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Brand Name :
N/A
Synonyms :
fruquintinib
Class :
Antineoplastics VEGF inhibitors
Brand Name :
N/A
Synonyms :
fruquintinib
Class :
Antineoplastics VEGF inhibitors
Actions and Spectrum
Action:
Inhibition of Vascular Endothelial Growth Factor Receptors (VEGFR): The drug effectively blocks VEGFR-1, VEGFR-2, and VEGFR-3, which play a crucial role in angiogenesis – the process of new blood vessel formation. By blocking these receptors, fruquintinib can impede tumor angiogenesis, thereby inhibiting the blood supply to the tumor and reducing its growth.
Inhibition of Platelet-Derived Growth Factor Receptors (PDGFR): The drug also inhibits PDGFR-α and PDGFR-β, which are involved in the growth and survival of cancer cells. By targeting these receptors, fruquintinib can interfere with signaling pathways that promote tumor cell proliferation and migration.
Spectrum: The medication has undergone extensive research and received authorization specifically for addressing advanced colorectal cancer. It is administered alongside or subsequent to conventional chemotherapy protocols. Colorectal cancer pertains to malignancies originating in the colon or rectum, and fruquintinib has exhibited positive outcomes in terms of extending overall survival and progression-free survival rates among patients with advanced stages of the disease.
Frequency not defined
Black Box Warning:
None
Contraindication/Caution:
Hypersensitivity: Patients who are allergic or hypersensitive to this medication or any of its ingredients should refrain from using this drug.
Severe liver impairment: The drug is primarily metabolized in the liver, and severe liver impairment can affect its clearance and increase the risk of adverse effects.
Pregnancy and breastfeeding: The drug use is generally not recommended during pregnancy. Additionally, it is unknown whether fruquintinib is excreted in human breast milk, so breastfeeding should be avoided during treatment.
Concurrent use of strong CYP3A4 inhibitors or inducers: Metabolism of the drug occurs through the liver enzyme CYP3A4. When taken simultaneously with potent inhibitors (medications that hinder the enzyme’s function) or potent inducers (medications that enhance the enzyme’s activity) of CYP3A4, the levels of fruquintinib in the body may be affected. This alteration can result in diminished effectiveness or enhanced toxicity.
Pregnancy warnings:
Pregnancy category: N/A
Lactation: Excreted into human milk is unknown
Pregnancy Categories:
Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.
Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology:
fruquintinib is a small molecule tyrosine kinase inhibitor (TKI) that belongs to a class of anti-cancer drugs.
Pharmacodynamics:
The drug selectively binds to and inhibits the tyrosine kinase activity of VEGFR-1, VEGFR-2, and VEGFR-3. By blocking the signaling pathways activated by these receptors, fruquintinib inhibits the growth of new blood vessels that supply nutrients and oxygen to tumors, thereby restricting tumor growth and metastasis.
Pharmacokinetics:
Absorption
The drug is well-absorbed after oral administration. The exact bioavailability (the fraction of the administered dose that reaches systemic circulation) of fruquintinib is not readily available in the public domain.
Distribution
The drug has a moderate volume of distribution, indicating that it distributes well throughout the body. Protein binding studies indicate that it is highly bound to plasma proteins, primarily albumin.
Metabolism
The metabolism of the drug takes place in the liver.through the cytochrome P450 enzyme system, specifically CYP1A2 and CYP3A4. The primary metabolic pathways involve oxidation and glucuronidation. The major metabolites formed are less active than the parent drug.
Excretion and Elimination
The drug and its metabolites are primarily eliminated through the feces, with a small portion excreted in the urine.
Administration:
fruquintinib is available in the form of oral tablets.
The specific dosage and administration schedule will depend the stage of cancer, and the treating physician’s recommendations.
The drug is taken orally once a day, with or without food.
Patient information leaflet
Generic Name: fruquintinib
Why do we use fruquintinib?
Colorectal cancer: It is commonly prescribed in patients who have already received previous chemotherapy or targeted therapy options.
Gastric or gastroesophageal junction cancer:
It is typically prescribed as a later-line treatment option when other therapies have not been effective.
Targeted therapy: This targeted approach helps to block the signals that promote tumor growth and can improve treatment outcomes.
Maintenance therapy: In certain situations, the drug could be employed as a form of maintenance therapy for individuals who have exhibited positive responses to their initial course of chemotherapy or targeted therapy. It can help to prolong the period of remission and delay disease progression.
Monotherapy or combination therapy: The drug can be used as a single-agent treatment or in combination with other chemotherapy drugs or targeted therapies.The choice of treatment approach is determined by the healthcare provider based on individual patient factors.
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