TMC-310911

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TMC-310911 (also known as ASC-09) is an antiretroviral drug in the protease inhibitor class. It was developed by Tibotec, a subsidiary of Johnson & Johnson, for the treatment of HIV infection.

Development and Mechanism

TMC-310911 was first synthesized in 2005 as part of a program to develop new protease inhibitors with improved resistance profiles. It is a non-peptidic protease inhibitor, meaning it does not mimic the natural substrates of the HIV protease enzyme. This gives it a unique resistance profile compared to other protease inhibitors.

The drug works by binding to the HIV-1 protease enzyme, preventing it from cleaving the viral polyprotein into individual functional proteins. This stops the production of new virus particles.

Clinical Trials

TMC-310911 has undergone Phase I and II clinical trials. In Phase I trials, it was found to be well-tolerated and to have a favorable pharmacokinetic profile. Phase II trials showed that it had potent antiretroviral activity, with a significant reduction in viral load seen in patients with HIV.

Future Prospects

While TMC-310911 has shown promise in early-stage clinical trials, further development has been halted. This is due to the development of other, more effective antiretroviral drugs. However, it remains a potential option for future drug development, particularly for patients with resistance to current protease inhibitors.

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