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ceritinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	4866	1032900-25-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: NVP-LDK378-NX ceritinib zykadia LDK378	Ceritinib is a kinase inhibitor. Targets of ceritinib inhibition identified in either biochemical or cellular assays at clinically relevant concentrations include ALK, insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (InsR), and ROS1. Among these, ceritinib is most active against ALK. Ceritinib inhibited autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and proliferation of ALK-dependent cancer cells in in vitro and in vivo assays. Molecular weight: 558.14 Formula: C28H36ClN5O3S CLOGP: 6.41 LIPINSKI: 2 HAC: 8 HDO: 3 TPSA: 105.24 ALOGS: -5.40 ROTB: 9 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

NVP-LDK378-NX
ceritinib
zykadia
LDK378

Ceritinib is a kinase inhibitor. Targets of ceritinib inhibition identified in either biochemical or cellular assays at clinically relevant concentrations include ALK, insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (InsR), and ROS1. Among these, ceritinib is most active against ALK. Ceritinib inhibited autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and proliferation of ALK-dependent cancer cells in in vitro and in vivo assays.

Molecular weight: 558.14
Formula: C28H36ClN5O3S
CLOGP: 6.41
LIPINSKI: 2
HAC: 8
HDO: 3
TPSA: 105.24
ALOGS: -5.40
ROTB: 9

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.45	g	O

ADMET properties:

None

Approvals:

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Date	Agency	Company
April 29, 2014	FDA	NOVARTIS PHARMS CORP
Feb. 26, 2015	EMA
March 28, 2016	PMDA	NOVARTIS PHARMA K.K.

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FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Malignant neoplasm progression	453.07	35.92	158	2529	81963	63404372
Metastases to central nervous system	265.26	35.92	69	2618	13036	63473299
Diarrhoea	129.70	35.92	154	2533	715212	62771123
Nausea	99.11	35.92	148	2539	854323	62632012
Vomiting	84.02	35.92	110	2577	559507	62926828
Death	69.47	35.92	82	2605	374299	63112036
Neoplasm progression	49.11	35.92	26	2661	36402	63449933
Non-small cell lung cancer	45.01	35.92	13	2674	3582	63482753
Alanine aminotransferase increased	44.32	35.92	36	2651	103734	63382601
Pericardial effusion	42.06	35.92	22	2665	30036	63456299

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Malignant neoplasm progression	344.94	36.14	139	1681	87907	34867204
Metastases to central nervous system	156.23	36.14	43	1777	8162	34946949
Diarrhoea	83.19	36.14	101	1719	389811	34565300
Nausea	56.42	36.14	78	1742	339830	34615281
Metastases to liver	44.22	36.14	19	1801	13644	34941467
Pericarditis	43.72	36.14	18	1802	11627	34943484
Vomiting	41.16	36.14	57	1763	247564	34707547

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Malignant neoplasm progression	651.60	30.90	247	3788	135743	79604610
Metastases to central nervous system	357.42	30.90	95	3940	16280	79724073
Diarrhoea	147.95	30.90	200	3835	880289	78860064
Nausea	117.88	30.90	188	3847	957008	78783345
Vomiting	97.45	30.90	142	3893	665686	79074667
Metastases to liver	75.24	30.90	34	4001	28280	79712073
Death	72.96	30.90	114	3921	566400	79173953
Pericardial effusion	59.46	30.90	34	4001	46203	79694150
Neoplasm progression	58.54	30.90	35	4000	51647	79688706
Decreased appetite	57.14	30.90	78	3957	342340	79398013

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01ED02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Anaplastic lymphoma kinase (ALK) inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:62434	ALK inhibitor
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000020001	Tyrosine Kinase Inhibitors
FDA MoA	N0000185504	Cytochrome P450 2C9 Inhibitors
FDA MoA	N0000190114	Cytochrome P450 3A Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Non-small cell lung cancer	indication	254637007	DOID:3908
ALK fusion gene-positive non-small-cell lung cancer	indication	830151004

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.21	Basic
pKa2	2.49	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
150MG	ZYKADIA	NOVARTIS	N205755	April 29, 2014	DISCN	CAPSULE	ORAL	8377921	Nov. 20, 2027	TREATMENT OF A CANCER MEDIATED BY AN ANAPLASTIC LYMPHOMA KINASE (ALK)
150MG	ZYKADIA	NOVARTIS	N211225	March 18, 2019	RX	TABLET	ORAL	8377921	Nov. 20, 2027	TREATMENT OF A CANCER MEDIATED BY AN ANAPLASTIC LYMPHOMA KINASE (ALK)
150MG	ZYKADIA	NOVARTIS	N205755	April 29, 2014	DISCN	CAPSULE	ORAL	8703787	Feb. 2, 2032	TREATMENT OF A CANCER MEDIATED BY AN ANAPLASTIC LYMPHOMA KINASE (ALK)
150MG	ZYKADIA	NOVARTIS	N211225	March 18, 2019	RX	TABLET	ORAL	8703787	Feb. 2, 2032	TREATMENT OF A CANCER MEDIATED BY AN ANAPLASTIC LYMPHOMA KINASE (ALK)

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
150MG	ZYKADIA	NOVARTIS	N205755	April 29, 2014	DISCN	CAPSULE	ORAL	May 26, 2024	TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS ARE ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE AS DETECTED BY AN FDA-APPROVED TEST
150MG	ZYKADIA	NOVARTIS	N211225	March 18, 2019	RX	TABLET	ORAL	May 26, 2024	FDA HAS NOT RECOGNIZED ORPHAN-DRUG EXCLUSIVITY (ODE) FOR THIS DRUG, BUT IT CONTAINS THE SAME ACTIVE MOIETY OR MOIETIES AS ANOTHER DRUG(S) THAT WAS ELIGIBLE FOR ODE, AND ALSO SHARES ODE-PROTECTED USE(S) OR INDICATION(S) WITH THAT DRUG(S). AN APPLICATION SEEKING APPROVAL FOR THE SAME ACTIVE MOIETY OR MOIETIES, INCLUDING AN ANDA THAT CITES THIS NDA AS ITS BASIS OF SUBMISSION, MAY NOT BE APPROVED FOR SUCH ODE-PROTECTED USE(S) AND INDICATION(S)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
ALK tyrosine kinase receptor	Kinase	Q9UM73	ALK_HUMAN	INHIBITOR	IC50	9.70	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.90	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		EC50	7.05	CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		IC50	5.90	CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN		IC50	5.89	CHEMBL
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		IC50	6.05	CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN		IC50	5.77	CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		IC50	6.25	CHEMBL
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN		IC50	7.22	CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		IC50	6.40	CHEMBL

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External reference:

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ID	Source
4MK	PDB_CHEM_ID
015504	NDDF
1535457	RXNORM
219616	MMSL
30281	MMSL
4033301	VUID
4033301	VANDF
57379345	PUBCHEM_CID
703146007	SNOMEDCT_US
704310000	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ZYKADIA	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0694	TABLET, FILM COATED	150 mg	ORAL	NDA	30 sections
ZYKADIA	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0694	TABLET, FILM COATED	150 mg	ORAL	NDA	30 sections
ZYKADIA	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0694	TABLET, FILM COATED	150 mg	ORAL	NDA	30 sections

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