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Monthly or Quarterly Injectable HIV Antiretrovirals Are Safe and Effective in Early Study

August 5, 2013

GSK744, an investigational integrase inhibitor, and TMC278 LA (a long-acting, injectable form of the NNRTI rilpivirine [Edurant]) both showed safety and efficacy when administered in once-monthly or once-quarterly doses, according to a study presented at IAS 2013. There were no drug-related serious adverse events and all adverse events were either mild or moderate.

The phase 1 study, conducted by GlaxoSmithKline and Janssen, assessed the safety, tolerability, and pharmacokinetics of GSK744 (when given intramuscularly or subcutaneously) in conjunction with TMC278 LA (injected intramuscularly). The researchers enrolled 47 HIV-uninfected individuals (17 female and 30 male) with a median age of 39.5. Thirty-five were white, 10 black, and two of another race.

All patients were given an oral lead-in of GSK744 (also known as S/GSK1265744) at 30 mg/day for 14 days, followed by a week-long break, to assess safety and tolerability. Seven of the 47 patients discontinued the oral GSK744 because of non-drug-related adverse events or dizziness. The remaining 40 were given an 800-mg "loading dose" of GSK744 through intramuscular injection, and then randomized into four cohorts.

  • Cohort 1 received three monthly doses of GSK744 at 200 mg via subcutaneous injection (at weeks 4, 8 and 12), without TMC278 LA.
  • Cohort 2 received three monthly doses of GSK744 at 200 mg via intramuscular injection (at weeks 4, 8 and 12), with TMC278 LA via intramuscular injection (1,200 mg at week 8 and 900 mg at week 12).
  • Cohort 3 received three monthly doses of GSK744 at 400 mg via intramuscular injection (at weeks 4, 8 and 12), with TMC278 LA via intramuscular injection (1,200 mg at week 8 and 600 mg at week 12).
  • Cohort 4 received a second dose of GSK744 at 800 mg (at week 12), without TMC278 LA.

All four cohorts showed relevant plasma concentrations of the drugs within three days, meaning concentration levels were high enough to be considered effective. Between doses, concentration levels remained well above 90% inhibitory concentration (IC90) for both GSK744 and TMC278. The plasma concentration levels of TMC278 LA were comparable to taking oral rilpivirine at 25 mg/day.

Three people withdrew during the injection phase, two for non-drug-related adverse events and one for self-limited rash. The most common event not related to injection site reaction (ISR) was headache, but there were no serious adverse events (grade 4 or higher). Local ISRs were common, but generally well tolerated and self-limited.

The researchers concluded that injections of GSK744 with TMC278 LA were safe and generally well tolerated in healthy adults, with monthly or quarterly doses showing long-lasting and effective levels of plasma concentrations. Further study and clinical evaluation will be needed.

While these drugs are still in early stages of study, the hope is that they can act as long-lasting PrEP (pre-exposure prophylaxis) or effective treatment for HIV-infected patients that could replace daily pills.

View the study abstract and presentation slides.

Warren Tong is the research editor for and

Follow Warren on Twitter: @WarrenAtTheBody.

Copyright © 2013 Remedy Health Media, LLC. All rights reserved.

This article was provided by It is a part of the publication The 7th International AIDS Society Conference on HIV Pathogenesis, Treatment and Prevention.

Reader Comments:

Comment by: corrie ferreira (south africa pretoria) Mon., Feb. 2, 2015 at 2:45 pm UTC
this seem to be the way to go i am hiv positive and suffer extreme side effects from arvs is there help out there
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Comment by: hlengiwe (south africa) Sun., Aug. 17, 2014 at 12:29 pm UTC
When is such a drug coming the South Africa?
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Comment by: THADDEUS (KAMPALA UGANDA) Wed., May. 28, 2014 at 12:37 am UTC
we are realy grateful for this effort which greatly provide great hope towards cabbing down this HIV scourge which is arestlessly noble problem. please we commend more effort.
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Comment by: CM (South Africa) Fri., May. 2, 2014 at 6:08 am UTC
How can I join the study,I support injecatables than oral medication
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Comment by: joost brantas (Rotterdam, Netherlands) Wed., Aug. 21, 2013 at 4:15 pm UTC
Hope that very soon the treatment comes to Holland, the advantage of once a month or twice a day Isentress is for meso big. Tested .89 HIV+ started with trials and like to try Isentress by monthly injection and once a day Truvada becomes also by monthly injection. So fed up of thinking not to forget. Weekly I miss 2-3times Isentress cause of takin the pill to late cause of that Truvada with 20hrs gap. Cause 30years chronicHBV must take Truvada.
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Comment by: Eric (Johannesburg, South Africa) Wed., Aug. 21, 2013 at 10:10 am UTC
can my viral load increase if i stop using ARVs and stop having sex?
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Comment by: Samuel Mokiri (South Sudan) Tue., Aug. 13, 2013 at 3:09 am UTC
Good to see there is antiretroviral drug that can be taken in three different doses discovered recently. The world has been washed out old, young and new born babies are also dying. My question is WHY HIV/AIDS is dominated or pandemic and crossed into every piece of the world with out the researcher get the curable medicine for this disease ?
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Comment by: Milagros Ortiz (NEW YORK) Fri., Aug. 9, 2013 at 2:20 pm UTC
This would be great to many patients that have difficully adhering to pill consumption but I see it was test on hiv neg individuals but how would this work on hiv pos individuals whom may have other inderlying health issues this is my questions caus i believe this would be in higher doses to cover extended periods without also then becoming resistant to meds in this inject-able source
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Comment by: Ishaku (Nigeria) Fri., Aug. 9, 2013 at 4:22 am UTC
A very interesting study. I am sure that every HIV infected individual will sing for joy at this. Wow! To save us from the odeal of daily dosage. Meanwhile, we pray that more wisdom will be endowed on the researchers to enable a very effective outcome as we await a final cure which, i believe, is feasible.
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Comment by: John (Lexington, ky) Thu., Aug. 8, 2013 at 10:08 pm UTC
I would easily take a shot over a pill any day?
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Comment by: Shirley (Nigeria) Thu., Aug. 8, 2013 at 3:04 pm UTC
This is very good news and I'm wondering if the study can be extended? I would sure like to be one of the cohorts .....?
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