Gandotinib

Gandotinib (LY-2784544) is an experimental drug developed by Eli Lilly for treatment of cancer. It is a small molecule JAK2 (Janus kinase) inhibitor, with additional minor inhibition of STAT3.

Gandotinib
Clinical data
Routes of
administration		PO
ATC code
  • none
Identifiers
IUPAC name
  • 3-(4-Chloro-2-fluorobenzyl)-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC23H25ClFN7O
Molar mass469.95 g·mol−1
3D model (JSmol)
SMILES
  • C12C(=CC(=NN1C(=C(N=2)C)CC1C(=CC(=CC=1)Cl)F)NC1=NNC(=C1)C)CN1CCOCC1
InChI
  • InChI=1S/C23H25ClFN7O/c1-14-9-21(29-28-14)27-22-11-17(13-31-5-7-33-8-6-31)23-26-15(2)20(32(23)30-22)10-16-3-4-18(24)12-19(16)25/h3-4,9,11-12H,5-8,10,13H2,1-2H3,(H2,27,28,29,30)
  • Key:SQSZANZGUXWJEA-UHFFFAOYSA-N

In a phase I trial, 16% of patients receiving the drug developed tumor lysis syndrome.[1] A phase II trial is underway for patients with myeloproliferative neoplasms, polycythemia vera, essential thrombocythemia, or myelofibrosis, who had failed ruxolitinib.[2][3]

References
  1. "Gandotinib - Eli Lilly". AdisInsight. Springer Nature Switzerland AG.
  2. Clinical trial number NCT01594723 for "A Study of LY2784544 in Participants With Myeloproliferative Neoplasms" at ClinicalTrials.gov
  3. Berdeja J, Palandri F, Baer MR, Quick D, Kiladjian JJ, Martinelli G, Verma A, Hamid O, Walgren R, Pitou C, Li PL, Gerds AT (August 2018). "Phase 2 study of gandotinib (LY2784544) in patients with myeloproliferative neoplasms". Leukemia Research. 71: 82–88. doi:10.1016/j.leukres.2018.06.014. PMID 30025280.
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