Ensartinib
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Nehal Eid
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Overview
Ensartinib is a Kinase inhibitor that is FDA approved for the treatment of It is indicated for the treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive locally advanced or metastatic non-small cell lung cancer (NSCLC) who have not previously received an ALK-inhibitor.. Common adverse reactions include Most common adverse reactions (incidence≥20%) were rash, musculoskeletal pain, constipation, pruritus, cough, nausea, edema, vomiting, fatigue, and pyrexia..
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
Select patients with ALK-positive locally advanced or metastatic NSCLC. Recommended dosage: 225 mg orally once daily with or without food until disease progression or unacceptable toxicity.
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Ensartinib in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Ensartinib in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
There is limited information regarding Ensartinib FDA-Labeled Indications and Dosage (Pediatric) in the drug label.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Ensartinib in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Ensartinib in pediatric patients.
Contraindications
Hypersensitivity reaction to Ensartinib or to any of its components.
Warnings
-Interstitial Lung Disease (ILD)/Pneumonitis: Monitor patients for new or worsening symptoms indicative of ILD/pneumonitis. Permanently discontinue in patients with ILD/pneumonitis.
-Hepatotoxicity: Monitor liver function tests during treatment Withhold, reduce the dose, or permanently discontinue treatment based on severity.
-Dermatologic Adverse Reaction: Monitor for dermatologic adverse reactions during treatment. Withhold, reduce the dose, or permanently discontinue based on symptom severity.
-Bradycardia: Monitor heart rate regularly during treatment. Withhold, reduce the dose, or permanently discontinue based on severity.
-Hyperglycemia: Monitor serum glucose periodically during treatment. Withhold, reduce the dose, or permanently discontinue based on severity.
-Visual Disturbances: Advise patients to report visual symptoms during treatment. Withhold ENSACOVE and obtain ophthalmologic evaluation, then reduce the dose or permanently discontinue.
-Increased Creatine Phosphokinase (CPK): Monitor CPK periodically during treatment. Withhold, reduce the dose, or permanently discontinue based on severity.
-Hyperuricemia: Monitor uric acid periodically during treatment. Withhold, reduce the dose, or permanently discontinue based on severity.
-Embryo-Fetal Toxicity: Can cause fetal harm. Advise patients of the potential risk to a fetus and to use effective contraception.
Adverse Reactions
Clinical Trials Experience
• Most common adverse reactions (incidence ≥20%) were rash, musculoskeletal pain, constipation, pruritus, cough, nausea, edema, vomiting, fatigue, and pyrexia.
• Most common Grade 3-4 laboratory abnormality (incidence ≥2%) were increased uric acid, decreased lymphocytes, increased alanine aminotransferase, decreased phosphate, increased gamma glutamyl transferase, increased magnesium, increased amylase, decreased sodium, increased glucose, decreased hemoglobin, increased bilirubin, decreased potassium, and increased creatine phosphokinase.
Postmarketing Experience
There is limited information regarding Ensartinib Postmarketing Experience in the drug label.
Drug Interactions
• Moderate or Strong CYP3A Inhibitors: Avoid concomitant use with ENSACOVE. • Moderate or Strong CYP3A Inducers: Avoid concomitant use with ENSACOVE. • P-gp Inhibitor: Avoid concomitant use with ENSACOVE.
Use in Specific Populations
Pregnancy
Pregnancy Category (FDA):
There is no FDA guidance on usage of Ensartinib in women who are pregnant.
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Ensartinib in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Ensartinib during labor and delivery.
Nursing Mothers
Advise not to breastfeed.
Pediatric Use
There is no FDA guidance on the use of Ensartinib in pediatric settings.
Geriatic Use
Clinical studies did not include sufficient numbers of patients ages 65 and over to determine whether they respond differently from younger patients. Exploratory analysis suggests a higher incidence of serious adverse events (43% vs 27%), more frequent adverse events leading to treatment discontinuations (18% vs 10%) and dose modifications (34% vs 16%) in patients 65 years or older as compared to those younger than 65 years.
Gender
There is no FDA guidance on the use of Ensartinib with respect to specific gender populations.
Race
There is no FDA guidance on the use of Ensartinib with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Ensartinib in patients with renal impairment.
Hepatic Impairment
Avoid use in patients with severe hepatic impairment.
Females of Reproductive Potential and Males
Can cause fetal harm. Advise patients of the potential risk to a fetus and to use effective contraception.
Immunocompromised Patients
There is no FDA guidance one the use of Ensartinib in patients who are immunocompromised.
Administration and Monitoring
Administration
-The recommended dosage is 225 mg orally once daily, with or without food, until disease progression or unacceptable toxicity.
-Swallow capsules whole, do not crush or chew. Do not open or dissolve the contents of the capsule. Take it at the same time each day.
-Missed dose: If a dose is missed, then take the missed dose as soon as possible unless the next dose is due within 12 hours.
-Vomiting: If vomiting occurs after taking a dose, do not take an additional dose and take the next dose at its scheduled time.
Monitoring
There is limited information regarding Ensartinib Monitoring in the drug label.
IV Compatibility
There is limited information regarding the compatibility of Ensartinib and IV administrations.
Overdosage
There is limited information regarding Ensartinib overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.
Pharmacology
There is limited information regarding Ensartinib Pharmacology in the drug label.
Mechanism of Action
Ensartinib is a kinase inhibitor of anaplastic lymphoma kinase (ALK) and inhibits other kinases including MET and ROS1. In vitro, ensartinib inhibited phosphorylation of ALK and its downstream signaling proteins AKT, ERK, and S6, thereby blocking ALK-mediated signaling pathways and inhibiting proliferation in cell lines harboring ALK fusions and mutations. In vivo,ensartinib showed anti-tumor activity in a mouse xenograft model of human NSCLC harboring an ALK fusion.
Structure
There is limited information regarding Ensartinib Structure in the drug label.
Pharmacodynamics
-Exposure-response relationship Ensartinib exposure-response relationships and the time course of the pharmacodynamic response have not been fully characterized.
-Cardiac Electrophysiology At the approved recommended dosage, a mean increase in the QTc interval > 20 ms was not observed.
Pharmacokinetics
Ensartinib mean (coefficient of variation [CV%]) maximum concentration (Cmax) is 292 ng/mL (60%), and the area under the concentration-time curve (AUC0–24h) is 4,920 ng·h /ml (62%) at the approved recommended dosage. Ensartinib steady state is reached within 15 days with a mean accumulation ratio of 2.7.
Nonclinical Toxicology
There is limited information regarding Ensartinib Nonclinical Toxicology in the drug label.
Clinical Studies
There is limited information regarding Ensartinib Clinical Studies in the drug label.
How Supplied
Capsules: 25 mg and 100 mg of Ensartinib.
Storage
There is limited information regarding Ensartinib Storage in the drug label.
Images
Drug Images
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Package and Label Display Panel
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Patient Counseling Information
There is limited information regarding Ensartinib Patient Counseling Information in the drug label.
Precautions with Alcohol
Alcohol-Ensartinib interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
There is limited information regarding Ensartinib Brand Names in the drug label.
Look-Alike Drug Names
There is limited information regarding Ensartinib Look-Alike Drug Names in the drug label.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.