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The History of HIV Protease Inhibitors
By Mary Bellis

HIV protease inhibitors were first invented between 1989 and 1994 by researchers working for the pharmaceutical companies of Hoffmann- La Roche Inc. (of Nutley, New Jersey), Abbott Laboratories and Merck & Co., Inc. HIV protease inhibitors are used in the treatment of patients with AIDS and were considered the first breakthrough in over a decade of AIDS research. HIV protease inhibitors can lower the viral load carried by AIDS patents. 

Currently, there are five HIV protease inhibitors approved by FDA for the treatment of HIV infection. These medications work at the final stage of viral replication and attempt to prevent HIV from making new copies of itself by interfering with the HIV protease enzyme. As a result, the new copies of HIV are not able to infect new cells.1 The United States Food and Drug Administration (FDA) approved the new drugs in December, 1995 for Invirase; and March, 1996 for Norvir and Crixivan.

Hoffmann- La Roche Inc invented the first HIV protease inhibitor trade named Invirase (saquinavir) U.S. patent #5,196,438; the inventors were:

  • Joseph A. Martin
  • Sally Redshaw

Abbott Laboratories' inventors created the HIV protease inhibitor trade named Norvir (ritonavir) U.S. patent #5,541,206; and the inventors were:

  • Dale J. Kempf
  • Daniel W. Norbeck
  • Hing L. Sham
  • Chen Zhao

Abbott Laboratories who were also behind the invention of Pentothal, later invented a second HIV protease inhibitor trade named Kaletra.

Merck & Co.'s inventors created the HIV protease inhibitor trade named Crixivan (indinavir) U.S. patent #5,413,999; and the inventors were:

  • Joseph P. Vacca
  • Bruce D. Dorsey
  • James P. Guare
  • M. Katharine Holloway
  • Randall W. Hungate
  • Rhonda B. Levin

The HIV protease inhibitor Viracept (nelfinavir) developed by Agouron Pharmaceuticals (the pharmaceutical division of Japan Tobacco) under U.S. patent #5,484,926; and the inventors were:

  • Bruce A. Dressman
  • James E. Fritz
  • Marlys Hammond
  • William J. Thornback
  • Stephen W. Kaldor
  • Vincent J. Kalish
  • John E. Munroe
  • Siegfried H. Reich
  • John H. Tatlock
  • Timothy A. Shepherd
  • Michael J. Rodriguez

Agenerase (amprenavir) is marketed by Glaxo Wellcome, Inc (licensed from Vertex Phamaceuticals) U.S. patent #5,585,397. Agenerase was invented by:

  • Roger D. Tung
  • Mark A.  Murcko
  • Govinda R. Bhisetti

Related Innovations
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HIV Protease Inhibitors

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