What is an investigational drug?
An investigational drug is one that is under study and is not approved by the U.S. Food and Drug Administration (FDA) for sale in the United States. Medical research studies are conducted to evaluate the safety and effectiveness of an investigational drug. These research studies are also called clinical trials. Once an investigational drug has been proven safe and effective in clinical trials, FDA may approve the drug for sale in the United States.
What is BMS-663068?
BMS-663068 is an investigational drug for the treatment of HIV infection.
- BMS-663068 is an investigational anti-HIV drug included in the entry inhibitor drug class.
- Entry inhibitors interfere with the first step in the HIV life cycle—binding and fusion to target cells. By preventing HIV from entering target immune cells, entry inhibitors stop HIV from replicating and reduce the amount of HIV in the blood.
- BMS-663068 is called a prodrug. A prodrug is an inactive drug that is converted inside the body into an active form. In the body, BMS-663068 is converted to an active drug known as BMS-626529.
- BMS-626529 binds to glycoprotein gp120, which is located on the HIV envelope. By binding to gp120, BMS-626529 prevents HIV from being able to bind to CD4 receptors—receptors found on certain immune cells, such as CD4 cells. When BMS-626529 blocks HIV from binding to the CD4 receptor, HIV cannot attach to, enter, or infect the immune cell.
How are clinical trials of investigational drugs conducted?
Clinical trials are conducted in “phases.” Each phase has a different purpose and helps researchers answer different questions.
- Phase I trials: Researchers test an investigational drug in a small group of people (20–80) for the first time. The purpose is to evaluate its safety and identify side effects.
- Phase II trials: The investigational drug is administered to a larger group of people (100–300) to determine its effectiveness and to further evaluate its safety.
- Phase III trials: The investigational drug is administered to large groups of people (1,000–3,000) to confirm its effectiveness, monitor side effects, compare it with standard or equivalent treatments, and collect information that will allow the investigational drug to be used safely.
An investigational drug must be proven safe and effective in a Phase III clinical trial to be considered for traditional approval by the FDA for sale in the United States. Some drugs go through the FDA’s accelerated approval process and are approved before a Phase III clinical trial is complete. After a drug is approved by the FDA and made available to the public, researchers track its safety in Phase IV trials to seek more information about the drug’s risks, benefits, and optimal use.
In what phase of testing is BMS-663068?
BMS-663068 is currently being studied in Phase II clinical trials.
What have recent studies shown about BMS-663068?
In an early Phase II study, two different strengths of BMS-663068 were investigated in both treatment-experienced and treatment–naive HIV-infected participants. Treatment-experienced participants were required to be off anti-HIV therapy for at least 8 weeks prior to starting BMS-663068. Study participants included only those who were infected with HIV-1 subtype B. BMS-663068 was given either once or twice daily, with and without the booster drug ritonavir (brand name: Norvir), an FDA-approved protease inhibitor. A control arm was not used in this trial. Study participants did not receive additional anti-HIV drugs as part of a background regimen. (A background regimen is a combination of drugs that are not being studied as the investigational drug[s] in the clinical trial, but are being given to help control a participant’s HIV infection.)
In this study, BMS-663068 was shown to have substantial antiviral activity, decreasing viral load from baseline. Investigators concluded that BMS-663068 may be given either once or twice daily and with or without a ritonavir booster. In terms of safety, BMS-663068 was well tolerated. The most common side effects were headache and rash.
An additional Phase II trial of BMS-663068 in treatment-experienced participants is under way.
More information on testing of BMS-663068 is available from these sources:
- BMS-663068 study results presented at the 18th Conference on Retroviruses and Opportunistic Infections (CROI), February 27–March 2, 2011:
- PubMed abstract:
Where can I get more information about clinical trials studying BMS-663068?
More information about BMS-663068-related research studies
is available from the AIDSinfo
database of ClinicalTrials.gov
study summaries. Click on the title of any trial in the list to see the ClinicalTrials.gov
trial summary and more information about the study.
I am interested in participating in a clinical trial of BMS-663068. How can I find more information about participating in a clinical trial?
Clinical trials involve benefits and risks. Before deciding to participate in a clinical trial, talk to your health care provider. For more information on participating in clinical trials, visit NIH Clinical Research Trials and You
Last Reviewed: January 25, 2013
Last Updated: January 25, 2013