Gandotinib

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	1229236-86-5 ;
PubChem CID	46213929;
ChemSpider	25027412;
UNII	ANC71R916O;
KEGG	D10365;
CompTox Dashboard (EPA)	DTXSID20153789 ;
Chemical and physical data
Formula	C23H25ClFN7O
Molar mass	469.95 g·mol−1
3D model (JSmol)	Interactive image;
	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;

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 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

"Gandotinib - Eli Lilly". AdisInsight. Springer Nature Switzerland AG.
Clinical trial number NCT01594723 for "A Study of LY2784544 in Participants With Myeloproliferative Neoplasms" at ClinicalTrials.gov
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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[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

[pmid30025280-3] 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.