Ensacove

Treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive locally advanced or metastatic non-small cell lung cancer (NSCLC) who have not received a prior ALK inhibitor.

Recommended dose: 225 mg orally once daily with or without food. Continue until disease progression or unacceptable toxicity.
Dose reduction: Reduce to 150 mg once daily for Grade 3 adverse reactions; reduce to 100 mg once daily for recurrence. Permanently discontinue if unable to tolerate 100 mg once daily.

Capsules: 100 mg, 150 mg, 225 mg

None established in prescribing information.

• Interstitial Lung Disease (ILD)/Pneumonitis: Occurred in 2.5% of patients, including Grade 3–4 in 1.3%. Withhold and investigate; permanently discontinue if confirmed.
• Bradycardia: Symptomatic bradycardia reported. Monitor heart rate. Avoid concomitant use of bradycardic agents if possible.
• Visual Disturbances: Visual disturbances including photopsia and blurred vision reported. Ophthalmologic evaluation recommended for new or worsening symptoms.
• Hepatotoxicity: ALT/AST elevations reported. Monitor liver function tests periodically.
• Myalgia/CPK Elevation: Creatine phosphokinase elevations and myalgia reported. Monitor CPK.
• Embryo-Fetal Toxicity: Can cause fetal harm. Advise effective contraception.

Rash (64%), Nausea (36%), Constipation (33%), Edema (31%), Vomiting (24%), Fatigue (26%), Diarrhea (21%), ALT Elevation (20%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Strong CYP3A4 inhibitors: Increase ensartinib exposure; avoid or reduce ensartinib dose to 150 mg.
Strong/moderate CYP3A4 inducers: Decrease exposure; avoid concomitant use.
CYP3A4 substrates with narrow therapeutic index: Monitor for increased toxicity.

Can cause fetal harm. Advise females of reproductive potential to use effective contraception. Consult the full prescribing information for pregnancy risk details.

Advise women not to breastfeed during treatment and for a period after the last dose. Refer to prescribing information for duration guidance.

Safety and effectiveness in pediatric patients have not been established unless otherwise noted in the full prescribing information.

Dose modifications for organ impairment are specified in the complete prescribing information.

Ensartinib is a potent, selective inhibitor of ALK and MET receptor tyrosine kinases. It inhibits ALK autophosphorylation and downstream signaling (PI3K/AKT, MAPK/ERK) in ALK-positive cancer cells, leading to cell cycle arrest and apoptosis. It also demonstrates activity against ALK resistance mutations.

Tmax: ~4 hours. Bioavailability: ~75%. Protein binding: ~99%. Vd: ~2850 L. Metabolized primarily by CYP3A4. Half-life: ~40 hours. Elimination: feces (80%), urine (~6%). Steady state: ~8 days.

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• eXalt3 — Ensartinib vs crizotinib in ALK-positive advanced NSCLC. Phase III, n=290.
  🔬 NCT02767804 ↗📄 Primary Publication ↗

Ensacove has FDA-approved indications across the following cancer types covered on CancerDrugEvidence: