The greater potency of oral atorvastatin in animals was confirmed in clinical trials where nearly 60% reductions of LDLc were achieved using an 80 mg dose of atorvastatin, substantially greater reductions than could be attained with the highest dose of other statins. Like the natural product-derived statins, orally administered atorvastatin has a relatively low overall bioavailability (~ 12%) in humans. Atorvastatin resembles lovastatin and simvastatin in being highly protein-bound (>95%), and is likewise metabolized by CYP3A4. Atorvastatin was approved for human use in 1997.

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