Formulary
Relugolix: Indications, Dosing, Side Effects and Interactions
Relugolix is a non-peptide gonadotrophin-releasing hormone (GnRH) receptor antagonist that reduces the release of luteinising hormone and follicle-stimulating...
MedNext Academy | 3 min read
Relugolix: Indications, Dosing, Side Effects and Interactions
Relugolix is a non-peptide gonadotrophin-releasing hormone (GnRH) receptor antagonist that reduces the release of luteinising hormone and follicle-stimulating...
Drug action
Relugolix is a non-peptide gonadotrophin-releasing hormone (GnRH) receptor antagonist that reduces the release of luteinising hormone and follicle-stimulating hormone, thereby reducing production of testosterone.
Indications and dose
**Prostate cancer (under expert supervision)**
- **Adult** (By Mouth): Loading dose 360 mg for 1 dose, then maintenance 120 mg once daily.
Cautions
History or risk of QT-interval prolongation; risk factors for cardiovascular disease; risk factors for osteoporosis
Side effects
Common or very common Anaemia; arthralgia; arthritis; asthenia; colitis; constipation; depression; diarrhoea; dizziness; gynaecomastia; headache; hot flush; hyperhidrosis; hypertension; insomnia; libido decreased; musculoskeletal discomfort; myalgia; nausea; pain; rash; weight increased Uncommon Bone disorders Rare or very rare Myocardial infarction Frequency not known QT interval prolongation
Interactions
**Severe interactions:**
- No clinically significant differences in the pharmacokinetics of dabigatran etexilate (P-gp substrate) were observed upon co-administration with relugolix, clinically meaningful effects of relugolix...
**Other interactions (25):**
- Potential for other medicinal products to affect the components of Ryeqo Relugolix Oral P-glycoprotein (P-gp) inhibitors: Concomitant use of Ryeqo with oral P-gp inhibitors is not recommended.
- Relugolix is a substrate of P-gp (see section 5.2) and in an interaction study with erythromycin, a P-gp and moderate cytochrome P450 (CYP) 3A4 inhibitor, the area under the curve (AUC) and maximum...
- Concomitant use of P-gp inhibitors may increase the exposure of relugolix, including certain anti-infective medicinal products (e.g.
- If concomitant use with once or twice daily oral P-gp inhibitors is unavoidable (e.g.
- In a clinical interaction study with rifampicin, a strong CYP3A4 and P-gp inducer, the C max and AUC of relugolix were reduced by 23% and 55%, respectively.
- Medicinal products that cause strong CYP3A4 and/or P-gp induction, such as anticonvulsants (e.g.
Renal impairment
Use with caution in severe impairment (risk of increased exposure). M
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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