Futuristic Anti-Retroviral Drugs/Therapy

After three decades since the discovery of the HIV and the AIDS complication, it can be said that the use of ARV has contributed greatly to the reduction of the fatality associated with the disease. Different classes of ARV drugs have been discovered, developed and approved for use and even for prevention (Post-exposure and Pre-exposure prophylaxis) over the years. Of recent, drugs such as integrase inhibitors with very high barriers to resistance and good safety profile have been added to the first line therapy all in a bid to give the patients the best available HIV chemotherapy .Despite this ,poor adherence due to the required daily intake of the ARV remains a challenge.

Some of the therapeutic interventions that were taken to improve adherence include the following

  1. Production of fixed dose combination (FDC) e.g. Tuvada
  2. Once daily dose ARV combination e.g. Atripla

The most recent chemotherapeutic intervention, which will also form the mainstay of future ART is the   Long-acting antiretroviral therapy (LA-ART) for HIV — also referred to as extended-release (ER) antiretroviral therapy.

The advantages of LA-ART include infrequent dosing; the potential for lower doses than oral medications using nanoformulations; and the prevention of poor adherence on oral antiretroviral, tissue targeting of the injectable therapy and the countering of fill fatigue with periodic injections. Also less-frequent treatment dosing could protect HIV-positive people’s health privacy and reduce stigma by eliminating their need to fill prescriptions and carry or store pills.

Some antiretroviral being developed for LA-ART administration include integrase inhibitor cabotegravir, the NNRTI rilpivirine, ibalizumab, PRO 140, albuvirtide and several  broadly neutralizing monoclonal antibodies (VRC01, VRC01-LS, 3BNC117 and 10-1074).

Currently,the  two injectable approved for LA-ART are ibalizumab by the US FDA and   albuvirtide by the Chinese FDA

Some currently approved antiretroviral, such as lopinavir, ritonavir (Norvir) and tenofovir (Viread), could be reformulated to extend their half-life to enhance their concentration in lymphatic tissue and therefore serve as LA-ART.

LA-ART unlike the currently available oral ARV can be administered via intramuscular injection, as implants, LA-ART implant allows for a consistent, predictable release of a drug (potentially for years) that is not dependent on the choice of injection sites, and it can still be removed in cases of drug toxicity or a necessary change in treatment.

In conclusion, long-acting drugs will not only cause dramatic change in HIV treatment other infectious diseases control such as tuberculosis, hepatitis virus, malaria and epidemics like Ebola will also be impacted greatly by these extended-release formulations.


Dr Abayomi Afe contributed this article.

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