Fruquintinib
Deterministic view of the source YAML entity. Clinical authority remains with the cited source IDs and reviewer sign-off state.
| ID | DRUG-FRUQUINTINIB |
|---|---|
| Type | Drug |
| Aliases | ElunateFruzaqlaHMPL-013Фруквінтиніб |
| Status | reviewed 2026-04-27 | pending_clinical_signoff |
| Diseases | DIS-CRC |
| Sources | SRC-ESMO-COLON-2024 SRC-NCCN-COLON-2025 |
Drug Facts
| Class | Highly selective oral VEGFR1/2/3 tyrosine kinase inhibitor |
|---|---|
| Mechanism | Highly selective ATP-competitive small-molecule TKI of vascular endothelial growth factor receptors 1, 2, and 3 (VEGFR-1/2/3), with sub-nanomolar in-vitro potency and minimal off-target inhibition (negligible activity vs FGFR, PDGFR, KIT, RET) — the selectivity profile is intentionally narrow to improve tolerability vs multikinase TKIs (regorafenib, sorafenib). Blocks VEGF-driven angiogenesis and lymphangiogenesis in the tumor microenvironment; no direct antiproliferative effect on tumor cells. Pivotal evidence FRESCO-2 (multinational, Western mCRC, refractory after chemo + anti-VEGF + anti-EGFR if RAS-WT, ± TAS-102 / regorafenib): fruquintinib vs placebo + best supportive care, mOS 7.4 vs 4.8 mo HR 0.66, mPFS 3.7 vs 1.8 mo HR 0.32. FDA approval Nov 2023. Original China approval 2018 (Elunate, FRESCO trial). |
| Typical dosing | 5 mg PO once daily on a 3-weeks-on / 1-week-off schedule (28-day cycle), with or without food, until progression / unacceptable toxicity. Dose level -1 = 4 mg daily; -2 = 3 mg daily; permanent discontinuation if recurrent G3-4 at -2. Hold for hypertensive crisis, G3-4 hand-foot syndrome, G3-4 proteinuria, GI perforation / fistula, or severe hemorrhage. Stop 2 weeks pre-elective surgery and resume only after wound healing (≥2 weeks post-op typically). No formal renal adjustment for CrCl ≥30; not studied in severe hepatic impairment. |
| Ukraine registered | False |
| NSZU reimbursed | False |
| Ukraine last verified | 2026-04-27 |
Notes
Late-line refractory mCRC option alongside regorafenib and trifluridine/tipiracil (TAS-102) ± bevacizumab. Cross-trial comparison suggests numerically better tolerability than regorafenib (less HFS, less LFT elevation, more straightforward HTN management). FRESCO-2 enrolled patients post all-major-classes including TAS-102 / regorafenib — true salvage population. Baseline workup: BP, urinalysis (UPCR), LFTs, CBC, TSH, ECG, pregnancy test. Monitor BP weekly first 6 weeks then monthly, urinalysis monthly, LFTs monthly, TSH q3 months. Hold for SBP >160/100 — escalate antihypertensives (ACE-i / ARB first then CCB). Hold ≥2 weeks before elective surgery; resume only after full wound healing (typically ≥2 weeks post-op). UA access via EAP / self-pay; not on НСЗУ.
Used By
Algorithms
ALGO-CRC-METASTATIC-2L- ALGO-CRC-METASTATIC-2L
Regimens
REG-FRUQUINTINIB-CRC-3L- Fruquintinib monotherapy (FRESCO-2) — 3L+ refractory metastatic CRC