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Chemical compound used in the treatment of tumors
Toceranib
Trade names Palladia
AHFS /
Drugs.com
Veterinary Use
License data
Routes of administration
By mouth
Drug class
Antineoplastic agent
ATCvet code
Legal status
Bioavailability 77%
Protein binding 91%-93%
Elimination half-life 16 h
5-[(5Z )-(5-fluoro-2-oxo-1,2-dihydro-3H -indol-3-ylidene)methyl]-2,4-dimethyl-N -[2-(pyrrolidin-1-yl)ethyl]-1H -pyrrole-3-carboxamide
CAS Number
PubChem
CID
ChemSpider
UNII
KEGG
ChEMBL
PDB ligand
CompTox Dashboard (
EPA )
Formula C 22 H 25 F N 4 O 2
Molar mass 396.466 g·mol−1 3D model (
JSmol )
Fc1ccc2c(c1)/C(C(=O)N2)=C/c4c(c(C(=O)NCCN3CCCC3)c([nH]4)C)C
InChI=1S/C22H25FN4O2/c1-13-19(12-17-16-11-15(23)5-6-18(16)26-21(17)28)25-14(2)20(13)22(29)24-7-10-27-8-3-4-9-27/h5-6,11-12,25H,3-4,7-10H2,1-2H3,(H,24,29)(H,26,28)/b17-12-
Key:SRSGVKWWVXWSJT-ATVHPVEESA-N
Toceranib is a
receptor tyrosine kinase inhibitor and is used in the treatment
[1] of canine
mast cell tumor also called
mastocytoma . Together with
masitinib (Kinavet (US)/Masivet (EU/ROW) by AB Science), toceranib is the only dog-specific anti-
cancer drug
[2] approved by the U.S.
Food and Drug Administration (FDA).
[3]
[4] It is sold under the brand name Palladia as its phosphate salt, toceranib phosphate (
INN ) by
Pfizer . It was developed by
SUGEN as SU11654,
[5] a sister compound to
sunitinib , which was later approved for human therapies. Toceranib is likely to act mostly through inhibition of the
kit tyrosine kinase, though it may also have an
anti-angiogenic effect.
References
^ London CA, Malpas PB, Wood-Follis SL, et al. (June 2009).
"Multi-center, Placebo-controlled, Double-blind, Randomized Study of Oral Toceranib Phosphate (SU11654), a Receptor Tyrosine Kinase Inhibitor, for the Treatment of Dogs with Recurrent (Either Local or Distant) Mast Cell Tumor Following Surgical Excision" . Clin Cancer Res . 15 (11): 3856–65.
doi :
10.1158/1078-0432.CCR-08-1860 .
PMID
19470739 .
^
CBS News FDA Approves First-Ever Dog Cancer Drug
^
"FDA: First Drug to Treat Cancer in Dogs Approved" . U.S.
Food and Drug Administration (FDA) (Press release). 3 June 2009. Archived from
the original on 22 July 2010. Retrieved 2 October 2021 .
^
"Palladia New Animal Drug Application" (PDF) . U.S.
Food and Drug Administration (FDA) . 22 May 2009. Archived from
the original (PDF) on 16 November 2010. Retrieved 2 October 2021 .
^
"In Trials for New Cancer Drugs, Family Pets Are Benefiting, Too" . The New York Times . 24 November 2006. Retrieved 2 October 2021 .
External links
"Toceranib" . Drug Information Portal . U.S. National Library of Medicine.
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)