Fruquintinib
Clinical data
Trade namesFruzaqla
Other namesHMPL-013
License data
Routes of
administration		By mouth
Drug classAntineoplastic
ATC code
Legal status
Legal status
Identifiers
  • 6-[(6,7-dimethoxyquinazolin-4-yl)oxy]-N,2-dimethyl-1-benzofuran-3-carboxamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC21H19N3O5
Molar mass393.399 g·mol−1
3D model (JSmol)
  • CNC(=O)C1=C(C)OC2=CC(OC3=NC=NC4=CC(OC)=C(OC)C=C34)=CC=C12
  • InChI=1S/C21H19N3O5/c1-11-19(20(25)22-2)13-6-5-12(7-16(13)28-11)29-21-14-8-17(26-3)18(27-4)9-15(14)23-10-24-21/h5-10H,1-4H3,(H,22,25)
  • Key:BALLNEJQLSTPIO-UHFFFAOYSA-N

Fruquintinib, sold under the brand name Fruzaqla, is an anti-cancer medication used for the treatment of colorectal cancer.[1] Fruquintinib is a kinase inhibitor.[1]

The most common adverse reactions include hypertension, palmar-plantar erythrodysesthesia, proteinuria, dysphonia, abdominal pain, diarrhea, and asthenia.[2]

Fruquintinib was approved for medical use in the United States in November 2023.[2][3]

Medical uses

Fruquintinib is indicated for adults with metastatic colorectal cancer who received prior fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if RAS wild-type and medically appropriate, an anti-EGFR therapy.[1][2][4][5]

History

Efficacy was evaluated in FRESCO-2 (NCT04322539) and FRESCO (NCT02314819).[2] FRESCO-2 (NCT04322539), an international, multicenter, randomized, double-blind, placebo-controlled trial, evaluated 691 participants with metastatic colorectal cancer who had disease progression during or after prior fluoropyrimidine-, oxaliplatin-, irinotecan-based chemotherapy, an anti-VEGF biological therapy an anti-EGFR biological therapy if RAS wild type, and at least one of trifluridine/tipiracil or regorafenib.[2] FRESCO, a multicenter, placebo-controlled trial conducted in China, evaluated 416 participants with metastatic colorectal cancer who had disease progression during or after prior fluoropyrimidine-, oxaliplatin, and irinotecan-based chemotherapy.[2]

References

  1. 1 2 3 4 "Fruzaqla- fruquintinib capsule". DailyMed. 14 November 2023. Archived from the original on 12 December 2023. Retrieved 12 December 2023.
  2. 1 2 3 4 5 6 "FDA approves fruquintinib in refractory metastatic colorectal cancer". U.S. Food and Drug Administration (FDA). 8 November 2023. Archived from the original on 10 November 2023. Retrieved 10 November 2023. Public Domain This article incorporates text from this source, which is in the public domain.
  3. ↑ "Takeda Receives U.S. FDA Approval of Fruzaqla (fruquintinib) for Previously Treated Metastatic Colorectal Cancer" (Press release). Takeda. 8 November 2023. Archived from the original on 8 November 2023. Retrieved 10 November 2023 – via Business Wire.
  4. ↑ Xu X, Yu Y, Liu M, Liang L, Liu T (January 2022). "Efficacy and safety of regorafenib and fruquintinib as third-line treatment for colorectal cancer: a narrative review". Translational Cancer Research. 11 (1): 276–287. doi:10.21037/tcr-20-3539. PMC 8841594. PMID 35261903.
  5. ↑ Lavacchi D, Roviello G, Guidolin A, Romano S, Venturini J, Caliman E, et al. (March 2023). "Evaluation of Fruquintinib in the Continuum of Care of Patients with Colorectal Cancer". International Journal of Molecular Sciences. 24 (6): 5840. doi:10.3390/ijms24065840. PMC 10051170. PMID 36982913.{{cite journal}}: CS1 maint: overridden setting (link)
  • Clinical trial number NCT04322539 for "A Study of Efficacy and Safety of Fruquintinib (HMPL-013) in Participants With Metastatic Colorectal Cancer (FRESCO-2)" at ClinicalTrials.gov
  • Clinical trial number NCT02314819 for "A Phase III Trial Evaluating Fruquintinib Efficacy and Safety in 3+ Line Colorectal Cancer participants （FRESCO) (FRESCO)" at ClinicalTrials.gov


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