- Etat: unused FDC
- Année: 2016-09-07
07Prof. RNDr. Antonín Holý working with a measuring cylinder and a conical flask, with an enlarged image of the human immunodeficiency virus in the background.
Antonín Holý (1 September 1936 - 16 July 2012) was a pioneering Czech scientist of the 20th century. He specialised in the field of chemistry and cooperated on the development of important antiretroviral drugs used in the treatment of HIV and hepatitis B.
From 1954-59, he studied organic chemistry at the Faculty of Science, Charles University in Prague. From 1960, he trained at the Institute of Organic Chemistry and Biochemistry (IOCB) of the Czechoslovak Academy of Sciences in Prague and has been a researcher there since 1963. He became the Institute’s lead scientist in 1967, and from 1983 headed its working group for nucleic acids. In 1987, he became chief of the Department of Nucleic Acid Chemistry and from 1994 to 2002 he was head of the IOCB. He habilitated at the Faculty of Science, Palacký University in Olomouc in 2004 after publishing his dissertation “Acyclic nucleosides: ideas and reality”, and was appointed professor of organic chemistry at Palacký University in 2005.
From 1976, he collaborated on the development of new antiretroviral drugs with Erik De Clercq of the Rega Institute for Medical Research at the Catholic University of Leuven, Belgium, who is the co-author of Holý’s 15 patents. The Web of Science results for Holý’s publications is 604 publications, 11,609 citations and an h-index of 49. Holý was also the author or co-author of 60 Czech and international patents.
The first drug developed by Holý’s team at the IOCB and the pharmaceutical company Léčiva was Duviragel for oral herpes. Czechoslovak and European pharmaceutical companies considered the development of drugs from the substances synthetised by Holý’s team as too expensive and time-consuming and were not willing to participate. The development was eventually started by the American pharmaceutical company Bristol-Myers, but was discontinued as unpromising.
In 1990, the patents were bought by a small American company Gilead Sciences with only 15 staff members, joined by some scientists from Bristol-Myers who considered Holý’s substances as promising. In 1996, cidofovir (brand name Vistide) was approved for production in the United States and European Union as a treatment for cytomegalovirus retinitis. It has also shown efficacy in the treatment of herpes zoster and smallpox. In 2001, tenofovir disoproxil, marketed as Viread, was approved by the U.S. Food and Drug Administration (FDA) for the treatment of HIV, and in 2008, for the treatment of hepatitis B. Adefovir (brand name Preveon) was another drug to be approved by the FDA for the treatment of HIV. In 1999, the FDA refused to approve it because of its serious adverse effects. Gilead Sciences continued to develop the drug for hepatitis B. The drug, marketed as Hepsera, was approved by the FDA in 2002. Tenofovir disoproxil/emtricitabine (brand name Truvada) is a fixed-dose combination of two antiretroviral drugs used for the treatment of HIV/AIDS (approved in 2004) and for the prevention of HIV infection (approved in 2012). Efavirenz/emtricitabine/tenofovir disoproxil, sold under the trade name Atripla among others, is a fixed-dose combination drug for the treatment of HIV infection, approved in 2006. Emtricitabine/rilpivirine/tenofovir (trade names Complera, Eviplera) is a fixed dose combination of antiretroviral drugs for the treatment of HIV, approved in 2011. Further drugs are being developed or clinically tested.
The IOCB has received almost CZK 2 billion a year from Gilead Sciences for licence fees and patents resulting from Antonín Holý and his team’s work. In 2006, Gilead Sciences and the IOCB jointly established a new research centre for the development of new preparations. Gilead Sciences promised the IOCB a $1.1 million donation, to fund its operations and research for 5 years. In 2011, the contract was extended by another five years.
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