KISQALI FEMARA CO-PACK

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Overview

What is KISQALI FEMARA CO-PACK?

KISQALI FEMARA CO-PACK consists of ribociclib 200 mg film coated tablets copackaged with letrozole 2.5 mg tablets.

Ribociclib:

KISQALI (ribociclib) is a kinase inhibitor.

Ribociclib succinate is a light yellow to yellowish brown crystalline powder. The chemical name of ribociclib succinate is: Butanedioic acid—7-cyclopentyl-,-dimethyl-2-{[5-(piperazin-1-yl) pyridin-2-yl]amino}-7-pyrrolo[2,3-]pyrimidine-6-carboxamide (1/1).

The molecular formula for ribociclib succinate is CHNO.CHOand the molecular weight is 552.64 g/mole .

The chemical structure of ribociclib is shown below:

KISQALI film-coated tablets are supplied for oral use and contain 200 mg of ribociclib free base (equivalent to 254.40 mg ribociclib succinate). The tablets also contain colloidal silicon dioxide, crospovidone, hydroxypropylcellulose, magnesium stearate and microcrystalline cellulose. The film-coating contains iron oxide black, iron oxide red, lecithin (soya), polyvinyl alcohol (partially hydrolyzed), talc, titanium dioxide, and xanthan gum as inactive ingredients.

Letrozole:

FEMARA (letrozole) is a nonsteroidal aromatase inhibitor (inhibitor of estrogen synthesis).

Letrozole is a white to yellowish crystalline powder, practically odorless, freely soluble in dichloromethane, slightly soluble in ethanol, and practically insoluble in water. It has a molecular weight of 285.31, empirical formula CHN, and a melting range of 184°C to 185°C.

The chemical name of letrozole is 4,4'-(1H-1,2,4-Triazol-1ylmethylene)dibenzonitrile, and its structural formula is

FEMARA is available as 2.5 mg tablets for oral administration.

Inactive Ingredients: Colloidal silicon dioxide, ferric oxide, hydroxypropyl methylcellulose, lactose monohydrate, magnesium stearate, maize starch, microcrystalline cellulose, polyethylene glycol, sodium starch glycolate, talc, and titanium dioxide.

What does KISQALI FEMARA CO-PACK look like?

What are the available doses of KISQALI FEMARA CO-PACK?

Tablets:

What should I talk to my health care provider before I take KISQALI FEMARA CO-PACK?

Lactation: Advise not to breastfeed. ()

How should I use KISQALI FEMARA CO-PACK?

The KISQALI FEMARA CO-PACK is indicated as initial endocrine-based therapy for the treatment of postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer.

The KISQALI FEMARA CO-PACK is comprised of ribociclib tablets copackaged with letrozole tablets, to provide a 28-day treatment regimen.

The KISQALI FEMARA CO-PACK should be coadministered, with or without food, as follows:

Patients should take their doses of KISQALI FEMARA CO-PACK at approximately the same time each day, preferably in the morning. If the patient vomits after taking the dose or misses a dose, no additional dose should be taken that day. The next prescribed dose should be taken at the usual time. Tablets should be swallowed whole (tablets should not be chewed, crushed or split prior to swallowing). No tablet should be ingested if it is broken, cracked, or otherwise not intact.

For additional information on KISQALI and FEMARA, refer to the Full Prescribing Information for each product.

What interacts with KISQALI FEMARA CO-PACK?

Sorry No Records found

What are the warnings of KISQALI FEMARA CO-PACK?

Sorry No Records found

What are the precautions of KISQALI FEMARA CO-PACK?

Sorry No Records found

What are the side effects of KISQALI FEMARA CO-PACK?

Sorry No records found

What should I look out for while using KISQALI FEMARA CO-PACK?

None.

What might happen if I take too much KISQALI FEMARA CO-PACK?

There were no known cases of overdose with ribociclib and letrozole in Study 1. General symptomatic and supportive measures should be initiated in all cases of overdose where necessary.

Refer to the Full Prescribing Information of FEMARA for additional overdosage information.

How should I store and handle KISQALI FEMARA CO-PACK?

KISQALI FEMARA CO-PACK is dispensed in a carton for a total of 28 days of therapy.Each carton contains individual ribociclib and letrozole drug products as follows:KISQALI (ribociclib) Tablets:200 mg tablets.Light greyish violet, round, curved with beveled edge, debossed with “RIC” on one side and “NVR” on the other side.FEMARA (letrozole) Tablets:2.5 mg tablets. Dark yellow, round, slightly biconvex, with beveled edges, imprinted with the letters “FV” on one side and “CG” on the other side.KISQALI FEMARA CO-PACK Cartons:Store KISQALI FEMARA CO-PACK at 20°C to 25°C (68°F to 77°F). Store in the original package.KISQALI FEMARA CO-PACK is dispensed in a carton for a total of 28 days of therapy.Each carton contains individual ribociclib and letrozole drug products as follows:KISQALI (ribociclib) Tablets:200 mg tablets.Light greyish violet, round, curved with beveled edge, debossed with “RIC” on one side and “NVR” on the other side.FEMARA (letrozole) Tablets:2.5 mg tablets. Dark yellow, round, slightly biconvex, with beveled edges, imprinted with the letters “FV” on one side and “CG” on the other side.KISQALI FEMARA CO-PACK Cartons:Store KISQALI FEMARA CO-PACK at 20°C to 25°C (68°F to 77°F). Store in the original package.KISQALI FEMARA CO-PACK is dispensed in a carton for a total of 28 days of therapy.Each carton contains individual ribociclib and letrozole drug products as follows:KISQALI (ribociclib) Tablets:200 mg tablets.Light greyish violet, round, curved with beveled edge, debossed with “RIC” on one side and “NVR” on the other side.FEMARA (letrozole) Tablets:2.5 mg tablets. Dark yellow, round, slightly biconvex, with beveled edges, imprinted with the letters “FV” on one side and “CG” on the other side.KISQALI FEMARA CO-PACK Cartons:Store KISQALI FEMARA CO-PACK at 20°C to 25°C (68°F to 77°F). Store in the original package.KISQALI FEMARA CO-PACK is dispensed in a carton for a total of 28 days of therapy.Each carton contains individual ribociclib and letrozole drug products as follows:KISQALI (ribociclib) Tablets:200 mg tablets.Light greyish violet, round, curved with beveled edge, debossed with “RIC” on one side and “NVR” on the other side.FEMARA (letrozole) Tablets:2.5 mg tablets. Dark yellow, round, slightly biconvex, with beveled edges, imprinted with the letters “FV” on one side and “CG” on the other side.KISQALI FEMARA CO-PACK Cartons:Store KISQALI FEMARA CO-PACK at 20°C to 25°C (68°F to 77°F). Store in the original package.KISQALI FEMARA CO-PACK is dispensed in a carton for a total of 28 days of therapy.Each carton contains individual ribociclib and letrozole drug products as follows:KISQALI (ribociclib) Tablets:200 mg tablets.Light greyish violet, round, curved with beveled edge, debossed with “RIC” on one side and “NVR” on the other side.FEMARA (letrozole) Tablets:2.5 mg tablets. Dark yellow, round, slightly biconvex, with beveled edges, imprinted with the letters “FV” on one side and “CG” on the other side.KISQALI FEMARA CO-PACK Cartons:Store KISQALI FEMARA CO-PACK at 20°C to 25°C (68°F to 77°F). Store in the original package.KISQALI FEMARA CO-PACK is dispensed in a carton for a total of 28 days of therapy.Each carton contains individual ribociclib and letrozole drug products as follows:KISQALI (ribociclib) Tablets:200 mg tablets.Light greyish violet, round, curved with beveled edge, debossed with “RIC” on one side and “NVR” on the other side.FEMARA (letrozole) Tablets:2.5 mg tablets. Dark yellow, round, slightly biconvex, with beveled edges, imprinted with the letters “FV” on one side and “CG” on the other side.KISQALI FEMARA CO-PACK Cartons:Store KISQALI FEMARA CO-PACK at 20°C to 25°C (68°F to 77°F). Store in the original package.KISQALI FEMARA CO-PACK is dispensed in a carton for a total of 28 days of therapy.Each carton contains individual ribociclib and letrozole drug products as follows:KISQALI (ribociclib) Tablets:200 mg tablets.Light greyish violet, round, curved with beveled edge, debossed with “RIC” on one side and “NVR” on the other side.FEMARA (letrozole) Tablets:2.5 mg tablets. Dark yellow, round, slightly biconvex, with beveled edges, imprinted with the letters “FV” on one side and “CG” on the other side.KISQALI FEMARA CO-PACK Cartons:Store KISQALI FEMARA CO-PACK at 20°C to 25°C (68°F to 77°F). Store in the original package.KISQALI FEMARA CO-PACK is dispensed in a carton for a total of 28 days of therapy.Each carton contains individual ribociclib and letrozole drug products as follows:KISQALI (ribociclib) Tablets:200 mg tablets.Light greyish violet, round, curved with beveled edge, debossed with “RIC” on one side and “NVR” on the other side.FEMARA (letrozole) Tablets:2.5 mg tablets. Dark yellow, round, slightly biconvex, with beveled edges, imprinted with the letters “FV” on one side and “CG” on the other side.KISQALI FEMARA CO-PACK Cartons:Store KISQALI FEMARA CO-PACK at 20°C to 25°C (68°F to 77°F). Store in the original package.KISQALI FEMARA CO-PACK is dispensed in a carton for a total of 28 days of therapy.Each carton contains individual ribociclib and letrozole drug products as follows:KISQALI (ribociclib) Tablets:200 mg tablets.Light greyish violet, round, curved with beveled edge, debossed with “RIC” on one side and “NVR” on the other side.FEMARA (letrozole) Tablets:2.5 mg tablets. Dark yellow, round, slightly biconvex, with beveled edges, imprinted with the letters “FV” on one side and “CG” on the other side.KISQALI FEMARA CO-PACK Cartons:Store KISQALI FEMARA CO-PACK at 20°C to 25°C (68°F to 77°F). Store in the original package.KISQALI FEMARA CO-PACK is dispensed in a carton for a total of 28 days of therapy.Each carton contains individual ribociclib and letrozole drug products as follows:KISQALI (ribociclib) Tablets:200 mg tablets.Light greyish violet, round, curved with beveled edge, debossed with “RIC” on one side and “NVR” on the other side.FEMARA (letrozole) Tablets:2.5 mg tablets. Dark yellow, round, slightly biconvex, with beveled edges, imprinted with the letters “FV” on one side and “CG” on the other side.KISQALI FEMARA CO-PACK Cartons:Store KISQALI FEMARA CO-PACK at 20°C to 25°C (68°F to 77°F). Store in the original package.

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Clinical Information

Chemical Structure

No Image found

Clinical Pharmacology

Ribociclib is an inhibitor of cyclin-dependent kinase (CDK) 4 and 6. These kinases are activated upon binding to D-cyclins and play a crucial role in signaling pathways which lead to cell cycle progression and cellular proliferation. The cyclin D-CDK4/6 complex regulates cell cycle progression through phosphorylation of the retinoblastoma protein (pRb).

In vitro

In vivo

Letrozole is a nonsteroidal competitive inhibitor of the aromatase enzyme system by competitively binding to the heme of the cytochrome P450 subunit of the enzyme, resulting in a reduction of estrogen biosynthesis in all tissues. In postmenopausal women, estrogens are mainly derived from the action of the aromatase enzyme, which converts adrenal androgens (primarily androstenedione and testosterone) to estrone and estradiol. The suppression of estrogen biosynthesis in peripheral tissues and in the cancer tissue itself can therefore be achieved by specifically inhibiting the aromatase enzyme.

In vivo

Non-Clinical Toxicology

None.

KISQALI has been shown to prolong the QT interval in a concentration-dependent manner, with estimated mean increase in QTc interval exceeding 20 ms (22.9 ms (90% CI: 21.6, 24.1)) at the mean steady-state C following administration at 600 mg once daily dose . In Study 1 (MONALEESA-2), one patient (0.3%) had >500 msec post-baseline QTcF value (average of triplicate), and nine patients out of 329 patients (3%) had a >60 msec increase from baseline in QTcF intervals (average of triplicate). These ECG changes occurred within the first four weeks of treatment and were reversible with dose interruption. There were no reported cases of Torsades de Pointes. Syncope occurred in 9 patients (2.7%) in the KISQALI plus letrozole arm versus 3 (0.9%) in placebo plus letrozole arm. On the KISQALI plus letrozole treatment arm, there was one (0.3%) sudden death in a patient with Grade 3 hypokalemia and Grade 2 QT prolongation .

Assess ECG prior to initiation of treatment. Initiate treatment with KISQALI FEMARA CO-PACK only in patients with QTcF values less than 450 msec. Repeat ECG at approximately Day 14 of the first cycle and the beginning of the second cycle, and as clinically indicated.

Monitor serum electrolytes (including potassium, calcium, phosphorous and magnesium) prior to the initiation of treatment, at the beginning of the first 6 cycles, and as clinically indicated. Correct any abnormality before starting KISQALI FEMARA CO-PACK therapy

Avoid the use of KISQALI FEMARA CO-PACK in patients who already have or who are at significant risk of developing QTc prolongation, including patients with:

Avoid using KISQALI FEMARA CO-PACK with drugs known to prolong QTc interval and/or strong CYP3A inhibitors as this may lead to prolongation of the QTcF interval .

Based on the observed QT prolongation during treatment, KISQALI may require dose interruption, reduction or discontinuation as described in Table 4

The following adverse reactions are discussed in greater detail in other sections of the labeling:

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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