Masitinib

Masitinib
Systematic (IUPAC) name

4-[(4-Methylpiperazin-1-yl)methyl]-N-(4-methyl-3-{[4-(pyridin-3-yl)-1,3-thiazol-2-yl]amino}phenyl)benzamide
Clinical data
Trade names	Masivet, Kinavet
AHFS/Drugs.com	International Drug Names
Identifiers
CAS Number	790299-79-5
ATC code	L01XE22 (WHO)
PubChem	CID 10074640
ChemSpider	8250179
ChEMBL	CHEMBL1908391
Chemical data
Formula	C₂₈H₃₀N₆OS
Molar mass	498.64 g/mol
SMILES O=C(c1ccc(cc1)CN2CCN(C)CC2)Nc3cc(c(cc3)C)Nc4nc(cs4)c5cccnc5
InChI InChI=InChI=1S/C28H30N6OSc1-20-5-10-24(16-25(20)31-28-32-26(19-36-28)23-4-3-11-29-17-23)30-27(35)22-8-6-21(7-9-22)18-34-14-12-33(2)13-15-34h3-11,16-17,19H,12-15,18H2,1-2H3,(H,30,35)(H,31,32) Key:WJEOLQLKVOPQFV-UHFFFAOYSA-N

Masitinib is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs.^[1]^[2] Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet and has been available for veterinaries since 2011.

Masitinib is being studied for several human conditions including cancers. It is used in Europe to fight orphan diseases.^[3]

Mechanism of action

Masitinib inhibits the receptor tyrosine kinase c-Kit which is displayed by various types of tumour.^[2] It also inhibits the platelet derived growth factor receptor (PDGFR) and fibroblast growth factor receptor (FGFR).

References

↑ Hahn, K.A.; Oglivie, G.; Rusk, T.; Devauchelle, P.; Leblanc, A.; Legendre, A.; Powers, B.; Leventhal, P.S.; Kinet, J.-P.; Palmerini, F.; Dubreuil, P.; Moussy, A.; Hermine, O. (2008). "Masitinib is Safe and Effective for the Treatment of Canine Mast Cell Tumors". Journal of Veterinary Internal Medicine 22 (6): 1301–1309. doi:10.1111/j.1939-1676.2008.0190.x. ISSN 0891-6640.
1 2 Information about Masivet at the European pharmacy agency website
↑ Orphan designation for Masitinib at the European pharmacy agency website

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)

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