What is Anlotinib Dihydrochloride used for?

14 June 2024
Introduction to Anlotinib Dihydrochloride:
Anlotinib Dihydrochloride, known by its trade name "FocusV," is a potent multi-target tyrosine kinase inhibitor primarily developed by Advenchen Laboratories in collaboration with Chi-Med. This innovative drug belongs to a category of targeted therapies designed to impede cancer proliferation by blocking specific molecular pathways essential for tumor growth and survival. Anlotinib targets a broad spectrum of receptor tyrosine kinases, including VEGFR, FGFR, PDGFR, and c-Kit, which are implicated in various malignancies.

Initially approved in China for the treatment of non-small cell lung cancer (NSCLC) after other treatments have failed, Anlotinib has shown promising efficacy in clinical trials for a range of other cancers, including soft tissue sarcoma, renal cell carcinoma, and medullary thyroid carcinoma. Research institutions worldwide are currently exploring its potential applications across different cancer types, aiming to expand its therapeutic indications.

Anlotinib Dihydrochloride Mechanism of Action:
Anlotinib Dihydrochloride operates through a multi-faceted mechanism of action, blocking the activity of several receptor tyrosine kinases (RTKs) that play crucial roles in tumor angiogenesis and growth. Specifically, it inhibits vascular endothelial growth factor receptors (VEGFR-2 and VEGFR-3), fibroblast growth factor receptors (FGFR-1, FGFR-2, and FGFR-3), platelet-derived growth factor receptors (PDGFR-α and PDGFR-β), and the stem cell factor receptor c-Kit. By targeting these kinases, Anlotinib disrupts critical signaling pathways that tumors exploit to sustain angiogenesis (the formation of new blood vessels), cellular proliferation, and metastasis.

The inhibition of VEGFR-2 and VEGFR-3 curtails angiogenesis, effectively starving the tumor of the nutrients and oxygen it requires to grow. Meanwhile, the blockade of FGFRs and PDGFRs impedes tumor cell proliferation and survival. Additionally, by inhibiting c-Kit, Anlotinib disrupts the tumor microenvironment, further dampening cancer progression. The multifaceted action of Anlotinib makes it a formidable opponent of cancer, targeting the disease from multiple angles to maximize therapeutic efficacy.

How to Use Anlotinib Dihydrochloride:
Anlotinib Dihydrochloride is administered orally, usually in the form of capsules. The recommended dosage and treatment schedule may vary based on the specific type of cancer being treated and the patient's overall health condition. Generally, the standard dosage for adults is 12 mg taken once daily for two consecutive weeks, followed by a one-week rest period (known as a 2/1 schedule). This cycle is repeated until there is evidence of disease progression or unacceptable toxicity.

The onset of action for Anlotinib can vary; however, patients may start experiencing clinical benefits within a few weeks of initiating treatment. It is crucial to adhere strictly to the prescribed dosage and schedule to maximize the drug's efficacy and minimize potential side effects. Patients are also advised to take the medication at the same time each day, with or without food, to maintain consistent drug levels in the body.

What is Anlotinib Dihydrochloride Side Effects:
Like all medications, Anlotinib Dihydrochloride can cause side effects, ranging from mild to severe. Common side effects include hypertension (high blood pressure), hand-foot syndrome, fatigue, diarrhea, nausea, anorexia, and proteinuria. These side effects are generally manageable with supportive care and dose adjustments.

More severe side effects, although less common, can include bleeding, cardiac issues such as myocardial infarction, and thromboembolic events. Due to these risks, Anlotinib is contraindicated in patients with a history of severe cardiovascular diseases, uncontrolled hypertension, or those who have experienced recent major bleeding episodes.

Patients taking Anlotinib should be closely monitored for any signs of adverse effects, and routine blood tests are often recommended to assess liver and kidney function, as well as blood cell counts. In case of severe side effects, the treating physician may decide to modify the dosage or discontinue the drug temporarily or permanently.

What Other Drugs Will Affect Anlotinib Dihydrochloride:
Anlotinib Dihydrochloride can interact with other medications, which may affect its efficacy or increase the risk of adverse effects. For instance, drugs that inhibit or induce cytochrome P450 enzymes, particularly CYP3A4, can alter the metabolism of Anlotinib. CYP3A4 inducers such as rifampin, phenytoin, and St. John's Wort can decrease Anlotinib levels, potentially reducing its efficacy. Conversely, CYP3A4 inhibitors like ketoconazole, itraconazole, and grapefruit juice can increase Anlotinib levels, heightening the risk of toxicity.

Patients should inform their healthcare providers of all medications they are currently taking, including over-the-counter drugs, supplements, and herbal products, to avoid potential drug interactions. Additionally, Anlotinib may enhance the effects of antihypertensive drugs, requiring close monitoring and possible adjustment of antihypertensive therapy.

In conclusion, Anlotinib Dihydrochloride is a promising multi-target tyrosine kinase inhibitor with broad applications in oncology. Its ability to disrupt multiple pathways essential for tumor growth and angiogenesis makes it a valuable therapeutic option for various cancers. However, like all potent medications, it must be used with caution and under the guidance of a healthcare professional to manage its side effects and potential drug interactions effectively. Ongoing research continues to explore the full potential of Anlotinib, offering hope for improved cancer treatment outcomes in the future.

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