Emerging anti-HIV drugs.

Article Details

Citation

De Clercq E

Emerging anti-HIV drugs.

Expert Opin Emerg Drugs. 2005 May;10(2):241-73.

PubMed ID
15934866 [ View in PubMed
]
Abstract

There are now exactly 20 anti-HIV drugs licenced (approved) for clinical use, and > 30 anti-HIV compounds under (pre)clinical development. The licensed anti-HIV drugs fall into five categories: nucleoside reverse transcriptase inhibitors (NRTIs: zidovudine, didanosine, zalcitabine, stavudine, lamivudine, abacavir and emtricitabine); nucleotide reverse transcriptase inhibitors (NtRTIs: tenofovir disoproxil fumarate); non-nucleoside reverse transcriptase inhibitors (NNRTIs: nevirapine, delavirdine and efavirenz); protease inhibitors (PIs: saquinavir, indinavir, ritonavir, nelfinavir, amprenavir, lopinavir, atazanavir and fosamprenavir); and fusion inhibitors (FIs: enfuvirtide). The compounds that are currently under clinical (Phase I, II or III) or preclinical investigation are either targeted at the same specific viral proteins as the licensed compounds (i.e., reverse transcriptase [NRTIs: PSI-5004, (-)-dOTC, DPC-817, elvucitabine, alovudine, MIV-210, amdoxovir, DOT; NNRTIs: thiocarboxanilide, UC-781, capravirine, dapivirine, etravirine, rilpivirine], protease [PIs: tipranavir, TMC-114]) or other specific viral proteins (i.e., gp120: cyanovirin N; attachment inhibitors: AIs, such as BMS-488043; integrase: L-870,812, PDPV-165; capsid proteins: PA-457, alpha-HCG); or cellular proteins (CD4 downmodulators: CADAs; CXCR4 antagonists: AMD-070, CS-3955; CCR5 antagonists: TAK-220, SCH-D, AK-602, UK-427857). Combination therapy is likely to remain the gold standard for the treatment of AIDS so as to maximise potency, minimise toxicity and diminish the risk for resistance development. Ideally, pill burden should be reduced to once-daily dosing so as to optimise the patient's compliance and reduce the treatment costs.

DrugBank Data that Cites this Article

Drugs
Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
AlovudineReverse transcriptase/RNaseHProteinHuman immunodeficiency virus 1
Unknown
Inhibitor
Details
AMD-070C-X-C chemokine receptor type 4ProteinHumans
Unknown
Antagonist
Inhibitor
Details
AmdoxovirReverse transcriptase/RNaseHProteinHuman immunodeficiency virus 1
Unknown
Inhibitor
Details
AplavirocC-C chemokine receptor type 5ProteinHumans
Unknown
Antagonist
Details
CapravirineReverse transcriptase/RNaseHProteinHuman immunodeficiency virus 1
Unknown
Inhibitor
Details
DexelvucitabineReverse transcriptase/RNaseHProteinHuman immunodeficiency virus 1
Unknown
Inhibitor
Details
DidanosineReverse transcriptase/RNaseHProteinHuman immunodeficiency virus 1
Yes
Inhibitor
Details
ElvucitabineReverse transcriptase/RNaseHProteinHuman immunodeficiency virus 1
Unknown
Inhibitor
Details
EtravirineReverse transcriptase/RNaseHProteinHuman immunodeficiency virus 1
Unknown
Inhibitor
Details
LamivudineReverse transcriptase/RNaseHProteinHuman immunodeficiency virus 1
Yes
Inhibitor
Details
NelfinavirHIV-1 proteaseProteinHuman Immunodeficiency Virus
Yes
Inhibitor
Details
RacivirReverse transcriptase/RNaseHProteinHuman immunodeficiency virus 1
Unknown
Inhibitor
Details
RilpivirineReverse transcriptase/RNaseHProteinHuman immunodeficiency virus 1
Yes
Inhibitor
Details
StavudineReverse transcriptase/RNaseHProteinHuman immunodeficiency virus 1
Yes
Inhibitor
Details
VicrivirocC-C chemokine receptor type 5ProteinHumans
Unknown
Antagonist
Details
ZalcitabineReverse transcriptase/RNaseHProteinHuman immunodeficiency virus 1
Yes
Inhibitor
Details
ZidovudineReverse transcriptase/RNaseHProteinHuman immunodeficiency virus 1
Yes
Inhibitor
Details