Difference between revisions of "Fruquintinib (Elunate)"

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==Mechanism of action==
 
==Mechanism of action==
VEGFR inhibitor
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From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/fruquintinib NCI Drug Dictionary]: An orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential anti-angiogenic and antineoplastic activities. Upon oral administration, fruquintinib inhibits VEGF-induced phosphorylation of VEGFRs 1, 2, and 3 which may result in the inhibition of migration, proliferation and survival of endothelial cells, microvessel formation, the inhibition of tumor cell proliferation, and tumor cell death.
  
==Preliminary data==
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==Diseases for which it is established==
===[[Colorectal cancer]]===
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*[[Colorectal cancer]]
#'''FRESCO:''' Li J, Qin S, Xu RH, Shen L, Xu J, Bai Y, Yang L, Deng Y, Chen ZD, Zhong H, Pan H, Guo W, Shu Y, Yuan Y, Zhou J, Xu N, Liu T, Ma D, Wu C, Cheng Y, Chen D, Li W, Sun S, Yu Z, Cao P, Chen H, Wang J, Wang S, Wang H, Fan S, Hua Y, Su W. Effect of fruquintinib vs placebo on overall survival in patients with previously treated metastatic colorectal cancer: the FRESCO randomized clinical trial. JAMA. 2018 Jun 26;319(24):2486-2496. [https://jamanetwork.com/journals/jama/fullarticle/2685988 link to original article] [https://pubmed.ncbi.nlm.nih.gov/29946728/ PubMed] [https://clinicaltrials.gov/study/NCT02314819 NCT02314819]
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#'''FRESCO-2:''' Dasari A, Lonardi S, Garcia-Carbonero R, Elez E, Yoshino T, Sobrero A, Yao J, García-Alfonso P, Kocsis J, Cubillo Gracian A, Sartore-Bianchi A, Satoh T, Randrian V, Tomasek J, Chong G, Paulson AS, Masuishi T, Jones J, Csőszi T, Cremolini C, Ghiringhelli F, Shergill A, Hochster HS, Krauss J, Bassam A, Ducreux M, Elme A, Faugeras L, Kasper S, Van Cutsem E, Arnold D, Nanda S, Yang Z, Schelman WR, Kania M, Tabernero J, Eng C; FRESCO-2 Study Investigators. Fruquintinib versus placebo in patients with refractory metastatic colorectal cancer (FRESCO-2): an international, multicentre, randomised, double-blind, phase 3 study. Lancet. 2023 Jul 1;402(10395):41-53. Epub 2023 Jun 15. [https://doi.org/10.1016/s0140-6736(23)00772-9 link to original article] [https://pubmed.ncbi.nlm.nih.gov/37331369/ PubMed] [https://clinicaltrials.gov/study/NCT04322539 NCT04322539]
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==History of changes in FDA indication==
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*2023-11-08: Approved for adult patients with metastatic [[colorectal cancer]] (mCRC) 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. ''(Based on FRESCO & FRESCO-2)''
  
 
==History of changes in NMPA indication==
 
==History of changes in NMPA indication==
*2018-09: Approved for the treatment of patients with metastatic [[colorectal cancer]] (“CRC”) who have been previously treated with fluoropyrimidine, oxaliplatin and irinotecan, including those who have previously received anti-VEGF therapy and/or anti-epidermal growth factor receptor (EGFR) therapy (RAS wild type). ''(Based on FRESCO)''
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*2018-09: Approved for the treatment of patients with metastatic [[colorectal cancer|colorectal cancer (CRC)]] who have been previously treated with fluoropyrimidine, oxaliplatin and irinotecan, including those who have previously received anti-VEGF therapy and/or anti-epidermal growth factor receptor (EGFR) therapy (RAS wild type). ''(Based on FRESCO)''
  
 
==Also known as==
 
==Also known as==
 
*'''Code name:''' HMPL-013
 
*'''Code name:''' HMPL-013
*'''Brand name:''' Elunate
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*'''Brand names:''' Elunate, Fruzaqla
  
 
[[Category:Drugs]]
 
[[Category:Drugs]]
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[[Category:Colorectal cancer medications]]
 
[[Category:Colorectal cancer medications]]
 
[[Category:NMPA approved in 2018]]
 
[[Category:NMPA approved in 2018]]
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[[Category:FDA approved in 2023]]
 
[[Category:Stub]]
 
[[Category:Stub]]

Latest revision as of 13:33, 9 November 2023

Mechanism of action

From the NCI Drug Dictionary: An orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential anti-angiogenic and antineoplastic activities. Upon oral administration, fruquintinib inhibits VEGF-induced phosphorylation of VEGFRs 1, 2, and 3 which may result in the inhibition of migration, proliferation and survival of endothelial cells, microvessel formation, the inhibition of tumor cell proliferation, and tumor cell death.

Diseases for which it is established

History of changes in FDA indication

  • 2023-11-08: Approved for adult patients with metastatic colorectal cancer (mCRC) 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. (Based on FRESCO & FRESCO-2)

History of changes in NMPA indication

  • 2018-09: Approved for the treatment of patients with metastatic colorectal cancer (CRC) who have been previously treated with fluoropyrimidine, oxaliplatin and irinotecan, including those who have previously received anti-VEGF therapy and/or anti-epidermal growth factor receptor (EGFR) therapy (RAS wild type). (Based on FRESCO)

Also known as

  • Code name: HMPL-013
  • Brand names: Elunate, Fruzaqla