Verzenio 100mg Tablets

Abemaciclib is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6). These kinases are activated by binding to D-cyclins and play a crucial role in regulating cell cycle progression from G1 to S phase. In many cancers, including HR-positive breast cancer, CDK4/6 are overactive, leading to uncontrolled cell proliferation. By inhibiting CDK4/6, abemaciclib prevents retinoblastoma protein (Rb) phosphorylation, leading to G1 cell cycle arrest and reduced tumor cell proliferation.

Urgent Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek emergency medical attention:

Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat
Signs of infection: fever, chills, severe sore throat, ear or sinus pain, cough, increased or changed sputum production, painful urination, mouth sores, or a wound that won't heal
Signs of liver problems: dark urine, fatigue, decreased appetite, stomach upset or pain, light-colored stools, vomiting, or yellow skin and eyes
Signs of fluid and electrolyte imbalance: mood changes, confusion, muscle pain or weakness, irregular or rapid heartbeat, severe dizziness or fainting, increased thirst, seizures, extreme fatigue or weakness, decreased appetite, difficulty urinating or changes in urine output, dry mouth, dry eyes, or severe stomach upset or vomiting
Unusual fatigue or weakness
Unexplained bruising or bleeding
Swelling in the arms or legs
Rapid breathing
Rapid heartbeat
Signs of a blood clot: chest pain or pressure, coughing up blood, shortness of breath, swelling, warmth, numbness, color changes, or pain in a leg or arm, or difficulty speaking or swallowing
Signs of lung problems: shortness of breath, difficulty breathing, new or worsening cough, or fever (note: lung problems have been reported with this medication, and in some cases, have been fatal)

Other Possible Side Effects

Like all medications, this drug can cause side effects. While many people may not experience any side effects or only mild ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects, contact your doctor if they bother you or persist:

Constipation, diarrhea, stomach pain, upset stomach, vomiting, or decreased appetite
Hair loss or thinning
Dizziness, fatigue, or weakness
Headache
Dry mouth
Mouth irritation or sores
Joint pain
Changes in taste
Weight loss
Signs of a common cold
Nose or throat irritation

Reporting Side Effects

This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you are currently taking any of the following medications: carbamazepine, ketoconazole, phenobarbital or similar drugs, rifampin, ritonavir, or St. John's wort.
If you are breastfeeding. Note that you should not breastfeed while taking this medication and for 3 weeks after your last dose.

Please be aware that this is not an exhaustive list of all potential interactions with this medication. To ensure your safety, it is crucial to:

Inform your doctor and pharmacist about all the medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins.
Discuss all your health problems with your doctor.
Verify that it is safe to take this medication with all your other medications and health conditions.
* Never start, stop, or change the dose of any medication without first consulting your doctor.

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.

Diarrhea is a common side effect of this drug, and in some cases, it can be severe, leading to dehydration or infection. Diarrhea typically occurs during the first month of treatment. If you experience diarrhea, follow the instructions provided by your doctor. If you are unsure about how to manage diarrhea, consult with your doctor.

Regular blood tests will be necessary as directed by your doctor. Discuss any concerns or questions you have with your doctor.

You may be at a higher risk of developing infections, some of which can be severe or life-threatening. To minimize this risk, practice good hygiene by washing your hands frequently, avoid close contact with individuals who have infections, colds, or flu, and consult with your doctor before receiving any vaccinations. Note that certain vaccines may not be effective or may increase the risk of infection when taken with this medication.

This medication may increase your risk of bleeding. Be cautious and take steps to avoid injury. Use a soft-bristled toothbrush and an electric razor to minimize the risk of bleeding.

There is a risk of developing blood clots while taking this medication, which can be life-threatening. Discuss this risk with your doctor.

Avoid consuming grapefruit and grapefruit juice while taking this medication.

If you are taking other medications in conjunction with this drug, discuss the potential risks and side effects with your doctor. This medication may affect fertility in men, so it is essential to discuss this with your doctor.

This medication can cause harm to an unborn baby. A pregnancy test will be conducted before initiating treatment to confirm that you are not pregnant. If you may become pregnant, you must use effective birth control while taking this medication and for a specified period after the last dose. Your doctor will advise you on the duration of birth control use. If you become pregnant while taking this medication, notify your doctor immediately.

• Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, cobicistat, grapefruit juice) - concomitant use should be avoided. If unavoidable, reduce abemaciclib dose.
• Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's Wort) - concomitant use should be avoided.

• Moderate CYP3A4 inhibitors (e.g., erythromycin, diltiazem, verapamil, fluconazole) - monitor for increased abemaciclib toxicity.
• Moderate CYP3A4 inducers (e.g., bosentan, efavirenz, etravirine, modafinil, nafcillin) - monitor for decreased abemaciclib efficacy.

• Diarrhea (frequency, consistency)
• Fatigue
• Nausea
• Abdominal pain
• Infections (fever, chills, sore throat)
• Signs of deep vein thrombosis (DVT) or pulmonary embolism (PE) (e.g., leg swelling, pain, redness; chest pain, shortness of breath, rapid heart rate)
• Signs of interstitial lung disease/pneumonitis (e.g., dyspnea, cough, fever)
• Signs of liver dysfunction (e.g., jaundice, dark urine, right upper quadrant pain)

Abemaciclib can cause fetal harm when administered to a pregnant woman. Based on animal studies and its mechanism of action, abemaciclib is expected to cause adverse developmental effects. Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment and for 3 weeks after the last dose.

It is not known whether abemaciclib or its metabolites are present in human milk. Because of the potential for serious adverse reactions in breastfed infants, advise lactating women not to breastfeed during treatment with abemaciclib and for 3 weeks after the last dose.

The safety and effectiveness of abemaciclib in pediatric patients have not been established. Not indicated for pediatric use.

No overall differences in safety or effectiveness were observed between patients ≥65 years of age and younger patients. No dose adjustment is required based on age alone.

• Diarrhea is the most common adverse event and typically occurs early in treatment (median onset 6-8 days). Proactive management with loperamide at the first sign of loose stools is crucial. Dose reduction or interruption may be necessary.
• Neutropenia is also common but generally manageable. Monitor CBCs closely, especially during the first two cycles.
• Abemaciclib has demonstrated activity in CNS metastases, which is a notable advantage compared to some other CDK4/6 inhibitors.
• Patients should be educated on the importance of avoiding strong CYP3A4 inhibitors (including grapefruit) and inducers.
• Consider dose reductions for moderate and severe hepatic impairment as per guidelines.
• Verzenio is approved for both metastatic and early breast cancer settings, including adjuvant therapy for high-risk patients.

• Endocrine therapy alone (e.g., aromatase inhibitors, fulvestrant)
• Chemotherapy (e.g., capecitabine, eribulin)
• Everolimus + Exemestane (for HR+/HER2- advanced breast cancer after failure of nonsteroidal aromatase inhibitor)

If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.