生物活性

• 描述Itacitinib is a selective JAK1 inhibitor with IC50 value of 2nM, and also exhibits less potency against JAK2 with IC50 value of 63nM. Itacitinib could both inhibit pancreatic tumor cell line growth (Hs700T and BxPC-3) in a 3D-spheroid culture system and reverse the growth of the spheroids stimulated by JAK/STAT3 signaling activated through addition of cytokines. Administration of Itacitinib at clinically relevant doses blocked tumor growth in human pancreatic xenograft models in mice both as monotherapy and in combination with cytotoxic agents such as gemcitabine. Combined therapy of Itacitinib at a dose of 60 mg/kg, BID, with BET inhibitor INCB054329 further reduced JAK-STAT signaling and synergized to inhibit myeloma cell growth in vivo.
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02257619	NSCLC (Non-small Cell Lung Car... more >>cinoma) Collapse <<	Phase 2	Terminated(Sponsor decision to... more >> not initiate part 2 due to slow enrollment and competing trials.) Collapse <<	-	United States, Arizona ... more >> Hot Springs, Arizona, United States United States, California Los Angeles, California, United States United States, District of Columbia Washington, District of Columbia, United States United States, Florida Orlando, Florida, United States United States, Michigan Detroit, Michigan, United States United States, Mississippi Pascagoula, Mississippi, United States United States, Missouri Kansas City, Missouri, United States United States, Nebraska Omaha, Nebraska, United States United States, New Hampshire Lebanon, New Hampshire, United States United States, North Carolina Goldsboro, North Carolina, United States United States, Ohio Cleveland, Ohio, United States United States, Pennsylvania Gettysburg, Pennsylvania, United States Hershey, Pennsylvania, United States United States, Rhode Island Pawtucket, Rhode Island, United States United States, South Carolina Spartanburg, South Carolina, United States United States, Texas Round Rock, Texas, United States Collapse <<
  NCT03272464	Melanoma	Phase 1	Recruiting	September 30, 2023	United States, Massachusetts ... more >> Massachusetts General Hospital Recruiting Boston, Massachusetts, United States, 02214 Contact: Keith Flaherty, MD    617-724-4800    KFLAHERTY@mgh.harvard.edu    Principal Investigator: Keith T. Flaherty, MD Collapse <<
  NCT02559492	Solid Tumors	Phase 1	Active, not recruiting	June 2019	United States, California ... more >> Duarte, California, United States United States, Colorado Denver, Colorado, United States United States, Connecticut New Haven, Connecticut, United States United States, Florida Tampa, Florida, United States United States, Illinois Chicago, Illinois, United States United States, Minnesota Rochester, Minnesota, United States United States, North Carolina Huntersville, North Carolina, United States United States, Tennessee Nashville, Tennessee, United States United States, Texas Dallas, Texas, United States Houston, Texas, United States United States, Utah Salt Lake City, Utah, United States Collapse <<

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• 参考文献

• [1] Bissonnette R, Luchi M, et al. A randomized, double-blind, placebo-controlled, dose-escalation study of the safety and efficacy of INCB039110, an oral janus kinase 1 inhibitor, in patients with stable, chronic plaque psoriasis. J Dermatolog Treat. 2016 Aug;27(4):332-8.

  [2] Zhang Y, Warren MS, et al. Impact on creatinine renal clearance by the interplay of multiple renal transporters: a case study with INCB039110. Drug Metab Dispos. 2015 Apr;43(4):485-9.