Gandotinib Explained

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
Routes Of Administration:PO
Cas Number:1229236-86-5
Unii:ANC71R916O
Atc Prefix:none
Pubchem:46213929
Chemspiderid:25027412
Kegg:D10365
C:23
H:25
Cl:1
F:1
N:7
O:1
Smiles:C12C(=CC(=NN1C(=C(N=2)C)CC1C(=CC(=CC=1)Cl)F)NC1=NNC(=C1)C)CN1CCOCC1
Stdinchi: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)
Stdinchikey:SQSZANZGUXWJEA-UHFFFAOYSA-N

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.

In 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]

Notes and References

  1. Web site: Gandotinib - Eli Lilly . AdisInsight . Springer Nature Switzerland AG .
  2. Berdeja J, Palandri F, Baer MR, Quick D, Kiladjian JJ, Martinelli G, Verma A, Hamid O, Walgren R, Pitou C, Li PL, Gerds AT . Phase 2 study of gandotinib (LY2784544) in patients with myeloproliferative neoplasms . Leukemia Research . 71 . 82–88 . August 2018 . 30025280 . 10.1016/j.leukres.2018.06.014 .