Ensartinib

Ensartinib is a prescription medication indicated for the treatment of anaplastic lymphoma kinase (ALK)-positive locally advanced or metastatic non-small cell lung cancer (NSCLC) in adults who have not previously received an ALK-inhibitor

• Ensartinib is available under the following different brand names: Ensacove.

Common side effects of Ensartinib include:

• rash 
• tiredness
• muscle or bone pain 
• fever
• constipation 
• increased levels of liver and pancreatic enzymes
• itching  
• decreased white blood cell counts
• coughing 
• changes in blood levels of phosphate, magnesium, sodium, and potassium
• nausea 
• decreased protein (hemoglobin) in red blood cells
• skin swelling (edema) 
• increased bilirubin blood levels
• vomiting 

Serious side effects of Ensartinib include:

• lung problem symptoms such as trouble breathing or shortness of breath, cough with or without mucus, chest pain, fever 
• liver problem symptoms include yellowing of your skin or the white part of your eyes, bleeding or bruising more easily than normal, itchy skin, dark or brown (tea color) urine, decreased appetite, nausea or vomiting, feeling tired, pain on the right side of your stomach area 
• skin reaction symptoms such as rash, itching, or skin swelling
• slow heart rate (bradycardia) 
• high blood sugar (hyperglycemia) symptoms include feeling very thirsty, feeling sick to the stomach, needing to urinate more than usual, feeling weak or tired, feeling very hungry, feeling confused
• vision problem symptoms include blurry vision, light-hurting eyes, double vision, new or increased floaters, seeing flashes of light
• muscle pain, tenderness, and weakness (myalgia) symptoms include unexplained muscle pain or muscle pain that does not go away, tenderness, or weakness
• increased uric acid level in the blood (hyperuricemia) symptoms include red, hot, tender, or swollen joints, especially your big toe, nausea or vomiting, pain in the abdomen or sides, pink or brown urine
• allergic reactions to FD&C Yellow No. 5 (tartrazine)

Rare side effects of Ensartinib include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors.
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Capsule

• 25 mg
• 100 mg

NSCLC

Adult dosage

• 225 mg orally daily until disease progression or unacceptable toxicity

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Ensartinib has no noted severe interactions with any other drugs
• Ensartinib has no noted serious interactions with any other drugs
• Ensartinib has no noted moderate interactions with any other drugs
• Ensartinib has no noted minor interactions with any other drugs

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• Hypersensitivity reaction to ensartinib, FD&C Yellow No. 5 (Tartrazine), or any of its components.

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Ensartinib?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Ensartinib?”

Cautions

• Interstitial lung disease (ILD)/Pneumonitis
  • Monitor patients for new or worsening symptoms indicative of ILD/pneumonitis (e.g., dyspnea, cough, and fever) during treatment with ensartinib
  • Immediately withhold ensartinib in patients with suspected ILD/pneumonitis
  • Permanently discontinue ensartinib if ILD/pneumonitis is confirmed
• Hepatotoxicity
  • Can cause hepatotoxicity including drug-induced liver injury
  • Monitor liver function tests including alanine aminotransferase, aspartate aminotransferase, and total bilirubin at baseline and every 2 weeks during the first cycle of treatment with ensartinib, and then monthly and as clinically indicated
  • Withhold, reduce the dose, or permanently discontinue ensartinib based on the severity of the adverse reaction
• Dermatologic Adverse Reaction 
  • Can cause dermatologic adverse reactions, including drug reactions with eosinophilia and systemic symptoms (DRESS), rash, pruritus, and photosensitivity
  • Monitor for dermatologic adverse reactions during treatment with ensartinib
  • If dermatologic adverse reactions occur, treat with antihistamine, topical or systemic steroids based on the severity. 
  • Advise patients to limit direct sun exposure while taking ensartinib and for at least 1 week after discontinuation
  • Withhold, reduce the dose, or permanently discontinue ensartinib based on the severity of the adverse reaction
• Bradycardia
  • Monitor heart rate regularly during treatment with ensartinib
  • Withhold, reduce the dose, or permanently discontinue ensartinib based on the severity of bradycardia
• Hyperglycemia
  • Assess fasting serum glucose at baseline and monitor serum glucose periodically during treatment with ensartinib
  • Withhold, reduce the dose, or permanently discontinue ensartinib based on severity
• Visual disturbances
  • Can cause visual disturbances including blurred vision, diplopia, photopsia,
  • vitreous floaters, visual impairment, visual field defect, and reduced visual acuity
  • Obtain an ophthalmologic evaluation in patients with new or worsening visual symptoms during treatment with ensartinib
  • Withhold ensartinib and obtain an ophthalmologic evaluation, then reduce the dose or permanently discontinue ensartinib
• Increased creatine phosphokinase (CPK) 
  • Advise patients to report any unexplained muscle pain, tenderness, or weakness
  • Monitor CPK periodically during treatment with ensartinib
  • Withhold, reduce the dose, or permanently discontinue ensartinib based on severity
• Hyperuricemia
  • Monitor serum uric acid levels before initiating ensartinib and periodically during treatment
  • Initiate treatment with urate-lowering medications as clinically indicated
  • Withhold, reduce the dose, or permanently discontinue ensartinib based on severity
• Embryo-fetal toxicity
  • Can cause fetal harm when administered to a pregnant woman
  • Advise patients of the potential risk to a fetus and to use effective contraception
• FD&C Yellow No. 5 (Tartrazine)
  • It contains FD&C Yellow No. 5 (tartrazine), which may cause allergic-type reactions (including bronchial asthma) in certain susceptible persons. 
  • Although the overall incidence of FD&C Yellow No. 5 (tartrazine) sensitivity in the general population is low, it is frequently seen in patients who also have aspirin hypersensitivity

Pregnancy and Lactation

Ensartinib can cause fetal harm when administered to a pregnant woman

There are no available data on the use of ensartinib in pregnant women to inform a drug-associated risk

• Pregnancy testing
  • Verify the pregnancy status of females of reproductive potential before initiating ensartinib
• Contraception
  • Females
    • Advise females of reproductive potential to use effective contraception during treatment with ensartinib and for 1 week after the last dose
  • Males
    • Advise male patients with female partners of reproductive potential to use effective contraception during treatment with ensartinib and for 1 week after the last
• Lactation
  • There are no data on the presence of ensartinib or its metabolites in human milk, the effects on the breastfed child, or milk production.
  • Because of the potential for serious adverse reactions in breastfed children, advise women not to breastfeed during treatment with ensartinib and for 1 week after the last dose