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Prevention Of Hiv-Infection With Tmc278

a technology of tmc278 and tmc278, which is applied in the direction of biocide, drug composition, animal husbandry, etc., can solve the problems of suppressing virus replication to a level, causing the outbreak of symptoms for a long time, and only transiently restraining viral replication by each drug if used alone, so as to achieve the effect of preventing hiv infection

Inactive Publication Date: 2008-08-14
TIBOTEC BVA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010]In one aspect, the present invention relates to the use of a parenteral formulation comprising an effective amount of TMC278 or a pharmaceutically acceptable acid-addition salt thereof, and a carrier, for the manufacture of a medicament for the long term prevention of HIV infection in an individual at risk of being infected by HIV, wherein the formulation is administered intermittently at a time interval of at leas

Problems solved by technology

The treatment of Human Immunodeficiency Virus (HIV) infection, which is causative to the acquired immunodeficiency syndrome (AIDS), remains a major medical challenge.
Each of these drugs can only transiently restrain viral replication if used alone.
However, none of the currently available drug therapies is capable of completely eradicating in HIV and long-term treatment usually results in suppressing virus replication to a level where it no longer can cause the outbreak of the symptoms associated with AIDS.
A high pill burden is undesirable for many reasons, such as the patient having to spend more time taking each dose and the patient having to store and / or transport a large number or volume of pills.
A high pill burden also increases the risk that a patient will not take his or her entire dose, thereby failing to comply with the prescribed dosage regimen.
As well as reducing the effectiveness of the treatment for that patient, this may also lead to the disease-causing organism or virus becoming resistant to the pharmaceutical agent.
Individuals infected by HIV virus often are unaware of the fact that they carry the virus and therefore constitute a continuous risk of transferring the infection to others.
Even in developed countries this is still the case but in particular is a threat in many of the less-developed countries, where people have no or limited access to medical care, including to HIV diagnostic tools.
Despite these measures there is always an imminent risk for certain population groups to become infected with HIV.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

examples

[0052]The present study was performed in order to study the plasma kinetics and the absolute bioavailability of TMC278 in beagle dogs after single intramuscular administration (IM) of an aqueous 30% dimethylacetamide (DMA) / 50% polyethylene glycol 400 (PEG400) solution of TMC278 at 2.5 mg / kg. The dogs were dosed IM.

[0053]Two male beagle dogs (dog No. 16924 and 16854), approximately 3 years old and weighing between 11 and 12 kg at the start of the experimental phase, were used in the present experiment. The dogs were dosed intramuscularly at 0.1 ml / kg body weight by injecting the formulation in the left (dog No. 16924) or right (dog No. 16854) m. biceps femoris.

[0054]One day before dose administration, TMC278 was formulated in an aqueous 30% (w / v) DMA / 50% (w / v) PEG400 solution at 25 mg / ml. The ingredients of the solution were: TMC278, DMA 30% (w / v), PEG 400 50% (w / v) and pyrogenic free water. The content of TMC278 in the formulation was checked using LC. The concentration of TMC278 in...

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Abstract

This invention relates to the use of a parenteral formulation comprising the NNRTI TMC278 for the long term prevention of HIV infection in a subject at risk of being infected by HIV, which comprises the intermittent administration of the said formulation at long time intervals.

Description

FIELD OF THE INVENTION[0001]This invention relates to the use of a parenteral formulation comprising the NNRTI TMC278 for the long term prevention of HIV infection in a subject at risk of being infected by HIV, which comprises the intermittent administration of the said formulation at long time intervals.BACKGROUND OF THE INVENTION[0002]The treatment of Human Immunodeficiency Virus (HIV) infection, which is causative to the acquired immunodeficiency syndrome (AIDS), remains a major medical challenge. HIV is able to evade immunological pressure, to adapt to a variety of cell types and growth conditions and to develop resistance against currently available drug therapies. The latter include nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), nucleotide reverse transcriptase inhibitors (NtRTIs), HIV-protease inhibitors (PIs) and the more recent fusion inhibitors.[0003]Each of these drugs can only transiently restrain viral repl...

Claims

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Application Information

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IPC IPC(8): A61K31/505A61P31/18
CPCA61K9/0019A61K47/16A61K47/10A61K31/505A61P31/00A61P31/18A61P43/00
Inventor BAERT, LIEVEN ELVIRE COLETTELEWI, PAULUS JOANNESHEERES, JAN
Owner TIBOTEC BVA