Exkivity

Exkivity (mobocertinib) is a tyrosine kinase inhibitor (TKI) used to treat non-small cell lung cancer (NSCLC) that has a specific EGFR gene mutation. Exkivity reduces the growth of non-small cell lung cancer by binding to and inhibiting EGFR exon 20 insertion mutations.

Exkivity capsules can be used by adults with non-small cell lung cancer that has spread to other parts of the body (metastatic) and cannot be removed with surgery, whose disease has worsened while on or after chemotherapy with platinum, and has cancer has epidermal growth factor receptor (EGFR) exon 20 insertion mutation.

Epidermal growth factor receptor (EGFR) is a protein that helps cells to grow and divide. When EGFR has an exon 20 insertion mutation, it drives cells to grow and divide abnormally, causing an EGFR-positive cancer. Exkivity works by binding to and blocking EGFR exon 20 insertion mutations, which helps to slow the growth of cancer cells.

Exkivity was granted accelerated FDA approval in 2021 based on results from the clinical trial NCT02716116. It is used with the Oncomine Dx Target Test, which identifies patients with exon 20 insertion mutations.

Follow all directions on your prescription label and read all medication guides or instruction sheets.

• Exkivity capsules should be taken exactly as directed.
• Exkivity capsule can be taken with or without food.
• Swallow the capsule whole and do not crush, chew, break, or open it.
• You should not stop using this medicine without your doctor's advice.
• Your cancer treatments may be delayed or permanently stopped if you have specific side effects.

Exkivity may cause changes in the electrical activity of your heart called QTc prolongation and Torsades de Pointes. QTc prolongation can cause irregular heartbeats that can be life-threatening and may lead to death. Your healthcare provider will check the electrical activity of your heart with a test called an electrocardiogram (ECG) and do blood tests to check your electrolytes before starting, and during treatment.

Call your doctor right away if you have fast or pounding heartbeats, fluttering in your chest, shortness of breath, and sudden dizziness (like you might pass out).

Tell your doctor if you have:

• heart problems, including long QT syndrome;
• an electrolyte imbalance (such as low blood levels of sodium, potassium, calcium, or magnesium); or
• lung or breathing problems other than lung cancer.

Pregnancy

Exkivity can harm an unborn baby if the mother or father is using this medicine. You may need to have a negative pregnancy test before starting this treatment.

• Both men and women using this medicine should use effective birth control to prevent pregnancy.
• Keep using birth control for at least 1 month for women and at least 1 week for men after your last dose. Tell your doctor right away if a pregnancy occurs.
• Exkivity can make birth control pills less effective. Ask your doctor about other birth control options such as an injection, implant, skin patch, vaginal ring, condom, diaphragm, cervical cap, or contraceptive sponge.
• Exkivity may affect fertility in men or women. Pregnancy could be harder to achieve while either parent is using this medicine.

Breastfeeding

• Do not breastfeed while using this medicine, and for at least 1 week after your last dose.

Get emergency medical help if you have signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Common Exkivity side effects may include:

• diarrhea, vomiting, nausea, decreased appetite;
• rash, dry skin, skin infection around nails;
• tiredness;
• mouth sores; or
• muscle or joint pain.

Exkivity may cause serious side effects.

Call your doctor at once if you have any symptoms listed below:

Lung problems. Exkivity may cause severe lung problems that may lead to death. Symptoms may be similar to those symptoms from lung cancer. Tell your healthcare provider right away if you develop any

• new or worsening breathing problems or shortness of breath, cough, or fever;

Heart problems, including heart failure. Exkivity may cause heart problems that may lead to death. Your healthcare provider should check your heart function before you start and during treatment. Tell your healthcare provider right away if you have any signs or symptoms of a heart problem, including

• fast or pounding heartbeats, fluttering in your chest, swelling in your ankles or feet, chest pain, and sudden dizziness (like you might pass out); or

Diarrhea. Diarrhea is common during treatment, and may sometimes be severe. Diarrhea can cause you to lose too much body fluid (dehydration) and kidney problems. Your healthcare provider may tell you to start drinking more fluids and electrolytes to replace body salts or start taking your antidiarrheal medicines. Tell your healthcare provider right away if you have any loose stools or have stools more often than is normal for you.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Usual Adult Dose of Exkivity for EGFR Exon20 Insertion+ Non-Small Cell Lung Cancer

• 160 mg orally once daily, with or without food.

Comment

Dose may be modified due to adverse reactions (side effects) or when taking other medication that has a drug interaction with Exkivity. To check dosage modifications in these circumstances click the link below.

Use the medicine as soon as you can, but skip the missed dose if you are more than 6 hours late for the dose. Do not use two doses at one time.

If you vomit shortly after taking this medicine, do not take another dose. Take your next dose as scheduled.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Grapefruit may interact with Exkivity and cause side effects. Avoid consuming grapefruit or drinking grapefruit juice products during treatment with this medicine.

Tell your healthcare provider about all the medicines you take, including prescription medicines and over-the-counter medicines, vitamins, and herbal supplements. Tell your healthcare provider if you take medicines for heart problems.

Exkivity and other medicines may affect each other causing serious side effects.

Especially tell your doctor if you are taking the following medicines:

• cyclosporine
• mifepristone
• nefazodone
• aprepitant
• antibiotics - clarithromycin, erythromycin, ciprofloxacin
• antifungal medicines - fluconazole, itraconazole, ketoconazole, posaconazole, voriconazole
• heart or blood pressure medicine - amiodarone, diltiazem, verapamil
• HIV medicines containing ritonavir, darunavir, indinavir, nelfinavir, saquinavir or cobicistat
• antipsychotics - chlorpromazine, haloperidol, droperidol, quetiapine, olanzapine, amisulpride, thioridazine
• antiarrhythmics - quinidine, procainamide, disopyramide, flecainide, sotalol, amiodarone
• antidepressants - fluvoxamine, amitriptyline, doxepin, imipramine, nortriptyline, desipramine, citalopram, escitalopram, venlafaxine, bupropion
• antihistamines - diphenhydramine, loratadine

Store at room temperature between 68°F to 77°F (20°C to 25°C), away from moisture and heat.

Active ingredient: mobocertinib

Inactive ingredients: None

Capsule shells: gelatin and titanium dioxide. The printing ink contains shellac, dehydrated alcohol, isopropyl alcohol, butyl alcohol, propylene glycol, strong ammonia solution, black iron oxide, potassium hydroxide, and purified water.

Distributed by: Takeda Pharmaceuticals America, Inc., Lexington, MA 02421.