- Overview
- Properties
- Genetics
- Related Genes
- Related Drugs
- Related Diseases
- Datasets
- Downloads/LinkOuts
Overview
| Generic Names: | ABC; abacavir |
|---|---|
| Trade Names: | Epzicom; Ziagen |
| Brand Mixtures: | Kivexa (Abacavir Sulfate + Lamivudine); Trizivir (Abacavir Sulfate + Lamivudine + Zidovudine) |
| PharmGKB Accession Id: | PA448004 |
Description
Abacavir (ABC) is the most powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS. Wikipedia (source: Drug Bank)
Indication
For the treatment of HIV-1 infection, in combination with other antiretroviral agents. (source: Drug Bank)
ATC Therapeutic Category
- J05AF:Nucleoside and nucleotide reverse transcriptase inhibitors
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Abacavir is a carbocyclic synthetic nucleoside analogue. Intracellularly, abacavir is converted by cellular enzymes to the active metabolite carbovir triphosphate, an analogue of deoxyguanosine-5'-triphosphate (dGTP). Carbovir triphosphate inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA. (source: Drug Bank)
Pharmacology
Abacavir is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Abacavir is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcriptase enzyme competitively and act as a chain terminator of DNA synthesis. The lack of a 3'-OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated. (source: Drug Bank)
Food Interactions
Abacavir is partly metabolised through the alcohol-dehydrogenase enzyme system.
Alcohol significantly increases abacavir's area under the curve (about 41%).
Avoid alcohol.
Take without regard to meals.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic, by alcohol dehydrogenase and glucuronosyltransferase to a 5′-carboxylic acid metabolite and 5′-glucuronide metabolite, respectively. These metabolites have no antiviral activity. Abacavir is not significantly metabolized by cytochrome P450 enzymes. (source: Drug Bank)
Protein Binding
Moderate (approximately 50%) (source: Drug Bank)
Absorption
Rapid and extensive after oral administration (83% bioavailability) (source: Drug Bank)
Toxicity
Some myocardial degeneration has been noticed in rats and mice (source: Drug Bank)
Isomeric SMILES Code:
C1CC1NC2=C3C(=NC(=N2)N)N(C=N3)[C@H]4C[C@H](C=C4)CO (source: Drug Bank)
Curated Annotations (
)
-
rs2395029
at chr6:31539759
in
HCP5
This variant is a tagging SNP for HLA-B*5701, which is associated with hypersensitivity to abacavir. This variant is also associated with low HIV viral load.- Variant Name:
- tagging SNP for HLA-B*5701
- Related Drugs:
- abacavir
- Related Diseases:
- HIV
- Evidence:
-
PMID:11888582
PMID:15247625
PMID:16998491
PMID:17641165
PMID:18256392
PMID:18536095
-
rs3093726
at chr6:31654768
in
LST1,
LTB,
TNF
This variant is a tagging SNP for HLA-B*5701, which is associated with hypersensitivity to abacavir.- Variant Name:
- tagging SNP for HLA-B*5701
- Related Drugs:
- abacavir
- Related Diseases:
- HIV
- Evidence:
-
PMID:11888582
PMID:15247625
PMID:16998491
PMID:18256392
PMID:18536095
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
ABCB1 |
|
Publications |
|
HCP5 |
|
Publications, Variants |
|
|
HLA-B |
|
Publications |
|
|
LST1 |
|
Variants |
|
|
LTB |
|
Variants |
|
|
TNF |
|
Variants |
A list of non-curated publications that mention this drug along with other genes is available.
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| amprenavir |
|
The serum concentration of Abacavir may be decreased by protease inhibitors such as Amprenavir. The antiviral response should be closely monitored. (source: Drug Bank) |
| atazanavir |
|
The serum concentration of Abacavir may be decreased by protease inhibitors such as Atazanavir. The antiviral response should be closely monitored. (source: Drug Bank) |
| darunavir |
|
The serum concentration of Abacavir may be decreased by protease inhibitors such as Darunavir. The antiviral response should be closely monitored. (source: Drug Bank) |
| ethanol |
|
Partly metabolized through the alcohol dehydrogenase enzyme system. Alcohol increases the area under the curve (about 41%) of Abacavir. (source: Drug Bank) |
| fosamprenavir |
|
The serum concentration of Abacavir may be decreased by protease inhibitors such as Fosamprenavir. The antiviral response should be closely monitored. (source: Drug Bank) |
| ganciclovir |
|
The adverse/toxic effects of reverse transcriptase inhibitors (nucleoside), such as Abacavir, may be enhanced by Ganciclovir. There is a risk of hematologic toxicity. Diligent monitoring during concomitant therapy is required. (source: Drug Bank) |
| indinavir |
|
The serum concentration of Abacavir may be decreased by protease inhibitors such as Indinavir. The antiviral response should be closely monitored. (source: Drug Bank) |
| lopinavir |
|
The serum concentration of Abacavir may be decreased by protease inhibitors such as Lopinavir. The antiviral response should be closely monitored. (source: Drug Bank) |
| nelfinavir |
|
The serum concentration of Abacavir may be decreased by protease inhibitors such as Nelfinavir. The antiviral response should be closely monitored. (source: Drug Bank) |
| ribavirin |
|
Ribavirin may increase the hepatotoxicity of reverse transcriptase inhibitors (nucleoside) such as Abacavir. Lactic acidosis may occur. Consider modifying therapy. (source: Drug Bank) |
| ritonavir |
|
The serum concentration of Abacavir may be decreased by protease inhibitors such as Ritonavir. The antiviral response should be closely monitored. (source: Drug Bank) |
| saquinavir |
|
The serum concentration of Abacavir may be decreased by protease inhibitors such as Saquinavir. The antiviral response should be closely monitored. (source: Drug Bank) |
| tipranavir |
|
The serum concentration of Abacavir may be decreased by protease inhibitors such as Tipranavir. The antiviral response should be closely monitored. (source: Drug Bank) |
| valganciclovir |
|
The adverse/toxic effects of reverse transcriptase inhibitors (nucleoside), such as Abacavir, may be enhanced by Valganciclovir. There is a risk of hematologic toxicity. Diligent monitoring during concomitant therapy is recommended. (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
|
HIV |
|
Publications, Variants |
|
|
HIV Infections |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
Search PubMed
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.