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Apricitabine
Systematic (IUPAC) name
4-amino-1-[(2R,4R)-2-(hydroxymethyl)-1,3- oxathiolan-4-yl]pyrimidin-2(1H)-one
Identifiers
CAS number 160707-69-7
ATC code none
PubChem 455041
Chemical data
Formula C 8H11N3O3S 
Mol. mass 229.256 g/mol
Pharmacokinetic data
Bioavailability 65 to 80%
Protein binding < 4%
Metabolism To apricitabine triphosphate
Half life 6 to 7 hours (triphosphate)
Excretion Renal
Therapeutic considerations
Pregnancy cat.  ?
Legal status Investigational
Routes Oral

Apricitabine (INN, codenamed AVX754 and SPD754) is an experimental nucleoside reverse transcriptase inhibitor (NRTI) against HIV. It is structurally related to lamivudine and emtricitabine, and, like these, is an analogue of cytidine.

Contents

History

It was first developed by BioChem Pharma (where it was called BCH10618). BioChem Pharma was then sold to Shire Pharmaceuticals (where apricitabine was called SPD754). Shire then sold the rights to develop the drug to Avexa Pharmaceuticals, an Australian pharmaceutical company.[1] As of 2009, apricitabine has closed its phase III clinical trial[2], and has been granted fast track status by the United States Food and Drug Administration.[3]

Dosage

As a monotherapy, 1200 mg apricitabine per day reduced the viral load by up to 1.65 logs (45 fold) in a small, 10-day randomized controlled trial.[4]

Adverse effects

Apricitabine appears to be well tolerated. The most common side effects associated with its use were headache (although there was no significant difference between participants who took apricitabine and those given a placebo), nasal congestion, and muscle pain.[4] In a six-month trial, common adverse effects were nausea, diarrhea, elevated blood levels of triglycerides, and upper respiratory infection—similar to those of lamivudine; apricitabine was not associated with abnormal lipase levels, bone marrow suppression, or liver and kidney toxicity.[5] No patients in either study had to stop taking apricitabine because of side effects.

Drug resistance

In vitro, apricitabine was effective against NRTI-(lamivudine and zidovudine)-resistant viruses.

In early studies, no mutations causing drug resistance were observed. Newer trials showed that apricitabine may induce K65R mutations, resulting in resistance against didanosine and tenofovir.[1]

References

  1. ^ a b AIDSmeds.com - apricitabine
  2. ^ Avexa Closes ATC's Phase III Trial To Evaluate Data
  3. ^ "Apricitabine". AIDSinfo. U.S. National Institutes of Health. March 13, 2007. http://www.aidsinfo.nih.gov/DrugsNew/DrugDetailT.aspx?int_id=415. Retrieved 2008-08-29.  
  4. ^ a b Cahn P, Cassetti I, Wood R, et al. (June 2006). "Efficacy and tolerability of 10-day monotherapy with apricitabine in antiretroviral-naive, HIV-infected patients". AIDS 20 (9): 1261–8. doi:10.1097/01.aids.0000232233.41877.63. PMID 16816554.  
  5. ^ Cox S, Moore S, Southby J, et al. (August 5, 2008). "Safety profile of apricitabine, a novel NRTI, during 24-week dosing in experienced HIV-1 infected patients". XVII International AIDS Conference (AIDS 2008). Mexico City. Abstract TUAB0106. http://www.aids2008.org/Pag/Abstracts.aspx?SID=256&AID=4376. Retrieved 2008-08-29.   Lay summary
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