Relugolix
Prostatic Neoplasms
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Drug Status
Government Approvals
US(FDA)
WHO Essential Medicine
NO
Known Teratogen
No
Pharmaceutical Class
Gonadotropin Releasing Hormone Receptor Antagonist
Controlled Drug Substance
No
Relugolix
Summary
Relugolix is used to treat advanced prostate cancer in adult men.
Relugolix acts as a gonadotropin-releasing hormone (GnRH) receptor antagonist. This means it binds to certain receptors in the body, reducing the release of hormones that stimulate testosterone production. By lowering testosterone levels, it helps to slow or stop the growth of prostate cancer cells.
The usual daily dose for adults is 120 mg. This medication is taken orally, once daily, after an initial loading dose of 360 mg on the first day.
Common side effects include hot flushes, increased blood sugar levels, increased triglycerides, musculoskeletal pain, decreased hemoglobin, increased liver enzymes, fatigue, constipation, and diarrhea.
Relugolix is not recommended for use in breastfeeding women, pregnant women, and children. It can cause fetal harm, so male patients with female partners of reproductive potential should use effective contraception. The medication is contraindicated in patients with severe hypersensitivity to it. Caution is advised in patients with long QT syndrome or those taking QT-prolonging drugs.
Indications and Purpose
How does Relugolix work?
Relugolix is a GnRH receptor antagonist that binds to pituitary receptors, reducing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This leads to decreased testosterone production, which is essential for slowing the growth of prostate cancer cells.
Is Relugolix effective?
Relugolix has been shown to effectively reduce testosterone levels in men with advanced prostate cancer. In clinical trials, a significant percentage of patients achieved and maintained castrate levels of testosterone, which is crucial for slowing the progression of prostate cancer.
What is Relugolix?
Relugolix is used to treat advanced prostate cancer in adult men. It works by decreasing testosterone levels, a hormone that prostate cancer cells need to grow. By blocking the GnRH receptors, it reduces the release of hormones that stimulate testosterone production, helping to slow or stop cancer progression.
Directions for Use
For how long do I take Relugolix?
Relugolix is typically used for the treatment of advanced prostate cancer, and the duration of use can vary based on individual treatment plans. It is often continued as long as it is effective and well-tolerated, but specific duration should be determined by a healthcare provider.
How do I take Relugolix?
Relugolix should be taken orally once daily, with or without food, at approximately the same time each day. Swallow the tablets whole without crushing or chewing. There are no specific food restrictions, but always follow your doctor's instructions regarding diet and medication.
How long does it take for Relugolix to start working?
Relugolix begins to reduce testosterone levels quickly, with 56% of patients reaching castrate levels by Day 4. Most patients maintain these levels throughout the treatment period, indicating its rapid onset of action.
How should I store Relugolix?
Store Relugolix at room temperature, away from excess heat and moisture. Keep it in its original container, tightly closed, and out of reach of children. Do not store it in the bathroom, and do not remove the desiccant packet included to absorb moisture.
What is the usual dose of Relugolix?
The usual daily dose for adults is 120 mg taken orally once daily after an initial loading dose of 360 mg on the first day. The safety and efficacy of Relugolix in children have not been established.
Warnings and Precautions
Can I take Relugolix with other prescription drugs?
Relugolix is a substrate of P-gp and CYP3A. Co-administration with P-gp inhibitors can increase relugolix exposure, while combined P-gp and strong CYP3A inducers can decrease its effectiveness. Avoid these combinations or adjust the dose as advised by a healthcare provider.
Can Relugolix be taken safely while breastfeeding?
The safety and efficacy of Relugolix in females, including those who are breastfeeding, have not been established. There is no data on whether Relugolix is present in human milk, so it is advised to consult a healthcare provider for personalized guidance.
Can Relugolix be taken safely while pregnant?
Relugolix is not intended for use in females, and its safety during pregnancy has not been established. It can cause fetal harm based on animal studies. Males with female partners of reproductive potential should use effective contraception during treatment and for 2 weeks after the last dose.
Is Relugolix safe for the elderly?
In clinical studies, no overall differences in safety or effectiveness were observed between elderly patients and younger patients. However, as with any medication, elderly patients should use Relugolix under the guidance of a healthcare provider, who will consider any age-related health conditions or medications.
Who should avoid taking Relugolix?
Relugolix may cause QT interval prolongation, which can affect heart rhythm. It is contraindicated in patients with severe hypersensitivity to the drug. Patients should be aware of potential embryo-fetal toxicity and use effective contraception if their partner can become pregnant. Monitoring for hypersensitivity reactions and heart-related symptoms is advised.
