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 that is being studied for the treatment of HIV infection.
BMS-663068 belongs to a class (group) of HIV drugs called entry and fusion inhibitors.2 Entry and fusion inhibitors block HIV from getting into and infecting certain cells of the immune system. This prevents HIV from multiplying and can reduce the amount of HIV in the body.
By attaching to the gp41 protein on the outer surface of HIV, BMS-663068 blocks HIV from getting into and infecting the immune cells. 3
BMS-663068 is a prodrug, which means that it is an inactive drug. Once taken, a prodrug does not work until the body converts it into an active form. In the body, BMS-663068 is converted to BMS-626529.3
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.4
- 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.4
In most cases, an investigational drug must be proven safe and effective in a Phase III clinical trial to be considered for 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.4
In what phase of testing is BMS-663068?
BMS-663068 is currently being studied in Phase II clinical trials.2
What have recent studies shown about BMS-663068?
In an early Phase II study, two different strengths of BMS-663068 were investigated in HIV-infected participants who had HIV-1 subtype B. Some of the participants had never taken HIV medicines before entering the study (treatment-naive), and others had taken HIV medicines previously (treatment-experienced). The treatment-experienced participants were required to be off HIV medicines for at least 8 weeks before starting BMS-663068. 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 study. Study participants did not receive additional HIV medicines 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.)3,5
In this study, BMS-663068 was shown to have substantial antiviral activity, decreasing viral load (the amount of HIV in the blood) 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, there were no clinically relevant effects on electrocardiogram (ECG), laboratory values, vital signs, or physical exams. The most common side effects were mild headache and rash.3,5
An additional Phase II trial of BMS-663068 in treatment-experienced participants is under way.6
What side effects might BMS-663068 cause?
In the first Phase II study discussed under the previous question, which looked at treatment with different doses of BMS-663068 over 8 days, the most common side effects were mild headache and rash.5
Because BMS-663068 is still being studied, information on possible side effects of the drug is not complete. As testing of BMS-66308 continues, additional information on possible side effects will be gathered.
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?
Participating in a clinical trial can provide benefits. For example, a volunteer participant can benefit from new research treatments before they are widely available. Participants also receive regular and careful medical attention from a research team that includes doctors and other health professionals. However, clinical trials may also involve risks of varying degrees, such as unpleasant, serious, or even life-threatening side effects from the treatment being studied.4
Your health care provider can help you decide whether participating in a clinical trial is right for you. For more information, visit NIH Clinical Research Trials and You
. United States National Library of Medicine. ChemIDplus Advanced
. National Institute of Allergy and Infectious Diseases (NIAID). NIAID ChemDB, HIV Drugs in Development
. Nettles RE, Schürmann D, Zhu L, et al. Pharmacodynamics, safety, and pharmacokinetics of BMS-663068, an oral HIV-1 attachment inhibitor in HIV-1-infected subjects
. J Infect Dis
. 2012 Oct 1;206(7):1002-11.
. National Institutes of Health (NIH). NIH Clinical Research Trials and You
. Nettles R, Schurmann D, Zhu L, et al. Pharmacodynamics, Safety, and Pharmacokinetics of BMS-663068: A Potentially First-in-class Oral HIV Attachment Inhibitor
. Paper presented at: 18th Conference on Retroviruses and Opportunistic Infections (CROI); February 27-March 2, 2011; Boston, MA. Paper 49.
. Bristol-Myers Squibb. A Phase IIb Randomized, Controlled, Partially-Blinded Trial to Investigate Safety, Efficacy and Dose-Response of BMS-663068 in Treatment-experienced HIV-1 Subjects, Followed by an Open-Label Period on the Recommended Dose
. In: ClinicalTrials.gov. Bethesda (MD): National Library of Medicine (US). Registered on June 23, 2011. NLM Identifier: NCT01384734. Last accessed April 3, 2013.
Last Reviewed: May 29, 2013
Last Updated: May 29, 2013