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Apricitabine Information

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[update], 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] Avexa announced its decision to end work on apricitabine in May 2010, which Avexa spent more than A$100 million ($90 million) developing and was in the final of three stages of patient studies usually needed for U.S. regulatory approval.

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
· · Antiviral drugs: antiretroviral drugs used against HIV (primarily J05)
Entry/fusion inhibitors (Discovery & development) gp41 (Enfuvirtide) • CCR5 (Maraviroc, Vicriviroc†, PRO 140†) • CD4 (Ibalizumab†)
Reverse-transcriptase inhibitors (RTIs)
Nucleoside & Nucleotide (NRTI)

Nucleoside analogues/NARTIs: Abacavir (ABC)°# • Emtricitabine (FTC)°# • Lamivudine (3TC)°# • Didanosine (ddI)# • Zidovudine (AZT)# • Apricitabine† • Stampidine† • Elvucitabine† • Racivir† • Amdoxovir†• Stavudine (d4T)# • Zalcitabine (ddC)◊ • Festinavir†

Nucleotide analogues/NtRTIs: Tenofovir°#
Non-Nucleoside (NNRTI) (Discovery & development) (1st generation) Efavirenz°# • Nevirapine# • Loviride◊ • Delavirdine◊ • (2nd generation) diarylpyrimidines (Etravirine, Rilpivirine†) • Lersivirine†
Integrase inhibitors Raltegravir • Elvitegravir† • Dolutegravir† • Globoidnan A (experimental) • MK-2048†
Maturation inhibitors Bevirimat† • Vivecon†
Protease Inhibitors (PI) (Discovery and development)
1st generation Fosamprenavir° • Lopinavir°# • Nelfinavir# • Ritonavir# • Saquinavir# • Amprenavir◊ • Indinavir◊#
2nd generation Atazanavir° • Darunavir • Tipranavir
Combined formulations Lamivudine/zidovudine • Emtricitabine/tenofovir/efavirenz • Abacavir/lamivudine/zidovudine • Tenofovir/emtricitabine • Lopinavir/ritonavir • Abacavir/lamivudine
Experimental agents
Uncoating inhibitors TRIM5alpha (gene)
Transcription inhibitors Tat antagonists
Translation inhibitors Trichosanthin
Other Abzyme • Calanolide A • Ceragenin • Cyanovirin-N • Diarylpyrimidines • Epigallocatechin gallate (EGCG) • Foscarnet • Griffithsin • Hydroxycarbamide • Miltefosine • Portmanteau inhibitors • Seliciclib† • Synergistic enhancers • Tre recombinase • Zinc finger protein transcription factor • KP-1461† • Cobicistat†
Failed agents Dexelvucitabine • Capravirine • Emivirine • Lodenosine • Atevirdine • Brecanavir • Aplaviroc
#WHO-EM. ‡Withdrawn from market. Clinical trials: †Phase III. §Never to phase III °DHHS preferred first-line agent. ◊Formerly or rarely used agent.

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Categories: Drugs not assigned an ATC code | Nucleoside analog reverse transcriptase inhibitors | Pyrimidones | Oxathiolanes

 

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