Mobocertinib

Mobocertinib is a prescription medication used for the treatment of locally advanced or metastatic non–small cell lung cancer (NSCLC) in adults.

• Mobocertinib is available under the following different brand names: Exkivity.

Common side effects of Mobocertinib include:

• diarrhea, 
• rash, 
• nausea, 
• stomatitis, 
• vomiting, 
• loss of appetite, 
• skin infection around a fingernail or toenail, 
• fatigue, 
• sores and inflammation in the mouth, 
• weight loss, 
• abdominal pain, 
• gastroesophageal reflux disease (GERD), 
• indigestion, 
• headache, 
• itching, 
• hair loss, 
• cough, 
• upper respiratory tract infection, 
• runny nose, 
• dry skin, and
• musculoskeletal pain

Serious side effects of Mobocertinib include:

• hives, 
• difficulty breathing, 
• swelling of the face, lips, tongue, or throat, 
• diarrhea, 
• shortness of breath, 
• vomiting, 
• fever, 
• acute kidney injury, 
• nausea, 
• fluid in the chest, 
• fatigue, 
• high blood pressure (hypertension),
• fast or irregular heartbeats, 
• swelling in the legs, and
• rapid heartbeat

Rare side effects of Mobocertinib 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, loss of coordination, feeling 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 dosage

Capsule

• 40 mg

Non-Small Cell Lung Cancer

Adult dosage

• 160 mg orally every day.

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.

• Mobocertinib has severe interactions with the following drug:
  • mavacamten
• Mobocertinib has serious interactions with at least 239 other drugs.
• Mobocertinib has moderate interactions with the following drugs:
  • atogepant
  • belumosudil
  • deutetrabenazine
  • doxepin
  • floxuridine
  • isavuconazonium sulfate
  • valbenazine
  • warfarin
• Mobocertinib has minor interactions with no 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 your products. 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

• None

Effects of drug abuse

• None

Short-Term Effects

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

Long-Term Effects

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

Cautions

• ILD/pneumonitis, which can be fatal, is reported; monitor for new or worsening pulmonary symptoms indicative of ILD/pneumonitis
• Cardiac toxicity (including decreased EF, cardiomyopathy, and congestive HF) resulting in HF, may occur; monitor cardiac function (eg, assessment of left ventricular EF at baseline and during treatment)
• May cause fetal harm
• QTc prolongation and torsades de pointes
• Life-threatening QTc prolongation, including torsades de pointes, reported
• Assess QTc and electrolytes at baseline and correct abnormalities in sodium, potassium, calcium, and magnesium before initiating therapy
• Diarrhea
  • Severe diarrhea reported
  • Median time to first onset of diarrhea was 5 days; diarrhea occurred within 24 hours after administration
  • Diarrhea may lead to dehydration or electrolyte imbalance, with or without renal impairment; treat diarrhea promptly
  • Advise patients to start an antidiarrheal agent (eg, loperamide) at the first sign of diarrhea or increased bowel movement frequency and to increase fluid and electrolyte intake
• Monitor electrolytes
• Drug interaction overview
  • CYP3A4 substrate
    • Moderate CYP3A4 inducer
    • Inhibitor of breast cancer resistance protein (BCRP); the clinical significance of changes in the pharmacokinetics of sulfasalazine (a BCRP substrate) when coadministered with multiple doses of mobocertinib is unknown
  • Strong or moderate CYP3A4 inhibitors
  • Avoid coadministration
    • If the use of moderate CYP3A4 inhibitors is unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently
    • Strong or moderate CYP3A4 inhibitors may increase mobocertinib plasma concentrations and toxicities, including QTc interval
  • Strong or moderate CYP3A4 inducers
  • Avoid coadministration
    • Strong or moderate CYP3A4 inducers may decrease mobocertinib plasma concentrations and antitumor activity
  • Sensitive CYP3A4 substrates
    • Avoid coadministration with hormonal contraceptives OR other CYP3A4 substrates where minimal concentration changes may lead to serious therapeutic failures
    • If use is unavoidable, increase CYP3A4 substrate dosage in accordance with its prescribing information
    • Mobocertinib may decrease plasma concentrations of CYP3A4 substrates
  • Drugs that prolong QTc interval
  • Avoid coadministration
    • If coadministration is unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently

Pregnancy and Lactation

• Based on findings from animal studies and its mechanism of action, may cause fetal harm when administered to pregnant females
• No data are available on use in pregnant females
• Verify pregnancy status in females of reproductive potential
• Contraception
  • Females of reproductive potential: Use effective nonhormonal contraception during treatment and for 1 month after the last dose; mobocertinib may render hormonal contraceptives ineffective
  • Males with female partners of reproductive potential: Use effective contraception during treatment and for 1 week after the last dose
• Infertility
  • Based on animal studies, fertility in males and females of reproductive potential may be impaired
• Lactation
  • There are no data on the presence of mobocertinib or its metabolites in human milk, its effects on breastfed children, or its effects on milk production
  • Advise women not to breastfeed during treatment and for 1 week after the last dose