Kisqali 200mg


Description


Ribociclib is a generic form of brand name Kisqali 200mg which belongs to selective cyclin-dependent kinase inhibitor, a class of drugs which help slow the progression of cancer by inhibiting two proteins called cyclin-dependent kinase 4 and 6 (CDK4/6). Kisqali 200mg is a prescription drug which is used under the supervision of medical practioners


Indication


Kisqali 200mg is used in combination with letrozole which an aromatase inhibitor for the treatment for women with breast cancer


Dosage


The recommended dose of Kisqali is 600mg (three 200mg film coated tablets) administrated orally once daily for 21 consecutive days followed by 7 days off therapy resulting in a complete cycle of 28 days.
The drug Kisqali can be administrated with or without food.
Overdose: overdose with Kisqali in human has experienced very limited. In case occurs provide general symptomatic and supportive measures.







Mechanism Of Action


Prevents cyclin dependent kinases (CDK) 4 and 6; stop cellular multiplication of G1 into S phase of the cell cycle
These kinases are activated upon bounding to D cyclins and play a critical role in indicating pathways which causes cell cycle progression and cellular replication; the cyclin D-CDK4/6 complex manage cell cycle progression through phosphorylation of the retinoblastoma protein (pRb).

ADME


Time to high plasma concentration is 1-4 hr and steady state achieved is 8 days
Human plasma protein bound is 70%
Mainly metabolised by hepatic through CYP3A4 in humans
Kisqali is eliminated through feces 69% and urine 23%
Half -life is 32.6 hours

Precautions


In patients with advanced or metastatic breast cancer will increases in transaminases were resulted; perform liver function test before starting treatment with Kisqali; based on severity of the transaminase elevations, Kisqali may require dose interference, reduction or stopping.
Kisqali has been exposed to prolong the QT interval in a concentration-dependent manner. Based on the observed QT prolongation during therapy, Kisqali may needed dose interruption, reduction, or discontinuation.
Do not use combination with tamoxifen due to increased QT prolongation.

Drug interaction


Kisqali 200mg concomitant use with strong CYP3A4 inhibitor will increased Ribociclib exposure in healthy subjects but this combination cannot be avoided, so reduce the dose of Kisqali to 400mg once daily
Kisqali 200mg interaction with strong CYP3A4 inducers will decreased Ribociclib exposure in healthy subjects by 89% Interaction of midazolam with multiple doses of Kisqali will increased the midazolam exposure by 3.8-fold in healthy subjects.

Pregnancy


There are no data available with the use of Kisqali 200mg in pregnant women to inform drug-associated risks. Hence avoid becoming pregnancy during Jakavi 5mg treatment.

Side Effects


Increased liver enzymes, Fatigue , Diarrhea, Hair loss, Decreased kidney function, Lack of appetite, Rash, Fever, Decreased in blood counts, Nausea and vomiting, Itching, Insomnia, Urinary tract infection.

Missed Dose


If dose is missed the have the dose immediately before next dose timing reaches or skip the missed dose and continue the regular schedule.
Consult doctors regarding missed dose.



Lactation


Do not breast feed during treatment with Kisqali 200mg. Excretion into human milk is unknown.


Storage


The drug Kisqali is store at 200C to 250C.


Contraindication


None.


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