Ceritinib
Generic Name: ceritinib
Brand Names:
Zykadia
11 DESCRIPTION Ceritinib is a kinase inhibitor for oral administration. The molecular formula for ceritinib is C 28 H 36 N 5 O 3 ClS. The molecular weight is 558.14 g/mol. Ceritinib is described chemically as 5-Chloro-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-N2-[5-methyl-2-(1-methylethoxy)-4-(4-piperidinyl)phenyl]-2,4-pyrimidinediamine. The chemical structure of ceritinib is shown below: Ceritinib is a white to almost white or light yellow powder.
Overview
11 DESCRIPTION Ceritinib is a kinase inhibitor for oral administration. The molecular formula for ceritinib is C 28 H 36 N 5 O 3 ClS. The molecular weight is 558.14 g/mol. Ceritinib is described chemically as 5-Chloro-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-N2-[5-methyl-2-(1-methylethoxy)-4-(4-piperidinyl)phenyl]-2,4-pyrimidinediamine. The chemical structure of ceritinib is shown below: Ceritinib is a white to almost white or light yellow powder.
Uses
1 INDICATIONS AND USAGE ZYKADIA ® is indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test [see Dosage and Administration (2.1)] . ZYKADIA is a kinase inhibitor indicated for the treatment of adults with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. ( 1 , 2.1 )
Dosage
2 DOSAGE AND ADMINISTRATION Recommended Dosage: 450 mg orally once daily with food. ( 2.2 ) 2.1 Patient Selection Select patients for treatment of metastatic NSCLC with ZYKADIA based on the presence of ALK positivity in tumor specimens [see Clinical Studies (14.1)] . Information on FDA-approved tests for the detection of ALK rearrangements in NSCLC is available at: http://www.fda.gov/CompanionDiagnostics. 2. 2 Recommended Dosage The recommended dosage of ZYKADIA is 450 mg orally once daily with food until disease progression or unacceptable toxicity [see Clinical Pharmacology (12.3)] . If a dose of ZYKADIA is missed, make up that dose unless the next dose is due within 12 hours.
Side Effects
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Gastrointestinal Adverse Reactions [see Warnings and Precautions (5.1)] Hepatotoxicity [see Warnings and Precautions (5.2)] Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions (5.3)] QT Interval Prolongation [see Warnings and Precautions (5.4)] Hyperglycemia [see Warnings and Precautions (5.5)] Bradycardia [see Warnings and Precautions (5.6)] Pancreatitis [see Warnings and Precautions (5.7)] The most common adverse reactions (incidence of ≥ 25%) in patients treated with ZYKADIA 450 mg with food are diarrhea, nausea, abdominal pain, vomiting, and fatigue; and with ZYKADIA 750 mg under fasted conditions are diarrhea, nausea, vomiting, fatigue, abdominal pain, de...
Interactions
7 DRUG INTERACTIONS CYP3A Inhibitors and Inducers : Avoid concurrent use of ZYKADIA with strong CYP3A inhibitors or inducers. If concurrent use of a strong CYP3A inhibitor is unavoidable, dose reduce ZYKADIA. ( 2.4 , 7.1 ) CYP3A Substrates : Avoid coadministration of ZYKADIA with sensitive CYP3A substrates. ( 7.2 ) CYP2C9 Substrates : Avoid coadministration of ZYKADIA with CYP2C9 substrates for which minimal concentration changes may lead to serious toxicities. ( 7.2 ) 7.1 Effect of Other Drugs on ZYKADIA Strong CYP3A Inhibitors A strong CYP3A4/P-gp inhibitor (ketoconazole) increased the systemic exposure of ceritinib [see Clinical Pharmacology (12.3)] , which may increase the incidence and severity of adverse reactions of ZYKADIA.
Warnings
5 WARNINGS AND PRECAUTIONS Gastrointestinal Adverse Reactions : ZYKADIA can cause gastrointestinal adverse reactions. If severe or intolerable, withhold if not responsive to antiemetics or antidiarrheals; upon improvement, resume ZYKADIA at a reduced dose. ( 2.3 , 5.1 ) Hepatotoxicity : ZYKADIA can cause hepatotoxicity. Monitor liver laboratory tests at least monthly. Withhold then dose reduce, or permanently discontinue ZYKADIA. ( 2.3 , 5.2 ) Interstitial Lung Disease/Pneumonitis : Occurred in 2.4% of patients. Permanently discontinue ZYKADIA in patients diagnosed with treatment-related interstitial lung disease (ILD)/pneumonitis. ( 2.3 , 5.3 ) QT Interval Prolongation : ZYKADIA can cause QTc interval prolongation. 4 CONTRAINDICATIONS None. None. ( 4 )
Pregnancy
8.1 Pregnancy Risk Summary Based on animal studies and its mechanism of action [see Clinical Pharmacology (12.1)] , ZYKADIA can cause fetal harm when administered to a pregnant woman. The limited available data on the use of ZYKADIA in pregnant women are insufficient to inform a risk. Administration of ceritinib to rats and rabbits during the period of organogenesis at maternal plasma exposures below the recommended human dose caused increases in skeletal anomalies in rats and rabbits ( see Data ). Advise a pregnant woman of the potential risk to a fetus. In the U.S.
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING ZYKADIA 150 mg capsules Hard gelatin capsule with opaque blue cap and opaque white body; opaque blue cap marked in black ink with “LDK 150MG”, opaque white body marked in black ink with “NVR”.
Frequently Asked Questions
What is Ceritinib used for?▼
1 INDICATIONS AND USAGE ZYKADIA ® is indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test [see Dosage and Administration (2.1)] . ZYKADIA is a kinase inhibitor indicated for the treatment of adults with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. ( 1 , 2.1 )
What are the side effects of Ceritinib?▼
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Gastrointestinal Adverse Reactions [see Warnings and Precautions (5.1)] Hepatotoxicity [see Warnings and Precautions (5.2)] Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions (5.3)] QT Interval Prolongation [see Warnings and Precautions (5.4)] Hyperglycemia [see Warnings and Precautions (5.5)] Bradycardia [see Warnings and Precautions (5.6)] Pancreatitis [see Warnings and Precautions (5.7)] The most common adverse reactions (incidence of ≥ 25%) in patients treated with ZYKADIA 450 mg with food are diarrhea, nausea, abdominal pain, vomiting, and fatigue; and with ZYKADIA 750 mg under fasted conditions are diarrhea, nausea, vomiting, fatigue, abdominal pain, de...
Can I take Ceritinib during pregnancy?▼
8.1 Pregnancy Risk Summary Based on animal studies and its mechanism of action [see Clinical Pharmacology (12.1)] , ZYKADIA can cause fetal harm when administered to a pregnant woman. The limited available data on the use of ZYKADIA in pregnant women are insufficient to inform a risk. Administration of ceritinib to rats and rabbits during the period of organogenesis at maternal plasma exposures below the recommended human dose caused increases in skeletal anomalies in rats and rabbits ( see Data ). Advise a pregnant woman of the potential risk to a fetus. In the U.S.
What are the important warnings for Ceritinib?▼
5 WARNINGS AND PRECAUTIONS Gastrointestinal Adverse Reactions : ZYKADIA can cause gastrointestinal adverse reactions. If severe or intolerable, withhold if not responsive to antiemetics or antidiarrheals; upon improvement, resume ZYKADIA at a reduced dose. ( 2.3 , 5.1 ) Hepatotoxicity : ZYKADIA can cause hepatotoxicity. Monitor liver laboratory tests at least monthly. Withhold then dose reduce, or permanently discontinue ZYKADIA. ( 2.3 , 5.2 ) Interstitial Lung Disease/Pneumonitis : Occurred in 2.4% of patients. Permanently discontinue ZYKADIA in patients diagnosed with treatment-related interstitial lung disease (ILD)/pneumonitis. ( 2.3 , 5.3 ) QT Interval Prolongation : ZYKADIA can cause QTc interval prolongation. 4 CONTRAINDICATIONS None. None. ( 4 )
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.