Relugolix
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Molecule Summary
| Uses | Advanced Prostate Cancer |
| Therapy | Anti-Neoplastic, Hormonal Therapy |
| Side Effects | Hot Flashes, Tiredness, Constipation, Diarrhoea |
Assurance
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Regulated
Molecule Description
Relugolix contains relugolix, a prescription medicine called a GnRH receptor antagonist. It works by blocking signals from the brain that tell the testicles to produce testosterone. Lowering testosterone can slow the growth of prostate cancer cells
It is used in adult men with advanced prostate cancer.Relugolix is an oral tablet taken under the supervision of a specialist doctor. Continue treatment as prescribed by your doctor.
Relugolix is a prescription-only medicine and should be used strictly under medical supervision. The treatment plan is decided by the treating doctor based on the condition being treated, your body response and the other medicines you are receiving. Do not change, stop or repeat a dose on your own.
Before starting Relugolix, tell your doctor about all your existing medical conditions, especially heart, liver or kidney problems, and about every medicine, vitamin, supplement and herbal product you take. Tell your doctor if you are pregnant, planning a pregnancy or breastfeeding. Regular blood tests and clinical check-ups are usually needed during treatment so that side effects are picked up early.
Uses
- Relugolix is used to treat adult men with advanced prostate cancer
Contraindications
When should one not use Relugolix
- If you are allergic to relugolix or any other ingredient in this medicine, as a serious allergic reaction may occur
Side effects
Common side effects of this drug are:
- Hot flushes and sweating
- Muscle and joint pain (musculoskeletal pain), including back pain, bone pain, and pain in the limbs
- Fatigue and weakness
- Diarrhoea
- Constipation
- Increased blood sugar and triglyceride levels
- Decreased haemoglobin levels
- Low red blood cell count (anaemia), causing tiredness and breathlessness
- Breast swelling or tenderness (gynaecomastia)
- Difficulty sleeping (insomnia)
- Feeling low or depressed
- Dizziness and headache
- High blood pressure (hypertension)
- Nausea
- Excessive sweating (hyperhidrosis) and skin rash
- Reduced sex drive (libido decreased)
- Weight gain
- Increased liver enzyme levels
- Hives (urticaria) and swelling under the skin (angioedema)
- Bone thinning (osteoporosis and osteopenia)
- Heart attack (myocardial infarction).
- Serious side effects requiring medical attention
- Allergic reactions, including angioedema
- Changes in the electrical activity of the heart (QT prolongation), particularly in patients with risk factors or medicines that also prolong the QT interval
- Cardiovascular problems associated with long-term androgen deprivation therapy
- Tell your doctor right away if you develop chest pain, an irregular heartbeat, severe dizziness, fainting, or swelling of the face or throat.
Precautions and Warnings
Pregnancy
Breast Feeding
Driving
Alcohol
Other General Warnings
Talk to your doctor if
- You develop chest pain, shortness of breath, sudden weakness, or numbness, as hormone therapy may increase cardiovascular risk.
- You have irregular heartbeats, dizziness, or fainting, as relugolix may affect heart rhythm.
- You have heart disease, high blood pressure, diabetes, or high cholesterol, as treatment may affect cardiovascular and metabolic health.
- You develop swelling of the face, lips, tongue, or throat, hives, or a widespread rash, which may indicate an allergic reaction.
- You have liver or severe kidney problems, as your doctor may need to monitor you more closely.
- You take P-gp inhibitors or strong CYP3A/P-gp inducers, as they can change relugolix levels.
- You develop bone pain or fractures, as long-term testosterone suppression can reduce bone density.
- You plan to have children, as treatment may affect fertility. Discuss fertility preservation with your doctor before starting treatment if appropriate.
- Take Relugolix exactly as your doctor prescribed. You can take it with or without food.
- Take it at about the same time each day.
- If treatment is interrupted for more than 7 days, contact your doctor before restarting.
- Unlike some older hormone injections, Relugolix does not cause an initial testosterone surge when treatment starts.
- Have your blood pressure, blood sugar, cholesterol, and bone health monitored regularly during treatment.
- Tell your doctor immediately if you develop chest pain, an irregular heartbeat, fainting, severe dizziness, or swelling of the face or throat.
- Men with partners who could become pregnant should follow their doctor's advice about contraception during treatment and after stopping treatment.
- Tell your doctors, dentists, and emergency healthcare providers that you are taking Relugolix.
- Keep out of reach of children and pets.
Mode of Action
How Does It Work?
Relugolix blocks GnRH receptors in the pituitary gland. This reduces the signals that tell the testicles to produce testosterone, causing testosterone levels to fall to very low levels. Lower testosterone reduces the hormonal stimulation of prostate cancer cells, helping slow their growth. Unlike GnRH agonist injections, Relugolix does not cause an initial testosterone surge (flare) when treatment is started.
Interactions
Interactions with other medicines
- Some medicines can increase relugolix levels and may increase the risk of side effects. Your doctor may adjust treatment or monitor you more closely.
- Rifampicin, carbamazepine, phenytoin, phenobarbital, and St. John’s wort can lower relugolix levels and may make it less effective. Generally, avoid these combinations unless your doctor advises otherwise.
- Medicines that can cause irregular heart rhythms should be used with caution, particularly if you have other risk factors for heart rhythm problems.
- Tell your doctor about all medicines, vitamins, supplements, and herbal products you take, especially medicines for heart problems, seizures, infections, or cancer.
- Your doctor should review potential interactions before combining relugolix with other cancer medicines such as abiraterone, enzalutamide, darolutamide, or docetaxel.
Interactions with food items
Relugolix can be taken with or without food, as eating does not meaningfully change how much medicine your body absorbs Eating small, light meals through the day can help manage nausea, diarrhoea, and hot flushes, which are common side effects. Drink enough water and fluids throughout the day to support general hydration and help manage constipation.
Dosage
Overdose
There is no known specific antidote for a Relugolix overdose. If an overdose is suspected, contact your doctor or seek medical attention. Treatment is supportive and based on the patient's symptoms and clinical condition.
Missed a Dose
Never double doses to make up for a missed one. Always follow your doctor's advice before taking a missed dose.
Frequently Asked Questions (FAQs)
Articles
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References:
- DailyMed. Relugolix prescribing information. 2026 [Cited 17th Sep 2026]
- electronic medicines compendium (emc). Relugolix Summary of Product Characteristics. 2026 [Cited 17th Sep 2026]
- LactMed. Relugolix. 2026 [Cited 17th Sep 2026] Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Relugolix.
- Central Drugs Standard Control Organisation (CDSCO). Drugs@CDSCO [Internet]. New Delhi: Directorate General of Health Services, Ministry of Health & Family Welfare, Government of India. 2026 [Cited 17th Sep 2026]
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