Ceritinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Ceritinib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2014. Its mechanism of action is classified as Cytochrome P450 2C9 Inhibitors, Cytochrome P450 3A Inhibitors and Tyrosine Kinase Inhibitors. DrugCentral lists 47 molecular targets, including ALK, INSR and IGF1R. Recorded indications include ALK fusion gene-positive non-small-cell lung cancer and Non-small cell lung cancer.

• Approval status: onp (first approved 2014 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Cytochrome P450 2C9 Inhibitors; Cytochrome P450 3A Inhibitors; Tyrosine Kinase Inhibitors.
• Molecular targets: ALK, INSR, IGF1R and TSSK1B (47 listed in DrugCentral).
• Indications: ALK fusion gene-positive non-small-cell lung cancer and Non-small cell lung cancer.
• ATC code: L01ED02 (Anaplastic lymphoma kinase (ALK) inhibitors).
• Molecular formula: C28H36ClN5O3S; molecular weight 558.15 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• ALK fusion gene-positive non-small-cell lung cancer
• Non-small cell lung cancer

Mechanism & targets

• Mechanism of action (MoA): Cytochrome P450 2C9 Inhibitors; Cytochrome P450 3A Inhibitors; Tyrosine Kinase Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (47)

Target	Gene	Action	Activity
ALK tyrosine kinase receptor	ALK	inhibitor	IC50 9.70
Insulin receptor	INSR	agonist	IC50 8.15
Insulin-like growth factor 1 receptor	IGF1R	unknown	IC50 8.10
Testis-specific serine/threonine-protein kinase 1	TSSK1B	unknown	IC50 7.64
Non-receptor tyrosine-protein kinase TNK1	TNK1	unknown	Kd 7.57
Receptor-type tyrosine-protein kinase FLT3	FLT3	unknown	IC50 7.22
Multidrug resistance protein 1	ABCB1	unknown	EC50 7.05
Proto-oncogene tyrosine-protein kinase ROS	ROS1	unknown	IC50 6.85
Tyrosine-protein kinase Fer	FER	unknown	Kd 6.67
Focal adhesion kinase 1	PTK2	unknown	Kd 6.66
Fibroblast growth factor receptor 2	FGFR2	unknown	IC50 6.59
Proto-oncogene tyrosine-protein kinase receptor Ret	RET	unknown	IC50 6.40
Fibroblast growth factor receptor 3	FGFR3	unknown	IC50 6.37
Tyrosine-protein kinase Lck	LCK	unknown	IC50 6.25
Tyrosine-protein kinase JAK2	JAK2	unknown	IC50 6.21
Calcium/calmodulin-dependent protein kinase type IV	CAMK4	unknown	Kd 6.20
Tyrosine-protein kinase Lyn	LYN	unknown	IC50 6.08
Epidermal growth factor receptor	EGFR	unknown	IC50 6.05
Activated CDC42 kinase 1	TNK2	unknown	Kd 6.03
Fibroblast growth factor receptor 4	FGFR4	unknown	IC50 6.02

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2016-03-28	PMDA	—	NOVARTIS PHARMA K.K.
2015-02-26	EMA	—	—
2014-04-29	FDA	—	NOVARTIS PHARMS CORP

ATC classification

ATC code	Therapeutic hierarchy
L01ED02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Anaplastic lymphoma kinase (ALK) inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: ALK · Testing Required
• FDA label: ALK · Testing Required
• HCSC label: ALK · Testing Required

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Malignant neoplasm progression	933.6
Metastases to central nervous system	483.4
Diarrhoea	231.1
Nausea	176.5
Death	137.1
Vomiting	127.5
Metastases to liver	91.5
Neoplasm progression	77.0
Pericardial effusion	76.5
Neoplasm	76.3
Alanine aminotransferase increased	71.6
Disease progression	70.8

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Ceritinib is on its molecule page.

• Molecular formula: C₂₈H₃₆ClN₅O₃S
• Molecular weight: 558.15 g/mol
• CAS number: —
• InChIKey: VERWOWGGCGHDQE-UHFFFAOYSA-N
• PubChem CID: 57379345

CC(C)OC1=C(NC2=NC=C(Cl)C(NC3=C(C=CC=C3)S(=O)(=O)C(C)C)=N2)C=C(C)C(=C1)C1CCNCC1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Ceritinib used for?

DrugCentral lists the following indications for Ceritinib: ALK fusion gene-positive non-small-cell lung cancer and Non-small cell lung cancer.

How does Ceritinib work?

Ceritinib is classified as Cytochrome P450 2C9 Inhibitors, Cytochrome P450 3A Inhibitors and Tyrosine Kinase Inhibitors; its molecular targets in DrugCentral include ALK (inhibitor), INSR (agonist), IGF1R and TSSK1B.

When was Ceritinib first approved?

Ceritinib was first approved by the FDA in 2014.

What drug class does Ceritinib belong to?

Ceritinib is in the Kinase Inhibitor class.

What is the chemical formula of Ceritinib?

Ceritinib has the molecular formula C28H36ClN5O3S and a molecular weight of 558.15 g/mol.

Sources

• DrugCentral drug card 4866 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2403108 — compound record and bioactivity
• PubChem CID 57379345 — chemical identifiers
• DrugBank DB09063 — drug record
• FDA UNII K418KG2GET — substance identity
• DailyMed: FDA labels for Ceritinib — current prescribing information (label search)
• UniProt Q9UM73 (ALK) — target protein
• UniProt P06213 (INSR) — target protein
• UniProt P08069 (IGF1R) — target protein
• UniProt Q9BXA7 (TSSK1B) — target protein
• UniProt Q13470 (TNK1) — target protein
• UniProt P36888 (FLT3) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.