day, and continue with a dose of 120 mg once daily. Dose modification: may be necessary when used with interacting medications.Comment:Treatment is usually continued upon the development of nonmetastatic or metastatic castration-resistant prostate cancer in patients treated with GnRH receptor agonists and antagonists.

Use the medicine as soon as you can, but skip the missed dose if you are more than 12 hours late for the dose. Do not use two doses at one time.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Follow your doctor's instructions about any restrictions on food, beverages, or activity.

Sometimes, it is not safe to use certain medicines at the same time. Some drugs can affect your blood levels of other drugs you use, which may increase side effects or make the medicines less effective.

Orgovyx can cause a serious heart problem. Your risk may be higher if you also use certain other medicines for infections, asthma, heart problems, high blood pressure, depression, mental illness, cancer, malaria, or HIV.

Certain other drugs should not be used within 6 hours after you take Orgovyx. Your dose should be taken first, before other medicines. Carefully follow your doctor's instructions about how to schedule the doses of all your medicines.

P-gp Inhibitors

• Relugolix is a P-gp substrate. Co-administration of ORGOVYX with an oral P-gp inhibitor increases relugolix exposure, which may increase the risk of Orgovyx side effects
• Avoid using Orgovyx with oral P-gp inhibitors as this increases relugolix exposure, which may increase the risk of adverse reactions associated with Orgovyx.
• If unavoidable, take Orgovyx first, separate dosing by at least 6 hours, and monitor patients more frequently for adverse reactions.
• If an oral P-gp inhibitor will only be administered for up to 2 weeks, Orgovyx treatment may be interrupted while the P-gp inhibitor is being administered. Resume Orgovyx after the P-gp is discontinued. If Orgovyx treatment is interrupted for more than 7 days, resume Orgovyx at 360 mg on the first day, followed by 120 mg once daily.

Combined P-gp and Strong CYP3A Inducers

Avoid co-administration of Orgovyx with combined P-gp and strong CYP3A inducers. If co-administration is unavoidable, increase the Orgovyx dose to 240 mg once daily. After discontinuation of the combined P-gp and strong CYP3A inducer, resume the recommended Orgovyx dose of 120 mg once daily

Many drugs can interact with relugolix. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed here. Tell your doctor about all other medicines you use.

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

Orgovyx tablets contain 120mg of relugolix and are light red, almond-shaped, film-coated, debossed with “R” on one side and “120” on the other side.

Orgovyx manufactured for Sumitomo Pharma America, Inc., Marlborough, MA 01752

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use Orgovyx only for the indication prescribed.