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Information

An Overview of Cabotegravir

November 14, 2016

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Other Names: 744 LA, CAB, GSK-1265744, GSK1265744, GSK744, GSK744 LA, GSK744 LAP, S-265744, S/GSK1265744, cabotegravir LA, cabotegravir sodium
Drug Class: Integrase Inhibitors
Molecular Formula: C19 H17 F2 N3 O5
Registry Number: 1051375-10-0 (CAS)
Chemical Name: (3S,11aR)-N-((2,4-difluorophenyl)methyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydrooxazolo(3,2-a)pyrido(1,2-d)pyrazine-8-carboxamide
Company: ViiV Healthcare
Phase of Development: Cabotegravir is in Phase IIb development for HIV treatment and Phase IIb/III development for HIV prevention.

Chemical Image:


cabotegravir

cabotegravir
Molecular Weight: 405.3553
(Compound details obtained from ChemIDplus Advanced,1 NIAID Therapeutics Database,2 and HIV i-BASE/Treatment Action Group 2016 Pipeline Report3)


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.

To learn more about investigational drugs, read the AIDSinfo What is an Investigational HIV Drug? fact sheet.


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What Is Cabotegravir?

Cabotegravir is an investigational drug that is being studied for the treatment and prevention of HIV infection.4

Cabotegravir belongs to a class (group) of HIV drugs called integrase inhibitors.2 Integrase inhibitors block an HIV enzyme called integrase. (An enzyme is a protein that starts or increases the speed of a chemical reaction.) By blocking integrase, integrase inhibitors prevent HIV from multiplying and can reduce the amount of HIV in the body.

Cabotegravir does not require boosting with an additional drug. (Boosting involves the use of a second drug to increase the effectiveness of the main [first] drug.)5

Two forms of cabotegravir are being studied: tablets that are taken by mouth (known as oral cabotegravir or oral CAB) and a long-acting injectable form that is injected into the muscle (known as cabotegravir LA or CAB LA; LA stands for "long-acting").6,7 (A long-acting drug formulation works over a long period of time. Using this type of drug might mean that the drug could be taken less often, making a treatment or prevention regimen simpler to take.)4


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.8

  • 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.8

In most cases, an investigational drug must be proven effective and must show continued safety in a Phase III trial to be considered for approval by FDA for sale in the United States. Some drugs go through FDA's accelerated approval process and are approved before a Phase III clinical trial is complete. After a drug is approved by 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.8 (Some clinical trials are categorized as "a" or "b," such as "Phase Ia" or "Phase IIb." These different sublevels typically mean that a study is researching certain types of information or using a certain type of participant population.)


In What Phase of Testing Is Cabotegravir?

Cabotegravir is currently being studied in Phase IIb testing for HIV treatment and Phase IIb/III testing for HIV prevention.2,3


What Are Some Studies on Cabotegravir?

Cabotegravir for HIV Treatment

Study Names: LAI116482 (LATTE); NCT01641809
Sponsor: ViiV Healthcare
Phase: IIb
Location: United States and Canada
Participants

  • The participants are HIV-infected adults who have never taken HIV medicines before entering the study (also called treatment-naive). 
  • Participants have Viral loads of at least 1,000 copies/mL at the start of the study. (Viral load is the amount of HIV in a blood sample.)
  • Participants have CD4 counts of at least 200 cells/mm3. (A CD4 count is a laboratory test that measures the number of CD4 cells in a sample of blood and is an important indicator of immune function. The CD4 count of a healthy person ranges from 500 to 1,600 cells/mm3.)

Purpose: The purpose of this study is to find a safe and effective dose of oral cabotegravir, given as HIV maintenance therapy with the HIV oral medicine rilpivirine (brand name: Edurant). (Maintenance therapy is an ongoing treatment used to help an initial treatment succeed or to prevent a return of disease or infection.)6,9,10 

Study Names: LATTE-2; NCT02120352
Sponsor: ViiV Healthcare
Phase: IIb
Location: United States, Canada, France, Germany, Spain
Participants:

  • The participants are HIV-infected, treatment-naive adults.
  • Participants have viral loads of at least 1,000 copies/mL at the start of the study.
  • Participants have CD4 counts of at least 200 cells/mm3.
Purpose: The purpose of this study is to look at the safety and effectiveness of using 2 investigational long-acting injectable medicines together as HIV maintenance therapy. The 2 medicines are cabotegravir LA and rilpivirine LA. (Rilpivirine LA is also known as TMC278 LA.) Other participants in the study will receive oral cabotegravir. On the basis of results from this study, investigators also plan to choose a dosing regimen to be used in Phase III studies.7,11


Cabotegravir for HIV Prevention

Study Names: ECLAIR; NCT02076178
Sponsor: ViiV Healthcare
Phase: IIa
Location: United States
Participants: The participants were HIV-uninfected adult males who had a low risk of being infected with HIV. 
Purpose: The purpose of this study was to look at the safety, tolerability, and acceptability of cabotegravir LA when used to prevent people from being infected with HIV (a method that is also known as pre-exposure prophylaxis, or PrEP). Participants received both oral cabotegravir and cabotegravir injections over the course of the study.12,13

For more details on the studies listed above, see the Health Professional version.

Another Phase IIa study, called HPTN 077 (NCT02178800), is evaluating the safety, tolerability, and drug properties of cabotegravir LA in HIV-uninfected men and women.14 Additionally, a Phase IIb/III study called HPTN 083 (NCT02720094) is evaluating the safety and effectiveness of cabotegravir LA and comparing cabotegravir LA to a regimen that combines the FDA-approved HIV drugs tenofovir disoproxil fumarate and emtricitabine. This study will be using these drugs as PrEP for HIV-uninfected men and transgender women, both of whom have sex with men and are at high risk of being infected with HIV.15

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Related Stories

Long-Acting Cabotegravir + Rilpivirine for Induction Then Maintenance Therapy
Long-Acting Cabotegravir -- Focus on Safety
More on HIV Medications
Other Integrase Inhibitors


  
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This article was provided by AIDSinfo. Visit the AIDSinfo website to find out more about their activities and publications.
 

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