Apricitabine

  • (-)- 2'-deoxy -3' -oxa -4'- thiocytidine ( DotC )
  • 4-amino- 1-[ (2R, 4R ) -2 - ( hydroxymethyl) - 1,3- oxathiolan -4-yl ] pyrimidin- 2-one
  • Antiviral
  • Nucleoside reverse transcriptase inhibitors

Competitive inhibition of reverse transcriptase

Template: Infobox chemical / molecular formula search available

Apricitabine ( SPD754, AVX754 ) is an experimental drug for the treatment of HIV and its subsequent stages in a combination therapy for HIV.

It belongs to the group of nukelosidischen reverse transcriptase - inhibitors ( NRTIs).

History

Apricitabine is currently being developed and tested by Avexa Pharmaceuticals, an Australian pharmaceutical company. Phase IIb studies were completed in 2006.

The drug was originally developed by BioChem Pharma as BCH10618. After being sold to Shire Pharmaceuticals, the active ingredient in SPD754 has been renamed. Shire then sold the rights to Avexa ( AVX754 ).

Pharmacology

Apricitabine was investigated in several studies. Result of the study is that among the best apricitabine monotherapy viral suppression was achieved at a dosage of 1200 mg. The drug was able to reduce the viral load by up to 1.65 logs.

The similarity to the active ingredients lamivudine (Epivir ®) and emtricitabine ( Emtriva ®) makes a combination with them meaningless.

Pharmacokinetics

Apricitabine was rapidly taken up in studies and mainly metabolized by the kidneys. Peak plasma levels are reached after 1.5 to 2.5 hours.

Side effects

Apricitabine was well tolerated in previous studies.

Resistance

In earlier studies, no treatment-related resistance mutations were observed.

In vitro apricitabine showed good activity against NRTI -resistant strains (including zidovudine (Retrovir ®) and lamivudine (Epivir ®) ). Previous studies showed that apricitabine is also effective against strains with Epivir resistance. New studies show that the active ingredient K65R mutations with resistance to didanosine (Videx ®) and tenofovir ( Viread ®) may cause.

In future studies will clarify whether the agent is actually responsible for the K65R mutation.

CAS registry number PubChem Shire plc AIDS (journal)
73240
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