Radotinib

Radotinib
Systematic (IUPAC) name

4-Methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyrazin-2-ylpyrimidin-2-yl)amino]benzamide
Clinical data
Trade names	Supect
Identifiers
CAS Number	926037-48-1
ATC code	None
PubChem	CID 16063245
ChemSpider	17222861
Chemical data
Formula	C₂₇H₂₁F₃N₈O
Molar mass	530.50 g/mol
SMILES CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)N3C=C(N=C3)C)C(F)(F)F)NC4=NC=CC(=N4)C5=NC=CN=C5
InChI InChI=1S/C27H21F3N8O/c1-16-3-4-18(9-23(16)37-26-33-6-5-22(36-26)24-13-31-7-8-32-24)25(39)35-20-10-19(27(28,29)30)11-21(12-20)38-14-17(2)34-15-38/h3-15H,1-2H3,(H,35,39)(H,33,36,37) Key:DUPWHXBITIZIKZ-UHFFFAOYSA-N

Radotinib (INN; trade name Supect), and sometimes referred to by its investigational name IY5511, is a drug for the treatment of different types of cancer, most notably Philadelphia chromosome-positive (Ph⁺) chronic myeloid leukemia (CML)^[1] with resistance or intolerance of other Bcr-Abl tyrosine-kinase inhibitors, such as patients resistant or intolerant to imatinib.

Radotinib is being developed by Ilyang Pharmaceutical Co., Ltd of South Korea^[2] and is co-marketed by Daewoong Pharmaceutical Co. Ltd, in South Korea.^[3] Radotinib completed a multi-national Phase II clinical trial study in 2012^[4] and in August 2011, Ilyang initiated a Phase III, multinational, multi-center, open-label, randomized study for first-line indication.^[5] Its mechanism of action involves inhibition of the Bcr-Abl tyrosine kinase and of platelet-derived growth factor receptor (PDGFR).^[6]

Targeted therapy / extracellular chemotherapeutic agents/antineoplastic agents (L01)

CI monoclonal antibodies ("-mab")

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)

Tyrosine-kinase inhibitors ("-nib")

Receptor tyrosine kinase	ErbB: HER1/EGFR (Erlotinib Gefitinib 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 Ruxolitinib Pacritinib MAP2K Cobimetinib Selumetinib Trametinib Binimetinib EML4-ALK Alectinib Ceritinib Crizotinib Bruton's (Ibrutinib)

Other

fusion protein against VEGF (Aflibercept)
proapoptotic peptide against ANXA2 and prohibitin (Adipotide)
exotoxin against IL-2 (Denileukin diftitox)
mTOR inhibitors
- Everolimus
- Temsirolimus
hedgehog inhibitors
- Sonidegib
- Vismodegib
CDK inhibitor (Palbociclib)

References

↑ Joanne Bronson, Amelia Black, T. G. Murali Dhar, Bruce A. Ellsworth, and J. Robert Merritt. "Radotinib (Anticancer)". Annual Reports in Medicinal Chemistry 48: 523–524. doi:10.1016/b978-0-12-417150-3.00028-4. |chapter= ignored (help)
↑ http://www.ilyang.co.kr/english/rnd/rnd03.asp
↑ http://www.dailypharm.com/Users/News/EnglishNews.html?NewsID=3108&nStart=1023&mode=&searchValue=
↑ http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4077080/
↑ https://clinicaltrials.gov/ct2/show/NCT01511289?term=radotinib&rank=1
↑ "Radotinib hydrochloride". NCI Drug Dictionary. National Cancer Institute.

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