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Regorafenib and DIBIRI

Sun Yat-sen University · Phase 3 active Small molecule

Regorafenib is a multi-kinase inhibitor that blocks tumor angiogenesis and growth signaling, while DIBIRI (dinitro-irinotecan) is a lipophilic prodrug of irinotecan that enhances drug delivery to tumors.

Regorafenib is a multi-kinase inhibitor that blocks tumor angiogenesis and growth signaling, while DIBIRI (dinitro-irinotecan) is a lipophilic prodrug of irinotecan that enhances drug delivery to tumors. Used for Metastatic colorectal cancer (Phase 3 trial).

At a glance

Generic nameRegorafenib and DIBIRI
Also known asDrug: Irinotecan, Procedure: TACE, Device: drug eluting-bead
SponsorSun Yat-sen University
Drug classMulti-kinase inhibitor (regorafenib) combined with topoisomerase I inhibitor (DIBIRI)
TargetVEGFR, FGFR, KIT, RET, RAF (regorafenib); Topoisomerase I (DIBIRI/irinotecan)
ModalitySmall molecule
Therapeutic areaOncology
PhasePhase 3

Mechanism of action

Regorafenib inhibits multiple receptor tyrosine kinases (VEGFR, FGFR, KIT, RET, RAF) involved in tumor angiogenesis and proliferation. DIBIRI is a nanoparticle-bound formulation of irinotecan designed to improve tumor accumulation and reduce systemic toxicity. The combination leverages anti-angiogenic and cytotoxic mechanisms to target colorectal cancer.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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