Long Term Treatment of HIV-Infection With TMC278

a technology of tmc278 and long-term treatment, applied in the field of long-term treatment of hiv infection, can solve the problems of resistance, no currently available drug therapy is capable of completely eradicating hiv, and emergence of mutants

Inactive Publication Date: 2021-06-17
JANSSEN SCI IRELAND UC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This approach results in stable plasma levels of TMC278, reducing the viral load and improving patient compliance by simplifying the administration schedule and minimizing the risk of resistance, thus effectively managing HIV infection with fewer drug administrations.

Problems solved by technology

The treatment of Human Immunodeficiency Virus (HIV) infection, known as cause of the acquired immunodeficiency syndrome (AIDS), remains a major medical challenge.
Although effective in suppressing HIV, each of these drugs, when used alone, is confronted with the emergence of resistant mutants.
However, none of the currently available drug therapies is capable of completely eradicating HIV.
Even HAART can face the emergence of resistance, often due to non-adherence and non-persistence with antiretroviral therapy.
A high pill burden is undesirable for many reasons, such as the frequency of intake, often combined with the inconvenience of having to swallow large dosage forms, as well as the need to store and transport a large number or volume of pills.
A high pill burden increases the risk of patients not taking their entire dose, thereby failing to comply with the prescribed dosage regimen.
As well as reducing the effectiveness of the treatment, this also leads to the emergence of viral resistance.
The problems associated with a high pill burden are multiplied where a patient must take a combination of different anti-HIV agents.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example

[0052]This example shows a study aimed at demonstrating that the administration of a parenteral formulation of TMC278 results in stable blood plasma levels during a prolonged period of time. By increasing the dose of TMC278 of the parenteral formulation higher blood plasma levels are obtained, for example a dose of about 10 mg / kg is expected to result in effective blood plasma levels. By administering the parenteral formulation intermittently at time intervals of one month, stable blood plasma levels of TMC278 are obtained, effectively suppressing viral multiplication.

[0053]The study was performed in order to study the plasma kinetics and the absolute bioavailability of TMC278 in the beagle dog 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.

[0054]Two male beagle dogs (dog No. 16924 and 16854), approximately 3 years old and weighing between 11 and 12 ...

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Abstract

This invention relates to the use of a parenteral formulation comprising an anti-virally effective amount of TMC278 or a pharmaceutically acceptable acid-addition salt thereof, and a carrier, for the manufacture of a medicament for the treatment of a subject being infected with HIV, wherein the formulation is to be administered intermittently at a time interval of at least one week.

Description

FIELD OF THE INVENTION[0001]This invention relates to the long term treatment of HIV infection by intermittently administering a parenteral formulation comprising the NNRTI TMC278 at relatively long time intervals.BACKGROUND OF THE INVENTION[0002]The treatment of Human Immunodeficiency Virus (HIV) infection, known as cause of 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]Although effective in suppressing HIV, each of these drugs, when used alone, is confronted with the emergence of resistant mutants. This led to the introduc...

Claims

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Application Information

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Patent Type & AuthorityApplications(United States)
IPC IPC(8): A61K31/505
CPCA61K31/505A61P31/00A61P31/18
InventorBAERT, LIEVEN ELVIRE COLETTEKRAUS, GUENTERVAN 'T KLOOSTER, GERBEN ALBERT ELEUTHERIUS
OwnerJANSSEN SCI IRELAND UC