424
Table 18.2 Chronological discovery of anti-HIV drugs by class
a
Class
Generic name
Role/function
Side effects
FDA approval date
Entry inhibitor
Maraviroc
Allosteric modulator of CCR5
Liver problems, skin reactions
August 6, 2007
Fusion inhibitor Enfuvirtide
gp41binding
Insomnia, depression, anorexia
March 13, 2003
NRTI
b
Zidovudine
NTP
c
mimic
Anemia, myopathy, neutropenia
March 19, 1987
NRTI
b
Didanosine
NTP
c
mimic
Diarrhea, nausea, vomiting,
abdominal pain
October 9, 1991
NRTI
b
Stavudine
NTP
c
mimic
Headache, dizziness, abnormal
thinking
June 24, 1994
NRTI
b
Lamivudine
NTP
c
mimic
Headache, nausea, fatigue
November 17, 1995
NRTI
b
Abacavir
NTP
c
mimic
Nausea, headache, fatigue, vomiting December 17, 1998
NRTI
b
Tenofovirdisoproxilfumerate NTP
c
mimic
Diarrhea, nausea, vomiting,
October 26, 2001
NRTI
b
Emtricitabine
NTP mimic
Diarrhea, nausea,
July 2, 2003
NNRTI
d
Nevirapine
Binding to RT and blocking DNA- and
RNA-dependent polymerase activity
Moderate rash
June 21, 1996
NNRTI
d
Delavirdine
Blocking RT catalytic site
Rash, fatigue, nausea
April 4, 1997
NNRTI
d
Efavirenz
Inhibiting viral DNA polymerase activity Insomnia, confusion, memory loss
September 17, 1998
NNRTI
d
Etravirine
Binding to RT and blocking DNA and
RNA dependent polymerase activity
Skin rash and allergic reactions
January 18, 2008
NNRTI
c
Rilpivirine
Binding to RT and blocking DNA and
RNA dependent polymerase activity
Depression, headache, insomnia
May 20, 2011
Integrase
inhibitor
Dolutegravir
Integrase-DNA complex binding
Insomnia and headache
August 13, 2003
Integrase
inhibitor
Raltegravir
Integrase-DNA binding inhibition
Headache. Stomach pain,
October 12, 2007
Integrase
inhibitor
Elvitegravir
Integrase-DNA binding inhibition
Diarrhea
September 24, 2014
Protease
inhibitors
Saquinavir
Enzyme active site binding
Diarrhea, nausea
December 6, 1995
N. Ranjan et al.