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.
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### 2. Mechanism of Action Fasudil inhibits Rho-kinase (ROCK), leading to several beneficial effects: ✅ Vasodilation: Reduces smooth muscle contractility, improving blood flow. ✅ Neuroprotection: Decreases apoptosis and promotes neuronal regeneration. ✅ Cytoskeletal modulation: Prevents fibrosis and pathological tissue stiffening. ✅ Anti-inflammatory effects: Reduces immune cell activation and oxidative stress.
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### 3. Clinical Indications
#### 3.1. Approved Uses (Japan & China) 🔹 Cerebral vasospasm after SAH → Approved in Japan & China. Improves cerebral perfusion and reduces secondary ischemia.
#### 3.2. Investigational Uses 🔹 Ischemic stroke → Potential neuroprotective and recovery-enhancing effects. 🔹 Pulmonary hypertension → Reduces pulmonary vascular resistance. 🔹 Neurodegenerative diseases (Parkinson’s, Alzheimer’s, ALS) → Anti-apoptotic and anti-inflammatory effects in experimental models. 🔹 Spinal cord injury & axonal regeneration → Inhibition of the RhoA-ROCK pathway promotes neuronal growth. 🔹 Glaucoma → Reduces intraocular pressure by improving aqueous humor drainage.
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### 4. Side Effects & Limitations ✅ Generally well-tolerated. 🚨 Possible adverse effects: - Hypotension - Nausea and vomiting - Headache - Rare liver enzyme elevation
📌 Limitations: - Intravenous administration, limiting outpatient use. - Not yet approved in the U.S. or Europe for broader indications.
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### 5. Future Perspectives 🔹 Development of oral formulations to enhance accessibility. 🔹 Clinical trials for neurodegenerative and fibrotic diseases. 🔹 Combination therapies to optimize effects in nerve injury and vascular diseases.
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### 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.
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