Angiokinase inhibitor (VEGFR / FGFR / PDGFR)
Triple receptor-tyrosine-kinase blockade of the fibrosis–angiogenesis axis
- Starves tumor vasculature
- Slows fibrosis
- VEGF-pathway effects: hypertension, bleeding, impaired wound healing
- One ATP-pocket inhibitor, three receptor families: VEGFR-1/2/3, FGFR-1/2/3, PDGFR-alpha/beta
- Slows fibroblast proliferation and vessel remodeling — the IPF rationale
- ➔ nintedanib (OFEV) — slows FVC decline in IPF, SSc-ILD, progressive fibrosing ILD
- Class marks: diarrhea, hepatotoxicity, VEGF-type bleeding/thrombosis risk, embryotoxicity
Drugs with this mechanism (4)
- Nintedanib — Oral angiokinase inhibitor that slows fibrosing interstitial lung disease.
- Pazopanib — Oral VEGFR-focused angiokinase inhibitor for renal-cell and soft-tissue cancers; hepatotoxic.
- Regorafenib — Oral multikinase inhibitor for refractory colorectal and GIST tumors.
- Sorafenib — Multikinase inhibitor for selected liver, kidney, and thyroid cancers; hand-foot skin reaction, diarrhea, and hypertension are prominent.
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