Verzenio 50mg Tablets

Abemaciclib is a cyclin-dependent kinase (CDK) 4 and 6 inhibitor. These kinases are activated by binding to D-cyclins. In estrogen receptor-positive (ER+) breast cancer cells, cyclin D1-CDK4/6 complexes promote cell proliferation by phosphorylating and inactivating the retinoblastoma (Rb) tumor suppressor protein, allowing progression from G1 to S phase of the cell cycle. In vitro, abemaciclib inhibited Rb phosphorylation and blocked progression from G1 to S phase, leading to cell senescence and apoptosis. In breast cancer xenograft models, abemaciclib alone or in combination with antiestrogens reduced tumor size.

Serious Side Effects: Seek Medical Help Immediately

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 or seek medical attention right away:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of infection, including:
+ Fever
+ Chills
+ Severe sore throat
+ Ear or sinus pain
+ Cough
+ Increased sputum production or change in sputum color
+ Painful urination
+ Mouth sores
+ Wounds that won't heal
Signs of liver problems, such as:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Signs of fluid and electrolyte problems, including:
+ Mood changes
+ Confusion
+ Muscle pain or weakness
+ Abnormal heartbeat
+ Severe dizziness or fainting
+ Increased thirst
+ Seizures
+ Feeling extremely tired or weak
+ Decreased appetite
+ Urination problems or changes in urine output
+ Dry mouth
+ Dry eyes
+ Severe stomach upset or vomiting
Extreme fatigue or weakness
Unexplained bruising or bleeding
Swelling in the arms or legs
Rapid breathing
Rapid heartbeat
Signs of a blood clot, such as:
+ Chest pain or pressure
+ Coughing up blood
+ Shortness of breath
+ Swelling, warmth, numbness, color change, or pain in a leg or arm
+ Difficulty speaking or swallowing
Lung problems, including:
+ Shortness of breath or other breathing difficulties
+ New or worsening cough
+ Fever

Other Possible Side Effects

Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. If you notice any of the following side effects, contact your doctor or seek medical attention if they bother you or persist:

Constipation
Diarrhea
Stomach pain
Upset stomach
Vomiting
Decreased appetite
Hair loss
Hair thinning
Dizziness
Fatigue
Weakness
Headache
Dry mouth
Mouth irritation or sores
Joint pain
Change in taste
Weight loss
Common cold symptoms
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 about side effects, 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 allergic reaction you experienced.
If you are currently taking or plan to take 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.

This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication with 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.

While taking this drug, you may experience diarrhea, which can sometimes be severe and lead to dehydration or infection. Diarrhea typically occurs during the first month of treatment. If you develop 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.

As this medication may increase your risk of developing infections, some of which can be severe or life-threatening, it is crucial to take preventive measures. Wash your hands frequently, avoid close contact with people 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.

You may be more prone to bleeding while taking this drug. To minimize the risk of injury, exercise caution and use a soft toothbrush and an electric razor.

There is a risk of developing blood clots, which can be fatal, associated with this medication. 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. Additionally, 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 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, notify your doctor immediately.

• Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, grapefruit juice)
• Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's Wort)

• Moderate CYP3A4 inhibitors (e.g., erythromycin, diltiazem, verapamil)
• CYP3A4 substrates with narrow therapeutic index (e.g., midazolam, alfentanil, cyclosporine, everolimus, fentanyl, sirolimus, tacrolimus)

• Diarrhea (frequency, consistency of stools)
• Fever, chills, sore throat, or other signs of infection (due to neutropenia)
• Unusual bruising or bleeding (due to thrombocytopenia)
• Fatigue, weakness, dizziness
• Nausea, vomiting, abdominal pain
• Yellowing of skin or eyes (jaundice), dark urine, right upper quadrant pain (signs of liver toxicity)
• Shortness of breath, chest pain, swelling in legs (signs of VTE)
• New or worsening cough, dyspnea, chest discomfort (signs of ILD/pneumonitis)

Verzenio can cause fetal harm when administered to a pregnant woman based on animal studies and its mechanism of action. Advise pregnant women of the potential risk to the fetus. Advise females of reproductive potential to use effective contraception during treatment and for 3 weeks after the last dose.

Advise lactating women not to breastfeed during treatment with Verzenio and for 3 weeks after the last dose due to the potential for serious adverse reactions in breastfed infants.

The safety and effectiveness of Verzenio in pediatric patients have not been established.

No dose adjustment is required based on age. Clinical studies included patients 65 years and older, and no overall differences in safety or effectiveness were observed between these patients and younger patients.

• Abemaciclib is the only CDK4/6 inhibitor approved for continuous daily dosing, which may contribute to its higher rates of diarrhea compared to intermittent dosing regimens of other CDK4/6 inhibitors.
• Proactive management of diarrhea is crucial. Patients should be educated to start antidiarrheal agents (e.g., loperamide) at the first sign of loose stools and to maintain hydration.
• Neutropenia is a common adverse event, but febrile neutropenia is less common than with some other chemotherapy agents. Regular CBC monitoring is essential.
• Liver function tests must be monitored regularly, especially during the initial cycles, due to the risk of hepatotoxicity.
• Abemaciclib has demonstrated CNS penetration, which may be relevant in patients with brain metastases, though specific efficacy in this setting is still under investigation.
• Patients should be advised to avoid grapefruit products due to the risk of increased abemaciclib exposure.

• Endocrine therapy alone (e.g., aromatase inhibitors, fulvestrant, tamoxifen)
• Chemotherapy (e.g., capecitabine, eribulin, paclitaxel)
• Targeted therapies (e.g., everolimus, alpelisib, capivasertib)
• Immunotherapy (in specific contexts)

If your symptoms or health issues persist or worsen, it's 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 be sure to check with your pharmacist for more details. 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 for clarification. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide information about the medication taken, the amount, and the time it happened, as this will help healthcare professionals provide the best possible care.