Bosutinib

Bosutinib
Clinical data
Trade names	Bosulif
License data	EU EMA: by INN; US DailyMed: Bosutinib;
Routes of; administration	By mouth
ATC code	L01EA04 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); UK: POM (Prescription only); US: ℞-only; EU: Rx-only;
Pharmacokinetic data
Protein binding	94–96%
Metabolism	By CYP3A4, to inactive metabolites
Elimination half-life	22.5±1.7 hours
Excretion	Fecal (91.3%) and kidney (3%)
Identifiers
	IUPAC name 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile;
CAS Number	380843-75-4 ;
PubChem CID	5328940;
IUPHAR/BPS	5710;
DrugBank	DB06616 ;
ChemSpider	4486102 ;
UNII	5018V4AEZ0;
KEGG	D03252;
ChEBI	CHEBI:39112 ;
ChEMBL	ChEMBL288441 ;
CompTox Dashboard (EPA)	DTXSID10861568 ;
ECHA InfoCard	100.149.122
Chemical and physical data
Formula	C26H29Cl2N5O3
Molar mass	530.45 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Clc1c(OC)cc(c(Cl)c1)Nc4c(C#N)cnc3cc(OCCCN2CCN(CC2)C)c(OC)cc34;
	InChI InChI=1S/C26H29Cl2N5O3/c1-32-6-8-33(9-7-32)5-4-10-36-25-13-21-18(11-24(25)35-3)26(17(15-29)16-30-21)31-22-14-23(34-2)20(28)12-19(22)27/h11-14,16H,4-10H2,1-3H3,(H,30,31) ; Key:UBPYILGKFZZVDX-UHFFFAOYSA-N ;
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Bosutinib, sold under the brand name Bosulif, is a small molecule BCR-ABL and src tyrosine kinase inhibitor used for the treatment of chronic myelogenous leukemia.^[2]

Originally synthesized by Wyeth, it is being developed by Pfizer.

^ "Prescription medicines: registration of new chemical entities in Australia, 2014". Therapeutic Goods Administration (TGA). 21 June 2022. Archived from the original on 10 April 2023. Retrieved 10 April 2023.
^ Lipton JH, Brümmendorf TH, Sweet K, Apperley JF, Cortes JE. Practical considerations in the management of patients treated with bosutinib for chronic myeloid leukemia. Ann Hematol. 2024 Jul 18. doi: 10.1007/s00277-024-05851-4. Epub ahead of print. PMID: 39023573.