Synthesis of tenofovir
Síntesis del tenofovir
- Date
- 1984-1985 · confidence medium
- Place
- Institute of Organic Chemistry and Biochemistry, Prague, Czechoslovakia (present-day Czech Republic)
- Credited to
- Antonín Holý, with Erik De Clercq for its anti-HIV activity
- Field
- Life & health
What was discovered
Czech chemist Antonín Holý synthesized the compound PMPA (tenofovir) in Prague and, together with Belgian virologist Erik De Clercq, described its anti-HIV activity in cell culture in 1985; since the original phosphonic acid was poorly absorbed orally, Gilead later developed the tenofovir disoproxil prodrug, approved in 2001.
The original 1986 patent application makes no mention of HIV: it claims activity against herpes simplex. The oral, marketable compound, tenofovir disoproxil fumarate, is a later achievement of Gilead Sciences in collaboration with the University of California, San Francisco.
What it led to
- Tenofovir disoproxil, the oral prodrug approved in 2001
- Once-daily combination antiretroviral therapy
- Preventive use (pre-exposure prophylaxis, PrEP) against HIV