infigratinib (Truseltiq)

Indications

• treatment of metastatic cholangiocarcinoma with FGFR2 fusion or other gener rearrangement as detected by an FDA-approved test*

* FDA also approved companion diagnostic test for FGFR2 fusion or other rearrangement

Dosage

• 125 mg PO QD for 21 days followed by 7 off days in 28 day cycles until disease progression or unacceptable toxicity

Tabs: 25 mg, 50 mg, 75 mg, 100 mg

Adverse effects

• >20%
  • hyperphosphatemia, increased serum creatinine, nail toxicity, stomatitis, dry eye, fatigue, alopecia, palmar-plantar erythrodysesthesia syndrome, arthralgia, dysgeusia, constipation, abdominal pain, dry mouth, eyelash changes, diarrhea, dry skin, decreased appetite, vision blurred, vomiting
• serious risks
  • hyperphosphatemia
  • retinal pigment epithelium detachment

Mechanism of action

• inhibits FGFR with IC50 values of 1.1, 1, 2, & 61 nM for FGFR1, FGFR2, FGFR3, & FGFR4, respectively
• major human metabolites of infigratinib have similar in vitro binding affinities for FGFR1, FGFR2, & FGFR3 compared to infigratinib.
• infigratinib inhibits FGFR signaling & decreased cell proliferation in cancer cell lines with activating FGFR amplifications, mutations, or fusions

More general terms

• small inhibitory antineoplastic agent (ib drug)