Entrectinib

Cytostatic · Protein kinase inhibitor

Indications

Treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumours are ROS1-positive. Treatment of adult and children =12 yrs with solid tumours that: have a neurotrophic tyrosine receptor kinase (NTRK) gene fusion without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and have progressed following treatment or have no satisfactory alternative therapy.

Dosage

ROS1-Positive Non-Small Cell Lung Cancer: Adults: 600 mg orally once a day. NTRK Gene Fusion-Positive Solid Tumours: Adults: 600 mg orally once a day. Children =12 yrs: Recommended dosage is based on BSA as following: BSA >1.50 m2: 600 mg once a day. BSA 1.11-1.50 m2: 500 mg once a day. BSA 0.91-1.10 m2: 400 mg once a day.

Adverse Effects

Fatigue, constipation, dysgeusia, oedema, dizziness, nausea, diarrhoea, dysesthesia, dyspnoea, myalgia, cognitive impairment, increased weight, cough, vomiting, pyrexia, arthralgia, and vision disorders.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Precautions: Congestive heart failure, hyperuricaemia, prolonged QTc interval.

Interactions

Moderate and strong CYP3A inhibitors and inducers such as itraconazole, rifampin (avoid; otherwise reduce dose). Lansoprazole, midazolam, digoxin.

Advice to Patient

Take with or without meals. Swallow capsules whole. Do not open, crush, chew or dissolve the contents of the capsule. If a dose is missed, take it as soon as you remember unless the next dose is due within 12 hrs. If vomiting occurs after a dose, repeat that dose. Avoid grapefruit products during treatment. Females of reproductive potential should use effective contraception during treatment with entrectinib and for 5 wks following the final dose. Males with female partners of reproductive potential should use effective contraception during treatment with entrectinib and for 3 months after the final dose. Inform prescriber if you experience bone pain, changes in mobility, any deformity, changes in vision, signs and symptoms of hyperuricaemia or hepatotoxicity.

Pharmacokinetics

Absorption: Well-absorbed through GI tract. Metabolism: Hepatic. Half-life elimination: Entrectinib: 20 hrs. M5 (active metabolite): 40 hrs. Time to peak, plasma: 4-6 hrs. Excretion: Faeces (83%). Urine (3%).

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.