Fact Sheet Number 401
- 1. REVERSE TRANSCRIPTASE INHIBITORS
(NUKES)
- 2. NON-NUCLEOSIDE REVERSE TRANSCRIPTASE
INHIBITORS (NNRTIs)
- 3. PROTEASE INHIBITORS
- 4. INTEGRASE INHIBITORS
- 5. ATTACHMENT AND FUSION INHIBITORS
- 6. ANTISENSE DRUGS
- 7. IMMUNE STIMULATORS
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PrintNone of these drugs can kill the HIV virus, but each class
slows down the multiplication of the virus (replication) in a
particular way.
INHIBITORS (NUKES)
The first anti-HIV drugs. They block reverse transcription
(the creation of viral DNA from RNA) by providing “decoy”
building blocks that interrupt the process. Most are nucleoside
analogs; tenofovir is a nucleotide analog.
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1987 |
Zidovudine |
Retrovir® |
AZT, ZDV |
GlaxoSmithKline |
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1991 |
Didanosine |
Videx® |
ddI |
Bristol-Myers Squibb |
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1992 |
Zalcitabine |
Hivid® |
ddC, dideoxycytidine |
Roche |
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1994 |
Stavudine |
Zerit® |
d4T |
Bristol-Myers Squibb |
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1995 |
Lamivudine |
Epivir® |
3TC |
GlaxoSmithKline |
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1997 |
Zidovudine/ Lamivudine |
Combivir® |
Combines AZT and 3TC |
GlaxoSmithKline |
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1998 |
Abacavir |
Ziagen® |
1592U89 |
GlaxoSmithKline |
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2000 |
Zidovudine/Lamivudine/Abacavir |
Trizivir® |
Combines AZT, 3TC, Abacavir |
GlaxoSmithKline |
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2001 |
Tenofovir |
Viread® |
bis-poc PMPA |
Gilead Sciences |
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Other nukes in human trials: ACH-126,443 (Beta-L-Fd4C) by Achillion Pharmaceuticals, Coviracil® (FTC, emtricitabine) and DAPD (amdoxovir) by Triangle Pharmaceuticals, and MIV-310 by Medivir. |
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REVERSE TRANSCRIPTASE INHIBITORS (NNRTIs or NON-NUKES)
These also interrupt reverse transcription, by binding to the
reverse transcriptase enzyme and restricting its activity.
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1996 |
Nevirapine |
Viramune® |
NVP, BI-RG-587 |
Boehringer Ingelheim |
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1997 |
Delavirdine |
Rescriptor® |
DLV |
Agouron Pharmaceuticals |
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1998 |
Efavirenz |
Sustiva® |
EFV, DMP-266 |
Bristol-Myers Squibb |
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Other NNRTI’s in human trials: +/-Calanolide A by Sarawak MediChem Pharmaceuticals, Capravirine (AG1549) by Agouron Pharmaceuticals, DPC083 by Bristol-Myers Squibb, MIV-150 by Medivir and TMC120 and TMC125 by Tibotec Virco. |
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Block the action of protease, an enzyme that cuts HIV protein
chains into specific proteins needed to assemble a new copy of
the virus.
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1995 |
Saquinavir |
Invirase® |
SQV |
Roche |
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1996 |
Ritonavir |
Norvir® |
RTV |
Abbott |
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1996 |
Indinavir |
Crixivan® |
IDV |
Merck |
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1997 |
Nelfinavir |
Viracept® |
NFV |
Agouron |
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1997 |
Saquinavir |
Fortovase® |
SQV |
Roche |
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1999 |
Amprenavir |
Agenerase® |
APV, 141W94 |
GlaxoSmithKline |
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2000 |
Lopinavir |
Kaletra® |
ABT-378/r |
Abbott |
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Other PIs in human trials: Atazanavir® (BMS 232632) by Bristol-Myers Squibb, GW433908 by GlaxoSmithKline, L-756,423 by Merck, Mozenavir (DMP-450) by Triangle Pharmaceuticals, Tipranavir® by Boehringer Ingelheim and TMC114 by Tibotec Virco. |
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Block the action of integrase, an enzyme that inserts the viral
DNA into the infected cell’s DNA strands. S-1360 by Shionogi Pharmaceuticals
and GlaxoSmithKline is currently in Phase II human trials.
AND FUSION INHIBITORS
No fusion inhibitors have been approved yet. Several are in human
trials: FP21399 by Fuji Pharmaceuticals, PRO 452 by Progenics
Pharmaceuticals, Inc. (Phase I/II trials), SCH-C by Schering,
Trimeris and Roche’s T-20 (enfuvirtide, Fuzeon®, Phase III
trials) and T-1249 (Phase I trials), and TNX-355 by Tanox
These are a “mirror image” of part of the HIV genetic
code that locks onto the virus to prevent it from functioning.
One antisense drug, HGTV43 by Enzo Therapeutics, is in Phase I
trials.
Use the body’s chemical messengers to stimulate the immune response.
Interleukin 2 (Il-2, Aldesleukin®, Proleukin®) by Chiron
Corporation is in Phase III trials, Multikine by Cel-Sci Corporation
is in Phase I trials, and Reticulose by Advance Viral Research
Corporation is in Phase III trials. Trials of Remune®, an
inactivated virus preparation by Immune Response Corporation,
were halted in 2001. HRG214 by Virionyx is in a Phase I trial,
and resveratrol, a plant chemical, is also in a Phase I trial.
Revised August 5, 2002
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