Emivirine
Overview of the antiretroviral drug Emivirine
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Emivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that was investigated for the treatment of HIV/AIDS. Although it showed promise in early studies, it was never marketed.
Mechanism of Action
Emivirine works by inhibiting the activity of reverse transcriptase, an enzyme crucial for the replication of HIV. By binding to the reverse transcriptase enzyme, emivirine prevents the conversion of viral RNA into DNA, thereby halting the replication process of the virus within the host cells.
Development and Clinical Trials
Emivirine was developed in the 1990s and underwent several clinical trials to assess its efficacy and safety in treating HIV infection. Despite initial positive results, further studies revealed limitations in its effectiveness compared to other available NNRTIs, leading to the discontinuation of its development.
Pharmacokinetics
The pharmacokinetic profile of emivirine includes its absorption, distribution, metabolism, and excretion. Emivirine is orally bioavailable and is metabolized primarily in the liver. The drug's half-life and clearance rates were studied to optimize dosing regimens during its clinical evaluation.
Side Effects
Like other NNRTIs, emivirine was associated with certain side effects. Common adverse effects included rash, nausea, and headache. More severe side effects were rare but included hepatotoxicity and hypersensitivity reactions.
Comparison with Other NNRTIs
Emivirine was compared with other NNRTIs such as efavirenz, nevirapine, and delavirdine. While it shared a similar mechanism of action, emivirine did not demonstrate superior efficacy or safety, which contributed to its lack of approval for clinical use.
Current Status
As of now, emivirine is not used in clinical practice and is not available on the market. Research and development efforts have shifted towards other antiretroviral agents with better efficacy and safety profiles.
Related pages
Emivirine
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Contributors: Prab R. Tumpati, MD