Abemaciclib

Breast Neoplasms

DRUG STATUS

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Approvals

US(FDA), UK(BNF)

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Essential Medicine

YES

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Teratogenicity

Unlisted

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Pharmaceutical Class

Kinase Inhibitor

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Drug Ingredient

Abemaciclib

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Summary

  • Abemaciclib is used to treat hormone receptor-positive, HER2-negative breast cancer. It can be used in both early and advanced stages of the disease. It's also used for advanced breast cancer that has progressed after prior treatments.

  • Abemaciclib works by inhibiting proteins called cyclin-dependent kinases 4 and 6. These proteins are crucial for cell division. By blocking these proteins, Abemaciclib slows or stops the growth of cancer cells.

  • Abemaciclib is typically prescribed for adults. The recommended dose is 150 mg taken orally twice daily. It can be used in combination with other therapies.

  • Common side effects of Abemaciclib include diarrhea, nausea, fatigue, and neutropenia. Serious adverse effects can include severe diarrhea, hepatotoxicity, and venous thromboembolism.

  • Abemaciclib can cause severe diarrhea, neutropenia, hepatotoxicity, and venous thromboembolism. It's contraindicated in patients with hypersensitivity to the drug or its components. It's also advised to avoid strong CYP3A4 inhibitors and inducers.

Indications and Purpose

What is Abemaciclib used for?

Abemaciclib is indicated for the treatment of hormone receptor-positive, HER2-negative breast cancer. It is used in combination with other therapies for early breast cancer at high risk of recurrence and for advanced or metastatic breast cancer. It can also be used as monotherapy for advanced breast cancer that has progressed after prior treatments.

How does Abemaciclib work?

Abemaciclib works by inhibiting cyclin-dependent kinases 4 and 6 (CDK4 and CDK6), which are enzymes that play a crucial role in cell division. By blocking these enzymes, Abemaciclib prevents cancer cells from progressing through the cell cycle, thereby slowing or stopping their growth and proliferation.

Is Abemaciclib effective?

Abemaciclib has been shown to be effective in clinical trials for treating hormone receptor-positive, HER2-negative breast cancer. In studies like MONARCH 2 and MONARCH 3, Abemaciclib, in combination with other therapies, significantly improved progression-free survival compared to placebo. These trials demonstrate its efficacy in both early and advanced stages of breast cancer.

How does one know if Abemaciclib is working?

The benefit of Abemaciclib is evaluated through regular monitoring of the patient's response to treatment, including imaging studies and laboratory tests to assess disease progression or recurrence. Healthcare providers also monitor for side effects and adjust the dosage as needed to ensure the medication is providing the intended therapeutic benefit.

Directions for Use

What is the usual dose of Abemaciclib?

Abemaciclib is typically prescribed for adults, with a recommended dose of 150 mg taken orally twice daily when used in combination with other therapies. As for children, the safety and effectiveness of Abemaciclib have not been established, and it is not typically prescribed for pediatric use.

How do I take Abemaciclib?

Abemaciclib should be taken orally, usually twice daily, with or without food. Patients are advised to take the medication at the same times each day. It is important to avoid grapefruit and grapefruit juice while taking Abemaciclib, as they can interact with the medication and affect its effectiveness.

For how long do I take Abemaciclib?

For early breast cancer, Abemaciclib is usually taken continuously for two years or until disease recurrence or unacceptable toxicity occurs. For advanced or metastatic breast cancer, it is taken continuously as long as the patient is deriving clinical benefit from therapy or until unacceptable toxicity occurs.

How long does it take for Abemaciclib to start working?

The content does not specify exactly how long it takes for Abemaciclib to start working. However, patients typically begin to see effects within the first few weeks of treatment, as the medication works to inhibit cancer cell growth. The exact timeline can vary depending on individual response and the specific condition being treated.

How should I store Abemaciclib?

Abemaciclib should be stored at room temperature, between 20°C to 25°C (68°F to 77°F), and kept in its original container, tightly closed, and out of reach of children. It should be stored away from excess heat and moisture, and not in the bathroom. Unused medication should be disposed of properly, preferably through a take-back program.

Warnings and Precautions

Who should avoid taking Abemaciclib?

Important warnings for Abemaciclib include the risk of severe diarrhea, neutropenia, hepatotoxicity, and venous thromboembolism. Patients should be monitored for these conditions, and dose adjustments may be necessary. Abemaciclib is contraindicated in patients with hypersensitivity to the drug or its components. It is also advised to avoid strong CYP3A4 inhibitors and inducers.

Can I take Abemaciclib with other prescription drugs?

Abemaciclib interacts with strong CYP3A4 inhibitors, which can increase its concentration and risk of toxicity. It is advised to avoid these inhibitors, such as ketoconazole. Moderate CYP3A4 inhibitors may also require dose adjustments. Additionally, strong CYP3A4 inducers can decrease Abemaciclib's effectiveness and should be avoided.

Can I take Abemaciclib with vitamins or supplements?

The content does not specifically mention interactions between Abemaciclib and vitamins or supplements. However, it is important for patients to inform their healthcare provider about all supplements they are taking, as some may interact with the medication. St. John's wort, a common herbal supplement, is known to interact with many medications and should be avoided.

Can Abemaciclib be taken safely while pregnant?

Abemaciclib can cause fetal harm when administered to a pregnant woman, based on animal studies and its mechanism of action. It is advised that females of reproductive potential use effective contraception during treatment and for at least 3 weeks after the last dose. There is no strong evidence from human studies, but the potential risk to a fetus is significant.

Can Abemaciclib be taken safely while breastfeeding?

It is not known if Abemaciclib is excreted in human milk, but due to the potential for serious adverse reactions in breastfed infants, it is recommended that women do not breastfeed during treatment and for at least 3 weeks after the last dose of Abemaciclib.

Is Abemaciclib safe for the elderly?

The content indicates that no overall differences in safety or effectiveness of Abemaciclib were observed between elderly patients and younger patients. However, elderly patients may be more susceptible to certain side effects, such as neutropenia and diarrhea. It is important for elderly patients to be closely monitored by their healthcare provider while taking Abemaciclib.

Is it safe to exercise while taking Abemaciclib?

The content does not specifically address whether Abemaciclib limits the ability to exercise. However, fatigue is a common side effect, which might affect physical activity levels. Patients should discuss their exercise plans with their healthcare provider to ensure safety and adjust activities as needed.

Is it safe to drink alcohol while taking Abemaciclib?

The provided content does not specifically mention the effects of alcohol on the safety or effectiveness of Abemaciclib. However, it is generally advisable to consult with a healthcare provider regarding alcohol consumption while taking any medication, as alcohol can potentially interact with medications and affect their efficacy or increase side effects.