relugolix

Absorption: 12% absorbed following oral administration.

Distribution: Unknown.

Metabolism/Excretion: Primarily metabolized in the liver via the CYP3A4 isoenzyme (and to a lesser extent by CYP2C8). Primarily excreted in feces (81%; 4.2% as unchanged drug), with 4.1% excreted in urine (2.2% as unchanged drug).

Half-Life: 61 hr.

Time/Action Profile ⬆ ⬇

(↓ in testosterone levels)

ROUTE	ONSET	PEAK	DURATION
PO	within 1 wk	unknown	48 wk

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity.

Use Cautiously in:

Congenital long QT syndrome, HF, electrolyte abnormalities, or concurrent use of QT interval prolonging drugs;
Rep: Men with female partners of reproductive potential.

Adv. Reactions/Side Effects ⬆ ⬇

CV: QT interval prolongation

Derm: hot flush, ↑sweating

Endo: hyperglycemia, gynecomastia

GI: ↑liver enzymes, constipation, diarrhea

GU: ↓fertility, ↓libido

Hemat: anemia

Metab: hypertriglyceridemia, weight gain

MS: pain

Neuro: fatigue, depression, insomnia

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

Concurrent use of QT interval prolonging drugs may ↑ risk of QT interval prolongation and torsades de pointes.
P-glycoprotein (P-gp) inhibitors may ↑ levels and risk of toxicity; avoid concurrent use. If concurrent use unavoidable, administer relugolix first and then administer P-gp inhibitor ≥6 hr later. If P-gp inhibitor only administered for ≤2 wk, may interrupt relugolix therapy.
Combined P-gp and strong CYP3A4 inducers may ↓ levels and effectiveness; avoid concurrent use. If concurrent use unavoidable, ↑ relugolix dose.

Route/Dosage ⬆ ⬇

PO (Adults ): 360 mg (loading dose) on Day 1; then 120 mg once daily (maintenance dose) starting on Day 2 and thereafter. Concurrent use of combined P-gp and strong CYP3A inducer: ↑maintenance dose to 240 mg once daily. If combined P-gp and strong CYP3A4 inducer discontinued, ↓ maintenance dose to 120 mg once daily.

Availability ⬆ ⬇

Assessment ⬆ ⬇

Assess cardiac history and ECG at baseline for prolonged QT/QTc interval or history of long QT syndrome; cardiac arrhythmias associated with prolonged QT interval can occur. Correct known electrolyte abnormalities.
Monitor for signs and symptoms of hypersensitivity reactions (rash, urticaria, pruritus, flushing, dizziness, vomiting, abdominal pain) and angioedema (swelling of throat, lips, tongue, or face; dyspnea; wheezing; hoarseness). Discontinue relugolix immediately and provide supportive care.

Lab Test Considerations:

Obtain periodic serum prostate specific antigen (PSA) levels; if PSA ↑, measure serum testosterone concentrations.
Monitor electrolytes periodically, especially in patients with congenital long QT syndrome, HF, or frequent electrolyte abnormalities and in those taking QT interval prolonging drugs.
May ↑ glucose and triglycerides.
May ↑ liver enzymes.

Implementation ⬆ ⬇

PO: Administer at approximately the same time each day without regard to food. DNC: Swallow tablets whole; do not crush or chew.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of relugolix . If a dose is missed, it should taken as soon as remembered; if a dose is missed >12 hr, do not take the missed dose and resume treatment with the next scheduled dose. Advise patient to read Patient Information before starting therapy.
Side effects may include flushing of the skin, hot flashes, musculoskeletal pain, fatigue, constipation, diarrhea, ↑ weight, ↓ sex drive, and erectile dysfunction.
Warn patient to report symptoms of arrhythmias and QT prolongation (fast heartbeat, skipped beats, palpitations, dizziness, light-headedness, trouble breathing, faintness).
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Rep: May cause fetal harm; advise men with female partners of reproductive potential to use effective contraception during treatment and for 2 wk after last dose.

Evaluation/Desired Outcomes ⬆ ⬇

Achievement and maintenance of serum testosterone suppression to medical castration levels.

US Brand Names ⬆ ⬇

Code ⬆

NDC Code

46014- Excella GmbH & Co. KG
- 46014-1130-
  - 46014-1130-1- 40 kg in 1 DRUM (46014-1130-1)

51148- Bushu Pharmaceuticals, Ltd.
- 51148-013-
  - 51148-013-01- 1 BAG in 1 DRUM (51148-013-01) / 134000 TABLET, FILM COATED in 1 BAG

53296- Medichem S.A.
- 53296-0131-
  - 53296-0131-0- 75 kg in 1 DRUM (53296-0131-0)

54893- MSN Laboratories Private Limited
- 54893-0511-
  54893-0511-1- 40 kg in 1 DRUM (54893-0511-1)

68554- Hetero Labs Limited
- 68554-0165-
  68554-0165-1- 1 kg in 1 DRUM (68554-0165-1)

70447- FAREVA LA VALLEE
- 70447-0005-
  70447-0005-1- 25 kg in 1 DRUM (70447-0005-1)

72974- Sumitomo Pharma America, Inc.
- 72974-120- Orgovyx
  72974-120-01- 30 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (72974-120-01)

72974- Sumitomo Pharma America, Inc.
- 72974-120-
  - 72974-120-04- 1 BAG in 1 DRUM (72974-120-04) / 1 TABLET, FILM COATED in 1 BAG

72974- Sumitomo Pharma America, Inc.
- 72974-120- Orgovyx
  72974-120-95- 16 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (72974-120-95)

72974- Sumitomo Pharma America, Inc.
- 72974-120- Orgovyx
  - 72974-120-97- 30 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (72974-120-97)

76361- BDR Lifesciences Private Limited
- 76361-0004-
  - 76361-0004-1- 20 kg in 1 DRUM (76361-0004-1)

83137- Shanghai Huilun Jiangsu Pharmaceutical Co., Ltd.
- 83137-0009-
  83137-0009-1- 5 kg in 1 CARTON (83137-0009-1)

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇