From Wikipedia, the free encyclopedia
Chemical compound
Radotinib
Trade names Supect
ATC code
4-Methyl-N -[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyrazin-2-ylpyrimidin-2-yl)amino]benzamide
CAS Number
PubChem
CID
ChemSpider
UNII
CompTox Dashboard (
EPA )
Formula C 27 H 21 F 3 N 8 O
Molar mass 530.515 g·mol−1 3D model (
JSmol )
Cc1cn(-c2cc(NC(=O)c3ccc(C)c(Nc4nccc(-c5cnccn5)n4)c3)cc(C(F)(F)F)c2)cn1
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]
References
^ Bronson J, Black A, Dhar TG, Ellsworth BA, Merritt JR (2013). "To Market, To Market - 2012: Radotinib (Anticancer)". Annual Reports in Medicinal Chemistry . 48 : 523–524.
doi :
10.1016/b978-0-12-417150-3.00028-4 .
ISBN
9780124171503 .
^
"Il-Yang Pharmaceutical" .
^ Yoon EK (23 October 2012).
"Daewoong will market Ilyang's new leukemia drug" . Daily Pharm News . Archived from
the original on 2016-03-03.
^ Kim SH, Menon H, Jootar S, Saikia T, Kwak JY, Sohn SK, et al. (July 2014).
"Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors" . Haematologica . 99 (7): 1191–1196.
doi :
10.3324/haematol.2013.096776 .
PMC
4077080 .
PMID
24705186 .
^ Clinical trial number
NCT01511289 for "A Phase 3 Multinational, Multi-center, Open-Label, Randomized Study of the Efficacy of Radotinib Versus Imatinib in Newly Diagnosed Ph+ CML Patients in Early Chronic Phase" at
ClinicalTrials.gov
^
"Radotinib hydrochloride" . NCI Drug Dictionary .
National Cancer Institute . 2011-02-02.
CI
monoclonal antibodies ("-mab")
Tyrosine kinase inhibitors ("-nib")
Receptor tyrosine kinase
RET inhibitors:
Entrectinib (ALK, ROS1, NTRK),
Futibatinib (FGFR2),
Infigratinib ,
Larotrectinib (NTRK),
Pemigatinib (FGFR),
Pralsetinib ,
Repotrectinib (ROS1, TRK, ALK),
Selpercatinib (VEGFR, FGFR),
Vandetanib (VEGFR, EGFR).
Non-receptor
Other
Angiopoietin
CNTF
EGF (ErbB)
FGF
FGFR1
FGFR2
Agonists:
Ersofermin
FGF (
1 ,
2 (bFGF) ,
3 ,
4 ,
5 ,
6 ,
7 (
KGF ),
8 ,
9 ,
10 (KGF2) ,
17 ,
18 ,
22 )
Palifermin
Repifermin
Selpercatinib
Sprifermin
Trafermin
FGFR3
FGFR4 Unsorted
HGF (c-Met)
IGF
LNGF (p75NTR )
PDGF
RET (GFL)
SCF (c-Kit)
TGFβ
Trk
TrkA
Negative allosteric modulators:
VM-902A
TrkB
Agonists:
3,7-DHF
3,7,8,2'-THF
4'-DMA-7,8-DHF
7,3'-DHF
7,8-DHF
7,8,2'-THF
7,8,3'-THF
Amitriptyline
BDNF
BNN-20
Deoxygedunin
Deprenyl
Diosmetin
DMAQ-B1
HIOC
LM22A-4
N-Acetylserotonin
NT-3
NT-4
Norwogonin (5,7,8-THF)
R7
R13
TDP6
TrkC
VEGF Others
Additional growth factors:
Adrenomedullin
Colony-stimulating factors (see
here instead)
Connective tissue growth factor (CTGF)
Ephrins (
A1 ,
A2 ,
A3 ,
A4 ,
A5 ,
B1 ,
B2 ,
B3 )
Erythropoietin (see
here instead)
Glucose-6-phosphate isomerase (GPI; PGI, PHI, AMF)
Glia maturation factor (GMF)
Hepatoma-derived growth factor (HDGF)
Interleukins /
T-cell growth factors (see
here instead)
Leukemia inhibitory factor (LIF)
Macrophage-stimulating protein (MSP; HLP, HGFLP)
Midkine (NEGF2)
Migration-stimulating factor (MSF; PRG4)
Oncomodulin
Pituitary adenylate cyclase-activating peptide (PACAP)
Pleiotrophin
Renalase
Thrombopoietin (see
here instead)
Wnt signaling proteins
Additional growth factor receptor modulators:
Cerebrolysin (neurotrophin mixture)