Palbociclib

What is Palbociclib?

• Palbociclib (Ibrance) is a kinase inhibitor used to treat hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative breast cancer.

What are the uses of this medicine?

This medicine is used to treat:

• hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative breast cancer that has spread to other parts of the body (metastatic) in combination with:
• letrozole as the first hormonal based therapy in women who have gone through menopause, or
• fulvestrant in women with disease progression following hormonal therapy.

How does this medicine work?

• Palbociclib (pal" boe sye' klib) is an orally available, specific inhibitor of cyclin-dependent kinases that is used in combination with aromatase inhibitors in the therapy of postmenopausal women with metastatic breast cancer that is positive for the estrogen receptor (ER+), but negative for human epidermal growth factor receptor 2 (HER2-).
• The cyclin kinases 4 and 6 regulate the cellular transition from the G1 to the S phase of the cell cycle.
• Inhibition of this transition blocks the progression of the cell cycle and results in growth arrest in rapidly dividing cells.
• The addition of palbociclib to letrozole or fulvestrant (aromatase inhibitors) therapy of metastatic breast cancer (ER+, HER2-) in postmenopausal women was associated with a prolongation of disease free survival.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Avoid concomitant use of strong CYP3A inhibitors (e.g., clarithromycin, indinavir, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, posaconazole, ritonavir, saquinavir, telaprevir, telithromycin, and voriconazole). Avoid grapefruit or grapefruit juice during Ibrance treatment. If coadministration of Ibrance with a strong CYP3A inhibitor cannot be avoided, reduce the dose of Ibrance.
• Avoid concomitant use of strong CYP3A inducers (e.g., phenytoin, rifampin, carbamazepine, enzalutamide, and St John's Wort).
• The dose of the sensitive CYP3A substrate with a narrow therapeutic index (e.g., alfentanil, cyclosporine, dihydroergotamine, ergotamine, everolimus, fentanyl, pimozide, quinidine, sirolimus and tacrolimus) may need to be reduced as Ibrance may increase their exposure.

Is this medicine FDA approved?

• It was approved for use in the United States in 2015.

How should this medicine be used?

Recommended Dosage:

• The recommended dose of Ibrance is a 125 mg capsule taken orally once daily for 21 consecutive days followed by 7 days off treatment to comprise a complete cycle of 28 days.
• When coadministered with palbociclib, the recommended dose of letrozole is 2.5 mg taken once daily continuously throughout the 28-day cycle.
• When coadministered with palbociclib, the recommended dose of fulvestrant is 500 mg administered on Days 1, 15, 29, and once monthly thereafter.
• If patients must be coadministered a strong CYP3A inhibitor, reduce the Ibrance dose to 75 mg once daily.

Administration

• Take Ibrance exactly as your healthcare provider tells you.
• Take Ibrance with food.
• Swallow Ibrance capsules whole. Do not chew, crush or open Ibrance capsules before swallowing them.
• Do not take any Ibrance capsules that are broken, cracked, or that look damaged.
• Avoid grapefruit and grapefruit products during treatment with Ibrance. Grapefruit may increase the amount of Ibrance in your blood.
• Do not change your dose or stop taking Ibrance unless your healthcare provider tells you.
• If you miss a dose of Ibrance or vomit after taking a dose of Ibrance, do not take another dose on that day. Take your next dose at your regular time.
• If you take too much Ibrance, call your healthcare provider right away or go to the nearest hospital emergency room.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Capsules: 125 mg, 100 mg, and 75 mg

This medicine is available in fallowing brand namesː

• Ibrance

What side effects can this medication cause?

The most common side effects of this medicine include:

• neutropenia
• leukopenia
• infections
• fatigue
• nausea
• anemia
• stomatitis
• headache
• diarrhea
• thrombocytopenia
• constipation
• alopecia
• vomiting
• rash
• decreased appetite

Ibrance may cause serious side effects, including:

• Low white blood cell counts (neutropenia)
• Blood clots in the arteries of your lungs (pulmonary embolism or PE)

What special precautions should I follow?

• Neutropenia may occur. Monitor complete blood count prior to start of Ibrance therapy and at the beginning of each cycle, as well as on Day 14 of the first 2 cycles, and as clinically indicated.
• Pulmonary embolism has been reported at a higher rate in patients treated with Ibrance plus letrozole. Monitor patients for signs and symptoms of pulmonary embolism and treat as medically appropriate.
• Ibrance Can cause fetal harm. Advise patients of potential risk to a fetus and to use effective contraception.

What to do in case of emergency/overdose?

Management for overdosage:

• There is no known antidote for Ibrance.
• The treatment of overdose of Ibrance should consist of general supportive measures.

Can this medicine be used in pregnancy?

• Ibrance can cause fetal harm when administered to a pregnant woman .
• There are no available data in pregnant women to inform the drug-associated risk.

Can this medicine be used in children?

• The safety and efficacy of Ibrance in pediatric patients have not been studied.

What are the active and inactive ingredients in this medicine?

• Active ingredient: palbociclib
• Inactive ingredients: Microcrystalline cellulose, lactose monohydrate, sodium starch glycolate, colloidal silicon dioxide, magnesium stearate, and hard gelatin capsule shells.

Who manufactures and distributes this medicine?

• Packager: U.S. Pharmaceuticals

What should I know about storage and disposal of this medication?

• Store Ibrance at 68 °F to 77 °F (20 °C to 25 °C).
• Keep Ibrance and all medicines out of the reach of children.

• Dailymed label info on Palbociclib
• FDA Palbociclib

Palbociclib Resources
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