Orgovyx (relugolix)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Relugolix, a gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone (LHRH), gonadorelin) antagonist, is used as an antineoplastic agent.
Relugolix is an oral nonpeptide gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, gonadorelin) antagonist. The drug rapidly, competitively, and reversibly binds to and blocks GnRH receptors in the pituitary, thereby reducing the release of gonadotropins (i.e., luteinizing hormone (LH), follicle-stimulating hormone (FSH)) and, consequently, testosterone without initial stimulation of the hypothalamic-pituitary-gonadal axis and the associated testosterone surge.
Relugolix is a substrate for intestinal P-glycoprotein (P-gp). Intestinal P-gp efflux is the primary determinant of relugolix absorption and oral bioavailability. Following oral administration, mean absolute bioavailability of relugolix is approximately 12%, and peak concentrations are achieved at a median of 2.25 hours.
With once-daily oral administration, accumulation of relugolix is approximately twofold. Although administration with a high-calorie, high-fat meal decreases relugolix absorption by approximately 20%, the effect is not considered clinically important. Relugolix is 68-71% bound to plasma proteins, mainly to albumin and to a lesser extent to alpha1-acid glycoprotein.
The mean effective half-life of relugolix is 25 hours, and the mean terminal elimination half-life is approximately 61 hours. Relugolix is metabolized mainly by CYP3A and to a lesser extent by CYP2C8 and other minor pathways. Following oral administration of a single 80-mg dose of radiolabeled relugolix, the drug was excreted in feces (81%) and urine (4.1%), mainly as metabolites; unchanged drug accounted for only about 6.4% of the recovered dose.
Age (45-91 years), race/ethnicity, and body weight (41-193 kg) do not have clinically important effects on the pharmacokinetics of relugolix.
USES: Relugolix is used to treat prostate cancer in men. It is not a cure. Most types of prostate cancer need the hormone testosterone to grow and spread.
Relugolix works by reducing the amount of testosterone that the body makes. This helps slow or stop the growth of cancer cells.
Generic name: relugolix
Pronunciation: (REL-ue-GOE-lix)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Orgovyx
Indications
The following indications are listed for Orgovyx:
- Advanced Prostatic Carcinoma
Also known as: Advanced Cancer Of Prostate Gland, Advanced Malignant Neoplasm Of Prostate, Advanced Prostate Cancer, Advanced Prostate Malignancy, Advanced Prostatic Cancer.
Dosing
Concomitant use of relugolix with a combined P-gp and strong cytochrome P-450 isoenzyme 3A (CYP3A) inducer should be avoided. If concomitant use is unavoidable, relugolix dosage should be increased to 240 mg once daily. The recommended relugolix dosage of 120 mg once daily should be resumed after discontinuation of the combined P-gp and strong CYP3A inducer.
Concomitant use of relugolix with oral P-gp inhibitors should be avoided. If concomitant use is unavoidable, relugolix should be administered first and separated from the P-gp inhibitor by at least 6 hours. Relugolix therapy may be interrupted for up to 2 weeks if short-term therapy with a P-gp inhibitor is required.
Relugolix is administered orally with a loading dose on the first day followed by once daily dosing at approximately the same time each day without regard to food.
The tablets should be swallowed whole and not crushed or chewed.
If a dose is missed, the missed dose should be taken as soon as it is remembered. However, if a dose is missed by more than 12 hours, the missed dose should not be taken and therapy should be resumed with the next scheduled dose.
The tablets should be stored at room temperature (not above 30oC).
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Severe hypersensitivity to relugolix or any of its components.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects reported in 10% or more of patients receiving relugolix include hot flush, musculoskeletal pain, fatigue, constipation, and diarrhea. Laboratory abnormalities reported in 15% or more of patients receiving the drug include increased glucose concentrations, increased triglyceride concentrations, decreased hemoglobin, and increased ALT and AST concentrations.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of relugolix in pediatric patients have not been established.
Safety and efficacy of relugolix have not been established in females. There are no data on use of relugolix in pregnant women to inform the drug-associated risk; however, based on animal findings and the drug's mechanism of action, relugolix can cause fetal harm.
Safety and efficacy of relugolix at the recommended dosage of 120 mg daily have not been established in females. It is not known whether relugolix distributes into human milk, affects breast-fed infants, or affects milk production. Relugolix and/or its metabolites are distributed into milk in rats at concentrations up to 10 times higher than 2-hour postdose plasma concentrations.
In the primary efficacy study of relugolix for treatment of prostate cancer, 81% of patients receiving relugolix were 65 years of age or older, while 35% were 75 years of age or older. No overall differences in safety or efficacy were observed between geriatric patients and younger adults. Population pharmacokinetic and pharmacokinetic/pharmacodynamic analyses in men 45-91 years of age revealed no clinically important effects of age on the pharmacokinetics of relugolix or on testosterone response to therapy.
ICD codes
No ICD codes are available for this drug.
Formulary status
Search health-plan coverage for this drug by ZIP code.
Choose the first character of a health plan name.
Last reviewed · Source: First Databank (FDB) drug data
On this page
Actions
Sign in to save favorites
Saving this drug requires a free Physicians Office Resource account.