GLBT News You Can Use #2
By JMcQ

Vocabulary:

CD4+ cells – aka T-helper cells. These are one of a section of T-4 cells, also known as lymphocyte. These cells protect (are antibodies) against disease. Less CD4+ cells means that less harmful diseases can create more serious consequences in a immuno-compromised individual.

Opportunistic Infections (OIs) – Diseases that are deadly in AIDS-infected individuals. OIs include thrush (fungus in the mouth or any other moist orifice), cytomegalovirus (an eye-infliction that can cause blindness), pneumocystis pneumonia, toxoplasmosis (infection of the brain).

Diarylpyrimidines (DAPYs) – Reverse transcriptase inhibitors (non-nucleoside reverse transcriptase inhibitor or NNRTI) that mimic HIV’s continually-changing shape, which blocks the use of a certain enzyme by the virus. This enzyme is needed to propagate HIV through the host body.

A brief history of HIV/AIDS:

A brief run-through of HIV (Human Immunodeficency Virus/AIDS (Acquired Immune Deficiency Syndrome) is necessary to understand the importance of the DAPYs in treating HIV. HIV is transmitted through breast milk, blood and vaginal/seminal fluid, and may remain in an infected individual’s system for years before becoming AIDS. The immediate affects of being infected by HIV are fairly mild, almost flu-like in symptoms: individuals my run a fever, have a skin rash, get inflamed lymph nodes, but the disease is insidious in its destruction of CD4+ cells. Healthy individuals have an average of 500-1500 of these CD4+ cells in the average milliliter of blood, where HIV treatment is recommended at 350/mL and full-blown AIDS is declared at 200/mL.

Contrary to popular belief, there has not been a cure for HIV/AIDS as of this piece, and with every passing year that this disease is incurable, over 5,000,000 more people will be infected by it. Between 1981 and 2003, 20,000,000 people died from AIDS-related illnesses. It must be known that AIDS is not a deadly disease itself, but through opportunistic infections (OIs) the death count rises. Treatment of OIs have curtailed the number of deaths by AIDS in places where there is adequate sanitation and medical facilities, but some of the most infected areas are in the poorest sections of the world, with Africa unfortunately leading the way.

There has been some progress in bringing AIDS-combating drugs to Africa, with the WTO relaxing some of the patent regulations, which lowers the cost of drugs for those individuals in foreign lands. While there is still debate on whether the pharmaceutical companies are price gouging, the prices of drug doses are cut by large amounts. For example, AZT (Azidothymidine) sells in South Africa for $2.16, compared to $10.12 in the United States . Again, many of the world’s 1.2 billion individuals who are in acute poverty – living under $1 a day – are living in Africa (307 million).

Even with a strong government, which is itself hard to find outside of South Africa, the 35 million (as of 1998) individuals infected with AIDS can’t pay for their medications. Nations have been criticized for not accepting free medications from pharmaceutical companies, but the simple fact is that a number of these companies are allowing for a five or ten year free period, after which, the drugs would end being free. Just like the free sample, individuals would be hooked on these medications, and the nations that have been approached by companies have rebuffed their shady dealings.

Ripilvirine and the DAPYs:

Still, even though their motives may be suspect, the simple fact is that these pharmaceutical companies and research university are doing enormous amounts of R&D to create new medications to treat HIV and AIDS. The most exciting work comes from Rutgers (State University of New Jersey), where Dr. Eddy Arnold’s (Professor of Chemistry) research team has created a set of new drugs, TMC-120 (dapivirine), TMC-125 (etravirine) and R278474 (ripilvirine). These three drugs may be grouped together because of their structures, but their effectiveness in combating different mutations of HIV are wildly different. For example, ripilvirine, in tests using a human T-cell line in calf serum, is three (.4 vs 1.2) to fifty-four (1.0 vs 54) times as effective as dapivirine. When compared to on-the-market medications like efavirenz, ripilvirine is ten to twenty times more effective.

A DAPY is radically different from the massive bulk of AIDS medications because of the way it operates – it is malleable enough that HIV cannot become resistant to its treatment. With the previous treatment, such as AZT (released in 1987 for consumption), HIV/AIDS could become resistant in the course of a week to the new regiment. Different in another way from the previous treatments, the DAPYs attack HIV before its entrance into a T-4 cell.

To go back to the problem concerning the massive number of those poverty-stricken infected with AIDS, Ripilvirine, the newest DAPY, is a single-pill treatment. Its precursor, etravirine has achieved a viral load that is comparable to one of the leading five-pill cocktails on the market in its tests. This mean that ripilvirine would have a lower per-dosage cost than a number of the current leading medications, which are a multi-pill combination (a “drug cocktail”). The synthesizing of the drug itself is easier than previous treatments, and all of the tests that the other two compounds have been in have been passed with flying colors. Individuals are already being chosen for Phase III testing (which is slated to state in the middle of the current year). Phase III is where the FDA makes the final decision on whether the medicine is permissible for use in the United States.

By all previous tests, ripilvirine is safe even up to large dosages (800 mg/kg), and does not have side-effects any more than increased salivation (even up to a month of continued dosing). While only the first of the DAPYs is getting to the stage where its effects can be shown on humans, the fact is that in the next decade or so, a new, low-morbidity, easy-to-take medication can be on the market that can stop HIV largely in its tracks. If it is as successful as both its predecessor was on humans and as it itself was on animals, ripilvirine may be a large part of the solution for Africa’s AIDS problem. It is cheaper to create, manufacture, and sell than previous medications. Let’s only hope that it will come out before too many more individuals perish.