Orgovyx 120mg Tablets
It is used to treat prostate cancer.
Drug Class
Gonadotropin-releasing hormone (GnRH) receptor antagonist
Pharmacologic Class
GnRH receptor antagonist
Pregnancy Category
Not applicable (Contraindicated in women who are or may become pregnant due to fetal harm risk)
FDA Approved
Dec 2020
DEA Schedule
Not Controlled
Overview
What is this medicine?
Orgovyx is a medication used to treat advanced prostate cancer. It works by lowering the amount of testosterone in your body, which helps to slow down the growth of prostate cancer cells. It is taken as a pill once a day.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food, and it's best to take it at the same time every day. Swallow the tablet whole - do not chew or crush it. Continue taking your medication as directed by your doctor or healthcare provider, even if you're feeling well.
If you're taking other oral medications, consult with your doctor or pharmacist to determine if you need to take them at a different time than this medication.
Storing and Disposing of Your Medication
Store your tablets in their original container at room temperature, keeping the cap tightly closed. Do not remove the antimoisture cube or packet. Protect the medication from heat and keep it out of reach of children and pets. Dispose of unused or expired medication properly. Do not flush it down the toilet or pour it down the drain unless instructed to do so. If you're unsure about the best way to dispose of your medication, consult with your pharmacist. You may also have access to drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's been 12 hours or more since the missed dose, skip it and return to your regular schedule. Do not take two doses at the same time or take extra doses. If you miss seven consecutive days of medication, contact your doctor for guidance on how to proceed.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food, and it's best to take it at the same time every day. Swallow the tablet whole - do not chew or crush it. Continue taking your medication as directed by your doctor or healthcare provider, even if you're feeling well.
If you're taking other oral medications, consult with your doctor or pharmacist to determine if you need to take them at a different time than this medication.
Storing and Disposing of Your Medication
Store your tablets in their original container at room temperature, keeping the cap tightly closed. Do not remove the antimoisture cube or packet. Protect the medication from heat and keep it out of reach of children and pets. Dispose of unused or expired medication properly. Do not flush it down the toilet or pour it down the drain unless instructed to do so. If you're unsure about the best way to dispose of your medication, consult with your pharmacist. You may also have access to drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's been 12 hours or more since the missed dose, skip it and return to your regular schedule. Do not take two doses at the same time or take extra doses. If you miss seven consecutive days of medication, contact your doctor for guidance on how to proceed.
Lifestyle & Tips
- Take Orgovyx exactly as prescribed by your doctor, at the same time each day, with or without food. Do not skip doses.
- Do not stop taking Orgovyx without talking to your doctor, even if you feel well.
- Maintain a healthy lifestyle, including a balanced diet and regular exercise, as recommended by your doctor.
- Report any new or worsening symptoms to your healthcare provider promptly.
- Be aware of potential side effects like hot flashes, fatigue, and musculoskeletal pain.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
120 mg orally once daily after an initial loading dose
Dose Range:
120 - 120 mg
Condition-Specific Dosing:
Loading Dose:
360 mg (three 120 mg tablets) orally on the first day
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed
Moderate:
No dose adjustment needed
Severe:
No dose adjustment needed
Dialysis:
Not studied in patients with end-stage renal disease (ESRD) requiring dialysis. Use with caution.
Hepatic Impairment:
Mild:
No dose adjustment needed
Moderate:
No dose adjustment needed
Severe:
Not studied in patients with severe hepatic impairment. Use with caution.
Pharmacology
Mechanism of Action
Relugolix is a non-peptide GnRH receptor antagonist that competitively binds to and blocks GnRH receptors in the anterior pituitary gland. This action leads to a rapid, reversible, and dose-dependent suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release, which in turn decreases testicular testosterone production.
Pharmacokinetics
Absorption:
Bioavailability:
~12.2% (absolute)
Tmax:
2-4 hours
FoodEffect:
High-fat meal decreases Cmax by 46% and AUC by 25%. Should be taken consistently with or without food.
Distribution:
Vd:
~191 L
ProteinBinding:
~68-71%
CnssPenetration:
Limited (not expected to cross BBB significantly)
Elimination:
HalfLife:
Mean 58 hours (range 25-60 hours)
Clearance:
Not available
ExcretionRoute:
Primarily feces (81.3%, 4.2% unchanged), minor renal (4.1%, 0.8% unchanged)
Unchanged:
4.2% (feces), 0.8% (urine)
Pharmacodynamics
OnsetOfAction:
Testosterone suppression to castration levels (<50 ng/dL) typically achieved within 4 days.
PeakEffect:
Sustained testosterone suppression with continued dosing.
DurationOfAction:
Testosterone levels return to baseline within 90 days after discontinuation.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Some allergic reactions can be severe.
Signs of high blood sugar, including:
+ Confusion
+ Feeling sleepy
+ Unusual thirst or hunger
+ Passing urine more often
+ Flushing
+ Fast breathing
+ Breath that smells like fruit
Chest pain or pressure
Fast heartbeat or abnormal heartbeat
Dizziness or fainting
Depression
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. If you notice any of the following side effects, or if they bother you or do not go away, contact your doctor:
Hot flashes
Feeling tired or weak
Diarrhea or constipation
Back, bone, joint, muscle, or neck pain
Pain in arms or legs
Weight gain
Trouble sleeping
Enlarged breasts
Excessive sweating
Decreased interest in sex
Difficulty getting or maintaining an erection
Reporting Side Effects
This is not a comprehensive list of all possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Some allergic reactions can be severe.
Signs of high blood sugar, including:
+ Confusion
+ Feeling sleepy
+ Unusual thirst or hunger
+ Passing urine more often
+ Flushing
+ Fast breathing
+ Breath that smells like fruit
Chest pain or pressure
Fast heartbeat or abnormal heartbeat
Dizziness or fainting
Depression
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. If you notice any of the following side effects, or if they bother you or do not go away, contact your doctor:
Hot flashes
Feeling tired or weak
Diarrhea or constipation
Back, bone, joint, muscle, or neck pain
Pain in arms or legs
Weight gain
Trouble sleeping
Enlarged breasts
Excessive sweating
Decreased interest in sex
Difficulty getting or maintaining an erection
Reporting Side Effects
This is not a comprehensive list of all possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Chest pain, shortness of breath, or discomfort in the arm, back, neck, jaw, or stomach (signs of heart attack or stroke)
- Sudden numbness or weakness on one side of the body, sudden severe headache, sudden vision changes, or problems with speech or balance (signs of stroke)
- Yellowing of your skin or the whites of your eyes, dark urine, severe stomach pain, or unusual bruising/bleeding (signs of liver problems)
- Severe dizziness or fainting spells
- Swelling in your legs or ankles
- New or worsening bone pain or fractures
- Symptoms of high blood sugar (e.g., increased thirst, frequent urination, increased hunger, blurred vision)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have low levels of potassium or magnesium in your blood, as this may affect your ability to take this medication safely.
Additionally, if you are a woman who is pregnant, plans to become pregnant, or is breastfeeding, it is crucial to discuss this with your doctor. This medication is not approved for use in pregnant or breastfeeding women, as it may cause harm to the unborn baby or increase the risk of pregnancy loss.
To ensure your safety, it is vital to provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
* Your complete medical history, including any health problems you have or have had in the past
Your doctor needs this information to determine whether it is safe for you to take this medication and to identify any potential interactions with other medications or health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor to confirm that it is safe to do so.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have low levels of potassium or magnesium in your blood, as this may affect your ability to take this medication safely.
Additionally, if you are a woman who is pregnant, plans to become pregnant, or is breastfeeding, it is crucial to discuss this with your doctor. This medication is not approved for use in pregnant or breastfeeding women, as it may cause harm to the unborn baby or increase the risk of pregnancy loss.
To ensure your safety, it is vital to provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
* Your complete medical history, including any health problems you have or have had in the past
Your doctor needs this information to determine whether it is safe for you to take this medication and to identify any potential interactions with other medications or health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor to confirm that it is safe to do so.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular blood work and laboratory tests, as directed by your doctor, are crucial to monitor your condition. Additionally, some individuals may require electrocardiogram (ECG) tests to check their heart rhythm.
If you have diabetes (high blood sugar), consult your doctor, as this medication may increase your blood sugar levels. Be sure to check your blood sugar levels as instructed by your doctor.
This medication can interact with numerous other drugs, which may increase the risk of side effects or reduce the medication's effectiveness. Therefore, it is crucial to discuss your medication regimen with your doctor and pharmacist to ensure safe use with your other prescription and over-the-counter medications, natural products, and vitamins.
Be aware that this medication may cause elevated triglyceride levels. If you have a history of high triglyceride levels, inform your doctor.
Lowering male hormones in the body with this medication may increase the risk of an abnormal heartbeat, known as prolonged QT interval. Discuss this potential risk with your doctor.
This medication may also affect fertility in men. Talk to your doctor if you have concerns about fathering a child.
If your partner may become pregnant, it is essential to use birth control while taking this medication and for 2 weeks after your last dose. If your partner becomes pregnant, notify your doctor immediately.
If you have diabetes (high blood sugar), consult your doctor, as this medication may increase your blood sugar levels. Be sure to check your blood sugar levels as instructed by your doctor.
This medication can interact with numerous other drugs, which may increase the risk of side effects or reduce the medication's effectiveness. Therefore, it is crucial to discuss your medication regimen with your doctor and pharmacist to ensure safe use with your other prescription and over-the-counter medications, natural products, and vitamins.
Be aware that this medication may cause elevated triglyceride levels. If you have a history of high triglyceride levels, inform your doctor.
Lowering male hormones in the body with this medication may increase the risk of an abnormal heartbeat, known as prolonged QT interval. Discuss this potential risk with your doctor.
This medication may also affect fertility in men. Talk to your doctor if you have concerns about fathering a child.
If your partner may become pregnant, it is essential to use birth control while taking this medication and for 2 weeks after your last dose. If your partner becomes pregnant, notify your doctor immediately.
Overdose Information
Overdose Symptoms:
- Symptoms of overdose are not well-characterized. May include exaggerated side effects.
What to Do:
In case of suspected overdose, seek immediate medical attention. Management should be supportive and symptomatic. Call 1-800-222-1222 (Poison Control Center).
Drug Interactions
Major Interactions
- Strong P-gp inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's Wort): Co-administration significantly decreases relugolix exposure, potentially reducing efficacy. Avoid concomitant use.
- Strong P-gp inhibitors (e.g., cyclosporine, erythromycin, verapamil, itraconazole, ritonavir): Co-administration can increase relugolix exposure. If unavoidable, monitor for adverse reactions.
Moderate Interactions
- Moderate P-gp inducers/inhibitors: May alter relugolix exposure. Monitor for efficacy or adverse reactions.
Monitoring
Baseline Monitoring
Serum Testosterone
Rationale: To establish baseline levels and confirm diagnosis.
Timing: Prior to initiation of therapy
Prostate-Specific Antigen (PSA)
Rationale: To establish baseline and monitor response to therapy.
Timing: Prior to initiation of therapy
Liver Function Tests (LFTs)
Rationale: To establish baseline and monitor for potential hepatic injury.
Timing: Prior to initiation of therapy
Electrolytes (Potassium, Magnesium)
Rationale: To assess risk factors for QTc prolongation.
Timing: Prior to initiation of therapy
Electrocardiogram (ECG)
Rationale: To assess for baseline QTc interval, especially in patients with risk factors for QT prolongation.
Timing: Prior to initiation of therapy, if indicated
Routine Monitoring
Serum Testosterone
Frequency: Periodically (e.g., monthly or every 3 months)
Target: <50 ng/dL (castration level)
Action Threshold: If levels are not suppressed, assess adherence and consider drug interactions.
Prostate-Specific Antigen (PSA)
Frequency: Periodically (e.g., every 3-6 months or as clinically indicated)
Target: Decreasing or stable levels
Action Threshold: Rising PSA may indicate disease progression or treatment failure.
Liver Function Tests (LFTs)
Frequency: Periodically (e.g., every 3-6 months or as clinically indicated)
Target: Within normal limits
Action Threshold: Significant elevations may require dose adjustment or discontinuation.
Electrolytes (Potassium, Magnesium)
Frequency: Periodically, especially if risk factors for QTc prolongation are present or develop.
Target: Within normal limits
Action Threshold: Correct hypokalemia or hypomagnesemia.
ECG
Frequency: As clinically indicated, especially if new risk factors for QTc prolongation develop or worsen.
Target: Normal QTc interval
Action Threshold: Significant QTc prolongation may require cardiology consultation or treatment modification.
Symptom Monitoring
- Hot flashes
- Fatigue
- Musculoskeletal pain
- Cardiovascular symptoms (e.g., chest pain, shortness of breath, palpitations, dizziness, fainting)
- Signs of liver injury (e.g., jaundice, dark urine, severe abdominal pain)
- Symptoms of diabetes (e.g., increased thirst, frequent urination)
- Symptoms of bone density loss (e.g., new or worsening bone pain, fractures)
Special Patient Groups
Pregnancy
Contraindicated. Orgovyx can cause fetal harm when administered to a pregnant woman based on its mechanism of action. It is not indicated for use in women.
Trimester-Specific Risks:
First Trimester:
High risk of fetal harm due to hormonal effects.
Second Trimester:
High risk of fetal harm due to hormonal effects.
Third Trimester:
High risk of fetal harm due to hormonal effects.
Lactation
Not recommended. It is not known whether relugolix is excreted in human milk. Due to the potential for serious adverse reactions in a breastfed infant, women should not breastfeed during treatment with Orgovyx.
Infant Risk:
Unknown, but potential for serious adverse reactions.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Orgovyx is not indicated for use in pediatric patients.
Geriatric Use
No specific dose adjustment is needed based on age alone. Clinical studies included patients 65 years and older, and no overall differences in safety or effectiveness were observed between these patients and younger patients.
Clinical Information
Clinical Pearls
- Orgovyx is the first oral GnRH receptor antagonist approved for advanced prostate cancer, offering a convenient oral alternative to injectable GnRH agonists/antagonists.
- Unlike GnRH agonists, Orgovyx provides rapid and profound testosterone suppression without an initial testosterone surge (flare), eliminating the need for anti-androgen co-administration to prevent flare symptoms.
- A loading dose is crucial on the first day to achieve rapid castration levels.
- Significant drug interactions exist with P-glycoprotein (P-gp) modulators (inhibitors and inducers). A thorough medication review is essential before and during treatment.
- Patients should be monitored for cardiovascular events, as androgen deprivation therapy (ADT) is associated with increased risk of cardiovascular disease, diabetes, and bone density loss.
- Adherence to daily dosing is critical for maintaining testosterone suppression.
Alternative Therapies
- Other GnRH receptor antagonists (e.g., degarelix - injectable)
- GnRH agonists (e.g., leuprolide, goserelin, triptorelin - injectable, often require anti-androgen co-administration for flare prevention)
- Androgen receptor pathway inhibitors (e.g., abiraterone, enzalutamide, apalutamide, darolutamide)
- Chemotherapy (e.g., docetaxel, cabazitaxel)
- Bilateral orchiectomy (surgical castration)
Cost & Coverage
Average Cost:
$2,500 - $3,500 per 30 tablets
Insurance Coverage:
Specialty tier, typically requires prior authorization and may have step therapy requirements.
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.