Formulary
Linzagolix: Indications, Dosing, Side Effects and Interactions
Linzagolix is a non-peptide gonadotrophin-releasing hormone (GnRH) receptor antagonist that competitively binds to GnRH receptors in the pituitary gland,...
MedNext Academy | 3 min read
Linzagolix: Indications, Dosing, Side Effects and Interactions
Linzagolix is a non-peptide gonadotrophin-releasing hormone (GnRH) receptor antagonist that competitively binds to GnRH receptors in the pituitary gland,...
Drug action
Linzagolix is a non-peptide gonadotrophin-releasing hormone (GnRH) receptor antagonist that competitively binds to GnRH receptors in the pituitary gland, thereby reducing production of oestrogen and progesterone.
Indications and dose
**Moderate to severe uterine fibroids [in combination with add-back hormone replacement therapy] (under expert supervision)**
- **Adult** (By Mouth): 18-56 years 100-200 mg once daily, to be taken in combination with estradiol 1 mg and norethisterone 500 micrograms once daily, dose to be started preferably in the first week of the menstrual cycle.
**Moderate to severe uterine fibroids [without add-back hormone replacement therapy] (under expert supervision)**
- **Adult** (By Mouth): 18-56 years 100 mg once daily, dose to be started preferably in the first week of the menstrual cycle, alternatively 200 mg once daily for maximum duration of 6 months, to be given for reduction of uterine and fibroid volume, dose to be started preferably in the first week of the menstrual cycle.
**Endometriosis (under expert supervision)**
- **Adult** (By Mouth): 18-56 years 200 mg once daily, to be taken in combination with estradiol 1 mg and norethisterone 500 micrograms once daily, dose to be started preferably in the first week of the menstrual cycle.
Cautions
Cardiovascular disease; history of depression and/or suicidal ideation (discontinue if severe depression recurs); risk factors for osteoporosis (dual X-ray absorptiometry (DXA) scan recommended before starting); risk factors for QT-interval prolongation
Contraindications
Genital bleeding of unknown cause; osteoporosis
Side effects
Common or very common Anxiety; arthralgia; asthenia; constipation; depression; haemorrhage; headache; hot flush; libido decreased; menstrual cycle irregularities; mood altered; nausea; pelvic pain; sweat changes; vomiting; vulvovaginal dryness Uncommon Abdominal pain upper; hypertension
Interactions
**Other interactions (2):**
- CYP2C8 substrate medicinal products Linzagolix has been shown to increase mean repaglinide (a CYP2C8 sensitive substrate) exposure in healthy subjects by less than 2-fold.
- Due to the risk of increased plasma concentrations, concomitant administration of Yselty and medicinal products primarily cleared by CYP2C8 metabolism and with a narrow therapeutic index such as...
Pregnancy
Avoid (embryotoxic in animal studies). M
Breast feeding
Avoid (present in milk in animal studies). M
Hepatic impairment
Caution in patients with a history of abnormal hepatic function (no information available); avoid in severe impairment (risk of increased exposure). M
Renal impairment
Caution in mild impairment (risk of increased exposure); avoid in moderate to severe impairment. 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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