Relupros Tablet 120 mg
Relupros Tablet 120 mg Uses, Dosage, Side Effects, Food Interaction and all others data.
Relupros Tablet 120 mg is a gonadotropin-releasing hormone (GnRH) receptor antagonist used in the treatment of several hormone-responsive conditions. It was first approved in Japan in 2019, under the brand name Relumina, for the symptomatic treatment of uterine fibroids, and more recently by the United States' FDA in 2020, under the brand name Orgovyx, for the treatment of advanced prostate cancer. Relupros Tablet 120 mg has also been studied in the symptomatic treatment of endometriosis.
Relupros Tablet 120 mg is the first (and currently only) orally-administered GnRH receptor antagonist approved for the treatment of prostate cancer - similar therapies such as degarelix require subcutaneous administration - and therefore provides a less burdensome therapeutic option for patients who might otherwise require clinic visits for administration by healthcare professionals. In addition to its relative ease-of-use, relugolix was shown to be superior in the depression of testosterone levels when compared to leuprolide, another androgen deprivation therapy used in the treatment of prostate cancer. In May 2021, the FDA approved the combination product made up of relugolix, estradiol, and norethindrone under the market name Myfembree for the first once-daily treatment for the management of heavy menstrual bleeding associated with uterine fibroids in premenopausal women.
Approximately 56% of patients achieved castrate-level testosterone concentrations (9 Relupros Tablet 120 mg requires once-daily oral administration to maintain the desired testosterone concentrations.
| Trade Name | Relupros Tablet 120 mg |
| Availability | Prescription only |
| Generic | Relugolix |
| Relugolix Other Names | Relugolix |
| Related Drugs | estradiol, Premarin, Xtandi, Casodex, Zytiga, Lynparza |
| Weight | 120 mg |
| Type | Tablet |
| Formula | C29H27F2N7O5S |
| Weight | Average: 623.64 Monoisotopic: 623.176244497 |
| Protein binding | Relugolix is 68-71% protein-bound in plasma, primarily to albumin and, to a lesser extent, α1-acid glycoprotein. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | Renata Limited |
| Available Country | Bangladesh |
| Last Updated: | October 19, 2023 at 6:27 am |
Uses
Relupros Tablet 120 mg is an oral GnRH receptor antagonist for androgen deprivation therapy in the treatment of advanced prostate cancer.
Relupros Tablet 120 mg is indicated for the treatment of adult patients with advanced prostate cancer. In a combination product with estradiol and norethindrone, relugolix is indicated for the once-daily treatment for the management of heavy menstrual bleeding associated with uterine fibroids in premenopausal women.
Relupros Tablet 120 mg is also used to associated treatment for these conditions: Advanced Prostate Cancer, Heavy Menstrual Bleeding
How Relupros Tablet 120 mg works
The pathogenesis and progression of prostate cancer appear driven, at least in part, by the effects of testosterone. Androgen deprivation has been demonstrated to result in cell death and tumor regression in many well-differentiated prostate cancer cell lines - for this reason, androgen deprivation therapy (ADT) has become a standard in the treatment of prostate cancer, particularly in advanced disease.
Testosterone production in males is carried out in the Leydig cells of testes and is stimulated by luteinizing hormone (LH), which itself is produced in the pituitary gland following the binding of gonadotropin-releasing hormone (GnRH) to corresponding GnRH receptors. Relupros Tablet 120 mg is a competitive antagonist of these GnRH receptors, thereby decreasing the release of LH and, ultimately, testosterone.
Toxicity
Data regarding overdose of relugolix are unavailable.
Food Interaction
- Take with or without food. Administration with food does not result in any clinically meaningful differences in pharmacokinetics.
Relupros Tablet 120 mg Drug Interaction
Moderate: famotidineMinor: enzalutamideUnknown: zolpidem, aspirin, alendronate, metoprolol, metoprolol, chlorhexidine topical, saw palmetto, pantoprazole, ubiquinone, bioflavonoids, cholecalciferol, alprazolam, rivaroxaban, abiraterone
Relupros Tablet 120 mg Disease Interaction
Elimination Route
The Cmax and AUC of orally-administered relugolix increase proportionally following single doses - in contrast, with repeat dosing the AUC remains proportional to the dose while the Cmax increases greater than proportionally to the dose. Following the administration of 120mg once daily, the steady-state AUC and Cmax of relugolix were 407 (± 168) ng.hr/mL and 70 (± 65) ng/mL, respectively.
The absolute oral bioavailability of relugolix is approximately 12% and the median Tmax following oral administration is 2.25 hours.
Half Life
The average effective half-life of relugolix is 25 hours, while the average terminal elimination half-life is 60.8 hours.
Clearance
The average renal clearance of relugolix is 8 L/h with a total clearance of 26.4 L/h.
Elimination Route
Approximately 81% of an orally administered dose was recovered in the feces, of which 4.2% was unchanged parent drug, while 4.1% of the dose was recovered in the urine, of which 2.2% remained unchanged.
Innovators Monograph
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