Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – C-o-group doai
Patent
1997-10-17
2000-07-04
Travers, Russell
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
C-o-group doai
514731, 424430, 424411, A01N 3100, A01N 3108, A01N 2534, A61F 606
Patent
active
060839953
DESCRIPTION:
BRIEF SUMMARY
This Application is a 371 continuation of PCT/GB96/00928 filed Apr. 18, 1996 which claims priority from British Application 9507883.8 filed Apr. 18, 1995.
The present invention relates to the use of formulations of 2,4-dichlorobenzyl alcohol (or 2,4 DCBA) and amylmetacresol (or AMC) in the treatment or prevention of Human Immunodeficiency Virus (HIV) viral infections.
HIV infections are now found in every country in the world and the most important method of transmission is sexual. The virus is present as free virus particles or as intracellular virions in monocyte cells in semen. The virus is thereby transmitted relatively easily from male to female or male to male. Alternatively, in an infected female, virus either free or cell bound is found in fluid in the vagina.
Existing antivirals have been found which inhibit important enzymes of the virus such as reverse transcriptase (RT), protease or integrase. The first clinically used drug namely AZT (or zidovudine, Retrovir.TM.), inhibits the virus RT enzyme. However, AZT does not represent a cure of infection and has not been demonstrated to prevent person to person spread. Indeed one of the clinical problems with the drug, apart from toxicity, is the emergence of drug resistant virus and the actual spread of the drug resistant virus in the community. A new approach against HIV is therefore to search for novel compounds which may destroy or inactivate free virus and/or cell associated virus directly on contact. These are so-called virucidal compounds. Such molecules have been described in the past (Oxford et al in App. Microbiology 21 606-610 (1971)), but have been little investigated recently.
Since the HIV virion is surrounded by a lipid bilayer it would be logical to test detergent like molecules for their ability to disrupt and dissolve the lipid membrane of the virus. For example the non-ionic surfactant nonoxynol-9 has been used in clinical practice as a spermicide and has direct anti-HIV activity (Malkovsky et al in The Lancet 645 (1988)). However, it has little selective anti-HIV effect and because it causes toxicity and cell destruction following application to the vagina its use may actually enhance infection with HIV (Kreiss et al in J.A.M.A. 268 477-482 (1992)).
The compound 2,4-dichlorobenzyl alcohol is known as an antiseptic agent i.e. as an antibacterial and antifungal agent, see for example Martindale "The Extra Pharmacopoeia" 28th edition, page 561, The Pharmaceutical Press (1982). Amylmetacresol or 6-pentyl-m-cresol is also known as a disinfectant used in mouth-washes or lozenges in combination with 2,4-dichlorobenzyl alcohol to treat mouth infections, see for example Martindale "The Extra Pharmacopoeia" 28th edition, page 549, The Pharmaceutical Press (1982). An antiseptic is defined in The Concise Oxford Dictionary (Oxford University Press, Oxford (1982)) as an agent which counters the development of sepsis, especially by preventing the growth of bacteria. Sepsis is defined in Black's Medical Dictionary (A & C Black, London (1990)) as poisoning by the products of the growth of micro-organisms in the body, and the general symptoms which accompany it are those of inflammation. Neither 2,4-dichlorobenzyl alcohol or amylmetacresol has previously been shown to demonstrate anti-viral or anti-retroviral activity and, in particular, anti-HIV activity.
Unexpectedly it has now been discovered that a formulation of 2,4-dichloroberzyl alcohol and amylmetacresol has anti-retroviral activity and causes inactivation of HIV infectivity.
According to the present invention there is provided the use of a composition comprising 2,4-dichlorobenzyl alcohol and amylmetacresol in the preparation of a medicament for the treatment or prevention of HIV viral infections.
In a particularly preferred embodiment of the present invention there is provided the use of a Strepsil.TM.-like formulation of 2,4-dichlorobenzyl alcohol and amylmetacresol in the preparation of a medicament for the treatment or prevention of HIV viral infections.
The pharmaceutical composition may
REFERENCES:
Dr. W. Forth et al., Allg. und spezielle Pharmakologie und Toxikologie, 1983, Bibliographisches Institute Mannheim (translation).
Merck Index 10th Ed #8756+634, 1984.
The Boots Company PLC
Travers Russell
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