BIBF-1120

BIBF-1120 화학적 특성, 용도, 생산

• 개요

  BIBF 1120 is a triple kinase inhibitor blocking vascular endothelial growth factor receptor, PDGF receptor, and FGF receptor, which has a potential to inhibit tumor growth and pulmonary fibrosis.

• Characteristics

  Primary targets: PDGFR; VEGFR; FGFR
  Class: receptor tyrosine kinase
  Treatment: ILD, IPF
  Oral bioavailability = 4.7%
  Elimination half-life = 10

• Anticancer Research

  BIBF 1120 is a potent inhibitor of VEGFR as well as PDGF and fibroblast growth factor receptor. In a randomized phase II placebo-controlled trial, patients who had just completed chemotherapy for relapsed ovarian cancer, with evidence of response, but at high risk of further early recurrence were treated with BIBF 1120. The study drug was taken continuously (28-day cycles) for 9 cycles (36 weeks) or until disease progression or patient withdrawal. The 36-week PFS 26-week rates were 16.3% and 5.0% in the BIBF 1120 and placebo groups, respectively (HR 0.65; 95% Cl, 0.42 to 1.02; P = .06). Toxicity was also well tolerated.This has prompted a phase III trial (NCTO1O15118) where BIBF 1120 will be combined with carboplatin/paclitaxel as front-line chemotherapy in ovarian cancer.

• 부작용

  Most of the adverse effects associated with BTBF-1120 were tolerable. They include diarrhea, nausea, vomiting, abdominal pain, and reversible increase in liver enzymes.

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