CRIZALK 250MG

Description

Crizalk 250mg belongs to type of tyrosine kinase inhibitor.

A kinase is an enzyme which help to cell growth. There are many types of kinases, which regulates different phases of cell growth. By stopping an enzyme from working, this medication can reduce the growth of cancer cells.

Crizalk 250mg is a prescription drug which is used under supervision of medical oncologist.

Indication

Crizalk 250mg is used for treatment in patients who suffering from locally advanced or metastatic non-small cell lung cancer (NSCLC) which is anaplastic lymphoma kinase-positive as detected by an FDA-approved test

Crizalk 250mg is also used for metastatic NSCLC tumors that are ROS1-positive

Mechanism of action

Crizotinib is an inhibitor of various receptor tyrosine kinases, consist of ALK and ROS1. It only works in cancer cells which have an overactive version of ALK or ROS1.

If NSCLC with genetic defects(rearrangements) in the ALK gene, a formation of ALK fusion proteins results in abnormal activation and signaling. This, in turn, supports the replication and survival of tumors which express these fusion proteins.

Crizotinib belongs to a potent inhibitor of ALK phosphorylation and signal transduction. This prevention was observed in preclinical and clinical studies to be analogue with cell cycle arrest and the initiation of programmed cell death in ALK-positive cancer cells.

ADME Properties

Peak plasma concentration is 4 to 6 hours and bioavailability were 43%.

Volume of distribution is 1772L and plasma protein bounding is 91%

Crizalk metabolised by CYP3A4 and CYP3A5

Crizalk is excreted via feces 63% and 22% via urine and half -life is 42 hours

Dosage and administration

Some patients are selected for the treatment with Crizalk based on ALK or ROS1 presences in tumor specimens

The prescribed dosage of Crizalk is 250mg orally twice in a day

Administer the Crizalk dose with or without food, until disease progression

The capsule Crizalk should be swallowed whole.

Crizalk should not break, open, or chew the capsule.

Dosage modification

Crizalk 200 mg taken orally twice daily for First dose reduction

Crizalk 250 mg taken orally once daily for Second dose reduction

Permanently discontinue if unable to tolerate Crizalk 250 mg taken orally once daily.

Side effects

• Bradycardia
• Feeling sick
• Swelling of hands and feet’s
• Decreased appetite
• Fatigue
• Infection increased
• Breathlessness
• Eyesight changes
• Bowel changes
• Liver changes
• Skin rash

Drug interaction

Interaction of Crizalk 250mg with strong or moderate CYP3A4 inhibitors will raise plasma concentration of Crizalk

Crizalk 250mg concomitant use with strong CYP3A inducers will reduces Crizalk plasma concentration

Crizalk 250mg Co administration with CYP3A substrates will increase plasma concentration of CYP3A substrates

Do not use combination with bradycardia causing drugs

Contraindication

None

Precautions

Before using Crizalk 250mg in some condition, consult with doctor.

When administrating Hepatotoxicity resulted, increase in ALT and total bilirubin resulted, regulate q2wk for 2 months, then monthly

Interstitial lung disease/pneumonitis is reported while using the drug

QT interval prolongation resulted, do not use congenital long QT syndrome.

Symptomatic bradycardia resulted, involving syncope; do not use coadministration with other drugs known to cause bradycardia; monitor heart rate and blood pressure regularly

Severe visual loss is reported

Embryo-fetal toxicity will occur while administrating to pregnant women

Pregnancy

Based on studies of animal and mechanism of action, Crizalk 250mg will cause fetal harm when given to pregnant women

Advice the female not to become pregnant while on treatment with Crizalk 250mg

Lactation

During treatment with Crizalk 250mg, advise the women not to breastfed to infants

Storage

Stored at 20⁰C – 25⁰C

Missed dose

If the patient vomits after taking a dose of Crizalk 250mg or missed to take a dose, then should not to take an extra dose, but to take the next dose at the regular time, skip the missed dose.