[Crizotinib instructions]_ efficacy _ effect
Crizotinib is a western medicine that was only marketed in 2011. It is mainly suitable for ALK-positive metastatic non-small cell lung cancer and ROS-1 positive non-small cell lung cancer.
Although many people don’t understand it, the symptoms that apply to it are tumor-specific drugs.
It is an oral capsule with two dosages, both circulating on the surface of a city in the United States, and the price is relatively high because of its good therapeutic effect.
[Drug Name]Xalkori[Brand Name]Crizotinib (Crozotinib)[Time to Market in the US]?
ROS-1 positive non-small cell lung cancer;
Patients with locally advanced advanced anaplastic lymphoma kinase (ALK) positive as determined by approved testing methods;
Time to market: 2011[Category]Tyrosinase inhibitor[Target]ALK[Molecular structure]Molecular formula: C21H22Cl2FN5O Chemical name: (R) -3-[1- (2,6-Dichloro-3-fluorophenyl) ethoxy]-5-[1- (piperidin-4-yl) -1H-pyrazol-4-yl]pyridin-2-amine has the structural formula:?
The molecular weight is 450.
Pfizer[Place of purchase]United States[Dosage form and specifications]Oral capsules in dosages of 250 mg and 200 mg.
250mg capsule: hard gelatin capsule, size 0, pink opaque cap and body, with “Pfizer” on the cap and “CRZ on the body”?
, 60 Capsule Bottle: NDC?
200mg capsules: Hard gelatin capsules, size 1, white opaque body and pink opaque cap with “Pfizer” on the cap and “CRZ on the body”?
200 “, 60 Capsule Bottle: NDC?
[Essential]crizotinib hard shell contains 250?
Mg or 200?
mg of crizotinini colloidal silica, microcrystalline cellulose, anhydrous calcium hydrogen phosphate, sodium starch glycolate, magnesium stearate and hard capsule shells are inactive ingredients.
The pink opaque capsule shell component contains gelatin, titanium dioxide, and iron oxide red.
The white opaque capsule shell component contains gelatin and titanium dioxide.
Printing inks contain shellac, propylene glycol, strong ammonia solution, potassium hydroxide, and black iron oxide.
[Mechanism of action]Crizotinib is a tyrosine kinase receptor including ALK, hepatocyte growth factor receptor (HGFR,?
c-Met), an inhibitor of ROS1 (c-ros), and tyrosine kinase (RON).
Translocation can affect the expression of oncogenic fusion proteins by ALK genes.
The formation of ALK fusion proteins leads to abnormal regulation of activation and gene expression and an increase in cell proliferation, which contributes to the signal, and surviving tumors express these proteins.
Crizotinib is responsible for the stabilization or regression of tumors by preventing a variety of cellular pathways that are critical for tumor cell growth and survival.
[Indications and uses]?
Crizotinib is a kinase inhibitor suitable for the treatment of patients with: (1)?
ALK-positive metastatic non-small cell lung cancer?
? Crizotinib is a kinase inhibitor for the treatment of patients with advanced or metastatic non-small cell lung cancer (NSCLC) who have been positive for anaplastic lymphoma kinase (ALK) by an FDA-approved test.
(2) ROS-1 positive non-small cell lung cancer XALKOR is suitable for the treatment of patients with metastatic NSCLC whose tumors are ROS1-positive.
[Usage and Dosage]Patient selection: Non-small cell lung cancer patients with ALK positive or ROS-1 positive tumor test results can be treated with crizotinib.
The current FDA-approved detection method for non-small cell lung cancer for detecting ROS1 rearrangement is not available. You can refer to identifying patients with non-small cell lung cancer with ROS1 rearrangement in clinical studies.
Recommended Dosage: The recommended oral dose of crizotinib is 250 mg twice daily until disease progression or patient intolerance.
In severe kidney damage?
[Creatinine clearance (CLcr)?
<30? mL / min]and does not require dialysis patients, the recommended oral dose of crizotinib is 250? mg once daily. ? ? Crizotinib can be taken with or without food. Swallow the capsules whole. If a dose of crizotinib is missing, make up the dose (if the next dose is within 6 hours, there is no need to make up). If vomiting occurs after taking one dose of crizotinib, take the next dose at the regular time. Dose adjustment: Adjust the dose according to personal safety and tolerability (CTCAE) version 4. 0 definition), need to reduce 1 dose or more: (1) the first dose reduction: 200mg capsules taken orally 2 times a day; (2) the second dose reduction: 250mg capsules taken once a day;(3) If crizotinib 250 mg cannot be taken orally once a day, the administration is permanently discontinued. [Storage]Store at room temperature 20o to 25oC (68o to 77oF); allow to go out temperature range is 15o-30oC (59o to 86oF). [Contraindications]None. [Warnings and Precautions](1) Hepatotoxicity: 0 after taking crizotinib Symptoms of liver toxicity occur in 1% of patients. Patients need to have regular liver function tests and adjust their medication according to the actual situation: pause, adjust the dose, or terminate the medication. (2) Interstitial lung disease (ILD) / pneumonia: 2. 9% of patients develop interstitial lung disease (ILD) / pneumonia symptoms. Dosage is permanently discontinued in patients with interstitial lung disease (ILD) / pneumonia. (3) Prolonged QT interval: 2 after taking crizotinib. 1% of patients developed symptoms of prolonged QT. Electrocardiogram and electrolyte monitoring should be performed on patients who previously had QT interval prolongation or have a tendency to QT interval prolongation, as well as patients who have taken QT interval prolongation. Adjust the medication according to the actual situation of the patient: pause the supplement, adjust the dose or terminate the replacement. (4) bradycardia: crizotinib can cause bradycardia. Patients need regular heart rate and blood pressure checks. Adjust the medication according to the actual situation of the patient: pause the supplement, adjust the dose or terminate the replacement. (5) Severe visual impairment: 0 after taking crizotinib. 2% of patients reported severe visual impairment. Crizotinib was discontinued in patients with severe visual impairment and an ophthalmological evaluation was performed. (6) Caused by-Vitamin Toxicity: There may be toxic toxicity after taking crizotinib. Advise women of reproductive potential that they need effective contraception. [Adverse reactions]The drug's adverse reactions include liver toxicity, interstitial lung disease, prolonged QT interval, bradycardia, and severe visual impairment. ? Common adverse reactions (≥25%) are: visual impairment, nausea, diarrhea, vomiting, edema, constipation, elevated transaminase, fatigue, decreased appetite, upper respiratory infections, dizziness, and mental illness. ?Note: Adverse reactions to the drug are described in detail in the[Warnings and Precautions]section of the instructions. [Use in special populations](1) Medication during pregnancy: May cause harm when administered to crizotinib in pregnant women. Advise crizotinib for potential harm. (2) Medication during breastfeeding: Because of the potential for adverse reactions in breastfed infants, do not replace breastfeeding during crizotinib treatment or 45 days after the last completion. (3) Females and males of reproductive potential: When supplementing pregnant women with crizotinib may cause hypertension, advise women with reproductive potential to take effective contraception during crizotinib treatment and for at least 45 days after the final dose; becausePotential for genotoxicity, men who advise female partners with reproductive potential need to take effective contraception during crizotinib treatment and another 90 days after it is completely completed; according to the reproductive organs found in animals, crizotinib is breedingPotential women and men can cause reduced fertility. It is unclear whether the effect on fertility is reversible. (4) Pediatric use: safety and efficacy of crizotinib have not been established in pediatric patients