Ceritinib

Ceritinib
Clinical data

Trade names	Zykadia
AHFS/Drugs.com	Multum Consumer Information
Pregnancy category	US: D (Evidence of risk)
Routes of administration	Oral
ATC code	L01XE28 (WHO)
Legal status
Legal status	US: ℞-only
Identifiers
IUPAC name 5-Chloro-N²-[2-isopropoxy-5-methyl-4-(4-piperidinyl)phenyl]-N⁴-[2-(isopropylsulfonyl)phenyl]-2,4-pyrimidinediamine
Synonyms	LDK378
CAS Number	1032900-25-6
PubChem (CID)	57379345
DrugBank	DB09063
ChemSpider	29315053
UNII	K418KG2GET^Y
KEGG	D10551
ChEBI	CHEBI:78432
ChEMBL	CHEMBL2403108
Chemical and physical data
Formula	C₂₈H₃₆ClN₅O₃S
Molar mass	558.14 g/mol
3D model (Jmol)	Interactive image
SMILES CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl
InChI InChI=1S/C28H36ClN5O3S/c1-17(2)37-25-15-21(20-10-12-30-13-11-20)19(5)14-24(25)33-28-31-16-22(29)27(34-28)32-23-8-6-7-9-26(23)38(35,36)18(3)4/h6-9,14-18,20,30H,10-13H2,1-5H3,(H2,31,32,33,34) Key:VERWOWGGCGHDQE-UHFFFAOYSA-N

Ceritinib (trade name Zykadia) is a drug for the treatment of a specific type of lung cancer.^[1] It is an anaplastic lymphoma kinase (ALK) inhibitor.^[2] It was approved in April 2014 by the Food and Drug Administration for the treatment of ALK-positive metastatic non-small cell lung cancer (NSCLC) following treatment with crizotinib.^[1]

References

1 2 "FDA Approves Ceritinib for ALK-Positive Lung Cancer". Medscape. April 29, 2014.
↑ Shaw AT, Kim DW, Mehra R, Tan DS, Felip E, Chow LQ, Camidge DR, Vansteenkiste J, Sharma S, De Pas T, Riely GJ, Solomon BJ, Wolf J, Thomas M, Schuler M, Liu G, Santoro A, Lau YY, Goldwasser M, Boral AL, Engelman JA (2014). "Ceritinib in ALK-Rearranged Non–Small-Cell Lung Cancer". N Engl J Med. 370: 1189–1197. doi:10.1056/NEJMoa1311107. PMID 24670165.

Receptor tyrosine kinase	ErbB: HER1/EGFR (Cetuximab Panitumumab) HER2/neu (Trastuzumab Trastuzumab emtansine)

Others for solid tumors	EpCAM (Catumaxomab Edrecolomab) VEGF-A (Bevacizumab)

Leukemia/lymphoma	lymphoid: CD20 (Ibritumomab Ofatumumab Rituximab Tositumomab), CD30 (Brentuximab), CD52 (Alemtuzumab) myeloid: CD33 (Gemtuzumab)

Receptor tyrosine kinase	ErbB: HER1/EGFR (Erlotinib Gefitinib Osimertinib Vandetanib) HER1/EGFR and HER2/neu Afatinib Lapatinib Neratinib RTK class III: C-kit and PDGFR (Axitinib Masitinib Pazopanib Sunitinib Sorafenib Toceranib) FLT3 (Lestaurtinib) VEGFR Axitinib Cediranib Lenvatinib Nintedanib Pazopanib Regorafenib Semaxanib Sorafenib Sunitinib Tivozanib Toceranib Vandetanib RET inhibitors: Vandetanib (also VEGFR and EGFR). Entrectinib (ALK, ROS1, NTRK). c-MET inhibitor: Cabozantinib (also VEGFR2).

Non-receptor	bcr-abl Imatinib Dasatinib Nilotinib Ponatinib Radotinib Src (Bosutinib) Janus kinase Lestaurtinib Momelotinib Ruxolitinib Pacritinib MAP2K Cobimetinib Selumetinib Trametinib Binimetinib EML4-ALK Alectinib Ceritinib Crizotinib Bruton's (Ibrutinib)

Other

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