pemigatinib (Pemazyre)

Indications

• unresectable locally advanced or metastatic cholangiocarcinoma with FGFR2 fusion or other rearrangement

Dosage

• 13.5 mg orally once daily for 14 consecutive days followed by 7 days off i 21-day cycles
• continue treatment until disease progression or unacceptable toxicity
• Swallow tablet whole, with or without food

Tabs: 4.5 mg, 9 mg, & 13.5 mg

Monitor

• ophthalmoscopy including optical coherence tomography
  • prior to initiation of therapy
  • every 2 months for the first 6 months of treatment
  • every 3 months thereafter,

Adverse effects

• >= 20%:
  • hyperphosphatemia, hypophosphatemia
  • diarrhea, constipation, dysgeusia, nausea, vomiting, stomatitis
  • dry eye, dry mouth, arthralgia, abdominal pain, back pain
  • alopecia, nail toxicity, dry skin
  • fatigue, decreased appetite
• serious: retinal pigment epithelium detachment

• drug adverse effects of tyrosine kinase inhibitor(s)

Drug interactions

• strong or moderate cyp3A inducers or inhibitors

Mechanism of action

• tyrosine kinase inhibitor
  • targets FGFR1, FGFR2 & FGFR3 with IC50 values of < 2 nM

More general terms

• small inhibitory antineoplastic agent (ib drug)
• tyrosine kinase inhibitor

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=86705695