Pacritinib

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Pacritinib
Pacritinib skeletal.svg
Clinical data
Other namesSB1518
Routes of
administration
Oral
ATC code
Legal status
Legal status
  • Investigational
Identifiers
  • (16E)-11-[2-(1-Pyrrolidinyl)ethoxy]-14,19-dioxa-5,7,26-triazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC28H32N4O3
Molar mass472.589 g·mol−1
3D model (JSmol)
  • c1cc2cc(c1)-c3ccnc(n3)Nc4ccc(c(c4)COC/C=C/COC2)OCCN5CCCC5
  • 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

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

  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 ^ "CTI BioPharma's (CTIC) Pacritinib Placed on Full Clinical Hold; NDA Withdrawn".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.
  5. ^ "CTI BioPharma Announces Removal Of Full Clinical Hold On Pacritinib". PR Newswire. Retrieved 18 April 2017.