Abemaciclib

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Generic Name: Abemaciclib Brand Name(s): Generics only. No brands available. Avability: Rx Pregnancy Category: N

Uses

What is Abemaciclib used for?

Abemaciclib is used to treat certain types of breast cancer. Abemaciclib works by slowing or stopping the growth of cancer cells. It belongs to a class of drugs known as kinase inhibitors.

How should I take Abemaciclib?

Take this medication by mouth with or without food as directed by your doctor, usually two times daily. Swallow the tablet whole with a glass of water. Do not chew, crush, or split the tablets. Do not take tablets that are broken, cracked, or not whole.

The dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). If you have certain side effects, your doctor may adjust your dose or stop treatment for some time.

Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of serious side effects will increase.

If you vomit your dose of abemaciclib, do not take another dose. Take your next dose at your regular scheduled time. Do not take two doses at the same time.

Take this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.

Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.

How do I store Abemaciclib?

Abemaciclib is best stored at room temperature away from direct light and moisture. To prevent drug damage, you should not store Abemaciclib in the bathroom or the freezer. There may be different brands of Abemaciclib that may have different storage needs. It is important to always check the product package for instructions on storage, or ask your pharmacist. For safety, you should keep all medicines away from children and pets.

You should not flush Abemaciclib down the toilet or pour them into a drain unless instructed to do so. It is important to properly discard this product when it is expired or no longer needed. Consult your pharmacist for more details about how to safely discard your product.

Precautions & warnings

What should I know before using Abemaciclib?

Before taking abemaciclib, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, bleeding/clotting problems (such as bleeding from intestinal/stomach ulcers).

Abemaciclib can make you more likely to get infections or may worsen any current infections. Avoid contact with people who have infections that may spread to others (such as chickenpox, measles, flu). Consult your doctor if you have been exposed to an infection or for more details.

Do not have immunizations/vaccinations without the consent of your doctor. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).

This drug may make you dizzy. Alcohol or marijuana can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.

Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while using abemaciclib. Abemaciclib may harm an unborn baby. Ask about reliable forms of birth control while using this medication and for at least 3 weeks after stopping treatment. If you become pregnant, talk to your doctor right away about the risks and benefits of this medication.

It is unknown if this drug passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug and for at least 3 weeks after stopping treatment is not recommended. Consult your doctor before breast-feeding.

Is it safe during pregnancy or breast-feeding?

There are no adequate studies in women for determining risk when using this Abemaciclib during pregnancy or while breastfeeding. Please always consult with your doctor to weigh the potential benefits and risks before taking Abemaciclib. Abemaciclib is pregnancy risk category N according to the US Food and Drug Administration (FDA).

FDA pregnancy risk category reference below:

  • A=No risk,
  • B=No risk in some studies,
  • C=There may be some risk,
  • D=Positive evidence of risk,
  • X=Contraindicated,
  • N=Unknown

Side effects

What side effects can occur from Abemaciclib?

Nausea, vomiting, upset stomach, loss of appetite, weight loss, constipation, tiredness/weakness, headache, or change in how food tastes may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

Diarrhea is a common side effect that can cause a serious loss of body water (dehydration). Tell your doctor right away if you have loose stools, and ask if you should take anti-diarrheal medication (such as loperamide). Drink plenty of fluids to reduce the risk of dehydration. Contact your doctor promptly if you notice any symptoms of dehydration, such as unusual decreased urination, unusual dry mouth/thirst, fast heartbeat, or dizziness/lightheadedness.

Temporary hair loss may occur. Normal hair growth should return after treatment has ended.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: unusual tiredness, easy bruising or bleeding (such as nose/gum bleeds, pink/dark urine), signs of liver damage (such as nausea/vomiting that doesn’t stop, loss of appetite, stomach/abdominal pain, yellowing eyes/skin, dark urine).

This medication may lower your ability to fight infections. This may make you more likely to get a serious (rarely fatal) infection or make any infection you have worse. Tell your doctor right away if you have any signs of infection (such as sore throat that doesn’t go away, fever, chills, cough).

This medication may rarely cause blood clots (such as pulmonary embolism, stroke, heart attack, deep vein thrombosis). You may be at increased risk for blood clots if you are severely dehydrated, or have a history of blood clots, or if you are immobile (such as on very long plane flights or being bedridden). If you use estrogen-containing products, these may also increase your risk. Before using this medication, if you have any of these conditions report them to your doctor or pharmacist. Get medical help right away if any of these side effects occur: shortness of breath/rapid breathing, chest/jaw/left arm pain, unusual sweating, confusion, sudden dizziness/fainting, pain/swelling/warmth in the groin/calf, sudden severe headaches, trouble speaking, weakness on one side of the body, sudden vision changes.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

Not everyone experiences these side effects. There may be some side effects not listed above. If you have any concerns about a side-effect, please consult your doctor or pharmacist.

Interactions

What drugs may interact with Abemaciclib?

Other medications can affect the removal of abemaciclib from your body, which may affect how abemaciclib works. Examples include azole antifungals (such as ketoconazole, itraconazole, voriconazole), macrolide antibiotics (such as clarithromycin), HIV protease inhibitors (such as ritonavir, atazanavir, nelfinavir, saquinavir, indinavir), rifamycins (such as rifampin, rifabutin), drugs to treat seizures (such as phenytoin, carbamazepine, phenobarbital), nefazodone, St. John’s wort, telithromycin, among others.

Abemaciclib may interact with other drugs that you are currently taking, which can change how your drug works or increase your risk for serious side effects. To avoid any potential drug interactions, you should keep a list of all the drugs you are using (including prescription drugs, nonprescription drugs and herbal products) and share it with your doctor and pharmacist. For your safety, do not start, stop, or change the dosage of any drugs without your doctor’s approval.

Does food or alcohol interact with Abemaciclib?

Abemaciclib may interact with food or alcohol by altering the way the drug works or increase the risk for serious side effects. Please discuss with your doctor or pharmacist any potential food or alcohol interactions before using this drug.

Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor or pharmacist says you may do so safely. Grapefruit can increase the chance of side effects with this medicine. Ask your doctor or pharmacist for more details.

What health conditions may interact with Abemaciclib?

Abemaciclib may interact with your health condition. This interaction may worsen your health condition or alter the way the drug works. It is important to always let your doctor and pharmacist know all the health conditions you currently have.

Dosage

The information provided is not a substitute for any medical advice. You should ALWAYS consult with your doctor or pharmacist before using this Abemaciclib.

What is the dose of Abemaciclib for an adult?

Usual Adult Dose for Breast Cancer

-As Combination Therapy: 150 mg orally twice a day

-As Monotherapy: 200 mg orally twice a day

-Duration of Therapy: Until disease progression or unacceptable toxicity

Comments:

-If using this drug in combination with fulvestrant on pre/perimenopausal women, treat these patients with a gonadotropin-releasing hormone agonist according to current clinical practice standards.

-When used in combination with this drug, the recommended dose of fulvestrant is 500 mg on Days 1, 15, and 29, then once monthly thereafter; refer to the manufacturer product information for fulvestrant.

Use: Treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer:

-as combination therapy with fulvestrant in adult women with disease progression following endocrine therapy OR

-as monotherapy in adult patients with disease progression following endocrine therapy AND prior chemotherapy in the metastatic setting

Renal Dose Adjustments

-Mild to Moderate Renal Impairment (CrCl 30 to 89 mL/min): No adjustment recommended

Liver Dose Adjustments

-Mild or Moderate Hepatic Impairment (Child-Pugh A or B): No adjustment recommended

-Severe Hepatic Impairment (Child-Pugh C): Reduce the dosing frequency to once a day

Management of Hepatotoxicity:

-Grade 1 (greater than upper limit of normal [ULN] to 3 x ULN) OR Grade 2 (greater than 3 to 5 x ULN); WITHOUT Increase in Total Bilirubin Above 2 x ULN: No adjustment recommended

-Persistent or Recurrent Grade 2 OR Grade 3 (greater than 5 to 20 x ULN); WITHOUT Increase in Total Bilirubin Above 2 x ULN: Suspend dose until toxicity resolves to baseline or Grade 1; resume at next lower dose

-Elevation in AST AND/OR ALT Greater Than 3 x ULN WITH Total Bilirubin Greater Than 2 x ULN In the Absence of Cholestasis OR Grade 4 (greater than 20 x ULN): Discontinue this drug

Comments: Monitor ALT, AST, and serum bilirubin prior to drug initiation, every 2 weeks for the first 2 months, monthly for the next 2 months, and as clinically indicated.

Dose Adjustments

CONCOMITANT USE of KETOCONAZOLE: Not recommended

CONCOMITANT USE of OTHER STRONG CYP450 3A INHIBITORS (excluding ketoconazole):

-In Patients with Starting Doses of 150 to 200 mg Twice a Day: 100 mg twice a day

-In Patients Who Already Had a Dose Reduction to 100 mg Twice a Day Due to Adverse Reactions: 50 mg twice a day

-Once Patient Discontinues Concomitant Use of Strong CYP450 3A Inhibitor: After 3 to 5 half-lives of the inhibitor, increase the dose of this drug to the dose that was used BEFORE the strong inhibitor was started.

MANAGEMENT of ADVERSE REACTIONS:

First Dose Reduction:

-Combination Therapy: 100 mg twice a day

-Monotherapy: 150 mg twice a day

Second Dose Reduction:

-Combination Therapy: 50 mg twice a day

-Monotherapy: 100 mg twice a day

Third Dose Reduction:

-Combination Therapy: N/A

-Monotherapy: 50 mg twice a day

DIARRHEA:

-Grade 1: No adjustment recommended

-Grade 2: If toxicity does not resolve within 24 hours to Grade 1 or less, suspend dose until resolution; dose reduction not required

-Persistent or Recurrent Grade 2 (persists or recurs after resuming the same dose despite maximal supportive measures): Suspend dose until toxicity resolves to Grade 1 or less; resume at next lower dose

-Grade 3 or 4 OR Hospitalization Required: Suspend dose until toxicity resolves to Grade 1 or less; resume at next lower dose

HEMATOLOGIC TOXICITIES:

-Grade 1 or 2: No adjustment recommended

-Grade 3: Suspend dose until toxicity resolves to Grade 2 or less; dose reduction not required

-Recurrent Grade 3 OR Grade 4: Suspend dose until toxicity resolves to Grade 2 or less; resume at next lower dose

-If Blood Cell Growth Factors (BCGF) Required: Suspend dose for at least 48 hours AFTER the last dose of BCGF and until toxicity resolves to Grade 2 or less; resume at next lower dose unless already performed for the toxicity that led to the use of the growth factor; use growth factor per current treatment guidelines

OTHER TOXICITIES (excluding diarrhea, hematologic toxicity, and hepatotoxicity):

-Grade 1 or 2: No adjustment recommended

-Persistent or Recurrent Grade 2 (does not resolve within 7 days to baseline or Grade 1 despite maximal supportive measures): Suspend dose until toxicity resolves to baseline or Grade 1 or less; resume at next lower dose

-Grade 3 or 4: Suspend dose until toxicity resolves to baseline or Grade 1 or less; resume at next lower dose

Comments:

-ADVERSE REACTIONS: Discontinue this drug if the patient is unable to tolerate 50 mg twice a day.

-DIARRHEA: At the first sign of loose stools, start treatment with antidiarrheal agents and increase intake of oral fluids.

-GENERAL: Consult the manufacturer product information for appropriate dose adjustments for co-administered fulvestrant.

-HEMATOLOGIC TOXICITIES: Monitor complete blood counts (CBC) prior to treatment initiation, every 2 weeks for the first 2 months, monthly for the next 2 months, and as clinically indicated.

Other Comments

Administration Advice:

-Instruct patients to take their doses at approximately the same times every day with or without food.

-Advise patients to swallow the drug tablets whole and not to chew, crush, or split them before swallowing.

-Instruct patients not to ingest drug tablets if they are broken, cracked, or otherwise not intact.

-In the event of a vomited or missed dose, direct patients to skip that dose and to take the next dose at the usual time.

Storage Requirements:

-Store at 20 to 25 degrees Celsius (68 to 77 degrees Fahrenheit); excursions permitted to 15 to 30 degrees Celsius (59 to 86 degrees Fahrenheit).

General:

-There is no known antidote for this drug; use general supportive measures to treat overdose.

Monitoring:

-Cardiovascular: Signs/symptoms of venous thrombosis and pulmonary embolism (during treatment)

-Hematologic: CBC (prior to initiation of this drug, every 2 weeks for the first 2 months, monthly for the next 2 months, and as clinically indicated)

-Hepatic: ALT, AST, and serum bilirubin (prior to initiation of this drug, every 2 weeks for the first 2 months, monthly for the next 2 months, and as clinically indicated)

Patient Advice:

-Avoid eating and drinking grapefruit products while taking this drug.

-This drug may cause side effects such as dizziness; avoid potentially dangerous activities such as driving and operating machinery until you know how this drug affects you.

What is the dose of Abemaciclib for a child?

The dosage has not been established in pediatric patients. It may be unsafe for your child. It is always important to fully understand the safety of the drug before using. Please consult with your doctor or pharmacist for more information.

How is Abemaciclib available?

Abemaciclib is available in the following dosage forms and strengths:

  • Oral tablet.

What should I do in case of an emergency or overdose?

In case of an emergency or an overdose, call your local emergency services or go to your nearest emergency room.

What should I do if I miss a dose?

If you miss a dose of Abemaciclib, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and take your regular dose as scheduled. Do not take a double dose.

Hello Health Group does not provide medical advice, diagnosis or treatment.

Sources

Review Date: August 16, 2018 | Last Modified: August 16, 2018

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