Abacavir drug data and news

Abacavir drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Abacavir
Brand Names/Synonyms 1592U89; ABC; Abacavir; Abacavir [Inn]; Ziagen
Indication For the treatment of HIV-1 infection, in combination with other antiretroviral agents
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Description Not Available
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.
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.
Abacavir News
(When available)

Research Needs State, Corporate Support  06 Mar 2006
For example, bio-markers can be used to test for susceptibility to ADRs induced by anti-retrovirals (ARVs) such as Nevirapine and Abacavir. ... - AllAfrica.com,

CROI: abacavir may be safer than nevirapine in Africans  Feb 8, 2006
Abacavir appears to cause fewer serious adverse drug reactions than nevirapine in African patients taking part in a substudy of the DART trial, investigators ... - Aidsmap,

CROI: abacavir gene testing reveals high levels of ...  Feb 14, 2006
...in Brighton of the efficacy of testing for the HLA-B*5701 mutation that is strongly associated with the hypersensitivity reaction to abacavir has revealed ... - Aidsmap,

CROI: early vs delayed Trizivir in TB/HIV coinfected - no ...  Mar 2, 2006
Starting antiretroviral treatment with Trizivir (abacavir, zidovudine and lamivudine fixed dose combination) almost immediately after beginning TB treatment ... - Aidsmap,

Advances in First-Line and "Switch" Antiretroviral Strategies for ...  Feb 2, 2006
3, randomized double-blind comparison of 3 simple regimens for the initial treatment of HIV infection: (1) zidovudine/lamivudine/abacavir coformulated (triple ... - Medscape (subscription)

AIDS: Help the victims  Feb 25, 2006
Remarkably, there is nothing complicated about dosage, which in most cases involves two capsules a day, each containing lamivudine, abacavir and zidovudine, or ... - The National,

Global Challenges | Clinton Foundation To Help Train Nurses in ...  Feb 22, 2006
Cipla will produce the drug abacavir for $447 per patient annually -- a price that reduces by 30% or more the cost of antiretroviral medications -- as part of ... - Kaiser network.org,

CROI: Risk of new illnesses declines sharply after first 2 months ...  Feb 10, 2006
...between being on a NNRTI-based regimen or a PI-based regimen, individuals taking other three drug regimens (triple nucleoside analogs such as abacavir/AZT/3TC ... - Aidsmap,

CROI: Lipodystrophy stable in children on HIV treatment and does ...  Feb 23, 2006
Adult studies have shown a modest improvement in limb fat levels after d4T is replaced with either abacavir (Ziagen) or tenofovir, but similar strategies have ... - Aidsmap,

CROI: AZT, 3TC and FTC achieve good concentrations in the female ...  Feb 17, 2006
The women were treated with antiretroviral regimens that included 3TC, AZT, abacavir (Ziagen), ddI (didanosine, Videx), d4T (stavudine, Zerit), efavirenz ... - Aidsmap,

AHF Applauds Idaho Medicaid for Placing Restrictions on Glaxo AIDS ...  Feb 23, 2006
...the NIH suspended part of a three-arm, two-year government sponsored AIDS Clinical Trials Group Study (ACTG 5095) comparing AZT+3TC+abacavir (the components of ... - Yahoo! News (press release)

Add new comment  Feb 15, 2006
...world at affordable prices. Cipla will make the antiretroviral abacavir for $447 for Clinton Foundation. Apart from Cipla, four ... - Herald Publications,

Simplified treatment regimens show promise in HIV-infected ...  Feb 6, 2006
After switching, all of the children were taking 3TC (lamivudine, Epivir) and abacavir (Ziagen), along with either AZT (zidovudine, Retrovir) or d4T (stavudine ... - Aidsmap,

CROI: Tenofovir and kidney toxicity - low rates seen, but some ...  Feb 9, 2006
...failing their current regimen. In addition all patients received abacavir plus another NRTI (usually 3TC). The only variable in ... - Aidsmap,

CROI News Feature: Experts divided over the future of treatment ...  Feb 9, 2006
...counts must never have fallen below 100 cells/mm 3 (the median CD4 nadir was, in fact, 280 cells/mm 3 ), and it excluded anyone taking abacavir (Ziagen) or ... - Aidsmap,

4-Day-A-Week Treatment Plan for HIV Infected Adolescents  Feb 18, 2006
On a HAART regimen containing an NNRTI or a HAART regimen with Abacavir (including Trizivir®). On any prohibited medication at the time of screening. ... - Community Dispatch (press release)

Dosage Forms SOLUTION; TABLET
Drug_Category Anti-HIV Agents; Nucleoside and Nucleotide Reverse Transcriptase Inhibitors; ATC:J05AF06
Absorption Rapid and extensive after oral administration (83% bioavailability)
Interactions -->Interactions for Abacavir:

Pharmacokinetic properties of abacavir were not altered by the addition of either lamivudine or zidovudine or the combination of lamivudine and zidovudine. No clinically significant changes to lamivudine or zidovudine pharmacokinetics were observed following concomitant administration of abacavir.

Abacavir has no effect on the pharmacokinetic properties of ethanol. Ethanol decreases the elimination of abacavir causing an increase in overall exposure .

The addition of methadone has no clinically significant effect on the pharmacokinetic properties of abacavir. In a study of 11 HIV-infected patients receiving methadone-maintenance therapy (40 mg and 90 mg daily) with 600 mg of ZIAGEN twice daily (twice the currently recommended dose), oral methadone clearance increased 22% (90% CI 6% to 42%). This alteration will not result in a methadone dose modification in the majority of patients; however, an increased methadone dose may be required in a small number of patients.

Toxicity Some myocardial degeneration has been noticed in rats and mice
Organisms Affected Human immunodeficiency virus
Chemical IUPAC Name [4-(2-amino-6-cyclopropylamino-9H-purin-9-yl)-1-cyclopent-2-enyl]methanol
Chemical Formula C14H18N6O
Molecular Weight 286.333 g/mol
Smiles String C1CC1NC2=NC(=NC3=C2N=CN3C4CC(C=C4)CO)N
Melting Point 165 °C
Water Solubility 77 mg/mL (sulfate salt)
State Solid
LogP/Hphobicity 0.389
Isoelectric Point Not Available
Biotransformation Hepatic, by alcohol dehydrogenase and glucuronosyltransferase
Half Life 1.5 hours
Protein Binding [%] 49%
RxList Link RXlist
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Drug Reference http://www.drugs.com/cons/Abacavir.html
http://www.rxlist.com/cgi/generic2/abavir.htm
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/cx1527.shtml
http://www.drugs.com/pdr/ABACAVIR_SULFATE.html
Drug Type Approved Drug
Accession No APRD00216
CAS Registry Number 136470-78-5
KEGG Compound ID C07624
PubChem ID SID:208126
PharmGKB ID PA448004
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 2240358

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