====== Fasudil ====== ===== Mechanism, Clinical Uses, and Therapeutic Potential ===== #### **1. What is Fasudil?** Fasudil is a **selective [[ROCK inhibitor]]**, an enzyme involved in cytoskeletal regulation, smooth muscle contractility, and vascular function. Initially developed for treating **cerebral vasospasm** after subarachnoid hemorrhage (SAH), it has shown potential for various **neurological and cardiovascular** conditions. --- ### **2. Mechanism of Action** Fasudil inhibits **Rho-kinase (ROCK)**, leading to several beneficial effects: โœ… **Vasodilation:** Reduces smooth muscle contractility, improving blood flow. โœ… **Neuroprotection:** Decreases apoptosis and promotes neuronal regeneration. โœ… **Cytoskeletal modulation:** Prevents fibrosis and pathological tissue stiffening. โœ… **Anti-inflammatory effects:** Reduces immune cell activation and oxidative stress. --- ### **3. Clinical Indications** #### **3.1. Approved Uses (Japan & China)** ๐Ÿ”น **Cerebral vasospasm after SAH** โ†’ Approved in Japan & China. Improves cerebral perfusion and reduces secondary ischemia. #### **3.2. Investigational Uses** ๐Ÿ”น **Ischemic stroke** โ†’ Potential neuroprotective and recovery-enhancing effects. ๐Ÿ”น **Pulmonary hypertension** โ†’ Reduces pulmonary vascular resistance. ๐Ÿ”น **Neurodegenerative diseases (Parkinsonโ€™s, Alzheimerโ€™s, ALS)** โ†’ Anti-apoptotic and anti-inflammatory effects in experimental models. ๐Ÿ”น **Spinal cord injury & axonal regeneration** โ†’ Inhibition of the RhoA-ROCK pathway promotes neuronal growth. ๐Ÿ”น **Glaucoma** โ†’ Reduces intraocular pressure by improving aqueous humor drainage. --- ### **4. Side Effects & Limitations** โœ… Generally well-tolerated. ๐Ÿšจ **Possible adverse effects:** - Hypotension - Nausea and vomiting - Headache - Rare liver enzyme elevation ๐Ÿ“Œ **Limitations:** - **Intravenous administration**, limiting outpatient use. - **Not yet approved** in the U.S. or Europe for broader indications. --- ### **5. Future Perspectives** ๐Ÿ”น **Development of oral formulations** to enhance accessibility. ๐Ÿ”น **Clinical trials for neurodegenerative and fibrotic diseases.** ๐Ÿ”น **Combination therapies** to optimize effects in nerve injury and vascular diseases. --- ### **6. Conclusion** Fasudil is a promising drug with **vasodilatory, neuroprotective, and anti-inflammatory** properties. While currently approved mainly in Asia for **cerebral vasospasm**, its potential applications in **neuroprotection, pulmonary hypertension, and nerve regeneration** make it a key candidate for future therapeutic advancements. ๐Ÿ“Œ Would you like more details on recent studies or its mechanism in a specific disease?