Pacritinib

Pacritinib
Clinical data
Other names	SB1518
Routes of; administration	Oral
ATC code	None;
Legal status
Legal status	Investigational;
Identifiers
	show IUPAC name
CAS Number	937272-79-2;
PubChem CID	46216796;
ChemSpider	28518965;
UNII	G22N65IL3O;
KEGG	D11768;
ChEMBL	ChEMBL2035187;
Chemical and physical data
Formula	C28H32N4O3
Molar mass	472.589 g·mol−1
3D model (JSmol)	Interactive image;
	show SMILES
	show InChI

Pacritinib (INN^[1]) is a macrocyclic Janus kinase inhibitor that is being developed for the treatment of myelofibrosis. It mainly inhibits Janus kinase 2 (JAK2) and Fms-like tyrosine kinase 3 (FLT3). The drug was in Phase III clinical trials as of 2013.^[2]

The drug was given fast-track status in 2014.^[3] In 2016, the FDA placed a full clinical hold on pacritinib due to concerns about increased mortality in patients receiving the drug in the "PERSIST-2" trial.^[4] The clinical hold was lifted in January 2017.^[5]

References[]

^ "International Nonproprietary Names for Pharmaceutical Substances (INN) List 104" (PDF). WHO Drug Information. 24 (4): 386. 2010.
^ "JAK-Inhibitoren: Neue Wirkstoffe für viele Indikationen". Pharmazeutische Zeitung (in German) (21). 2013.
^ Adams B (29 August 2016). "Struggling CTI reveals new pacritinib data, misses a primary endpoint". Fierce Biotech.
^ "CTI BioPharma's (CTIC) Pacritinib Placed on Full Clinical Hold; NDA Withdrawn". StreetInsider. 10 February 2016.
^ "CTI BioPharma Announces Removal Of Full Clinical Hold On Pacritinib". PR Newswire. Retrieved 18 April 2017.

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[1] "International Nonproprietary Names for Pharmaceutical Substances (INN) List 104" (PDF). WHO Drug Information. 24 (4): 386. 2010.

[2] "JAK-Inhibitoren: Neue Wirkstoffe für viele Indikationen". Pharmazeutische Zeitung (in German) (21). 2013.

[3] Adams B (29 August 2016). "Struggling CTI reveals new pacritinib data, misses a primary endpoint". Fierce Biotech.

[4] "CTI BioPharma's (CTIC) Pacritinib Placed on Full Clinical Hold; NDA Withdrawn". StreetInsider. 10 February 2016.

[Newswire2017-5] "CTI BioPharma Announces Removal Of Full Clinical Hold On Pacritinib". PR Newswire. Retrieved 18 April 2017.

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Clinical data

Other names	SB1518
Routes of administration	Oral
ATC code	None
Legal status
Legal status	Investigational
Identifiers
show IUPAC name (16E)-11-[2-(1-Pyrrolidinyl)ethoxy]-14,19-dioxa-5,7,26-triazatetracyclo[19.3.1.1^2,6.1^8,12]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene
CAS Number	937272-79-2
PubChem CID	46216796
ChemSpider	28518965
UNII	G22N65IL3O
KEGG	D11768
ChEMBL	ChEMBL2035187
Chemical and physical data
Formula	C₂₈H₃₂N₄O₃
Molar mass	472.589 g·mol⁻¹
3D model (JSmol)	Interactive image
show SMILES c1cc2cc(c1)-c3ccnc(n3)Nc4ccc(c(c4)COC/C=C/COC2)OCCN5CCCC5
show InChI InChI=1S/C28H32N4O3/c1-2-13-32(12-1)14-17-35-27-9-8-25-19-24(27)21-34-16-4-3-15-33-20-22-6-5-7-23(18-22)26-10-11-29-28(30-25)31-26/h3-11,18-19H,1-2,12-17,20-21H2,(H,29,30,31)/b4-3+ Key:HWXVIOGONBBTBY-ONEGZZNKSA-N