Preclinical studies of alkylureas as anti-HIV-1 contraceptive

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

The HIV-I epidemic continues to spread at a rate ofover 15,000 new cases daily. HIV-I transmission through heterosexual contact became the dominant risk for women globally. About half of the over 40 million HIV- I infected individuals worldwide are now women. The lack of empowerment of women is the fundamental cause for the rampant spread of HIV-1 inwomen. Topical microbicides applied intravaginally offer an option for female-initiated HIV-1 prevention. There is an urgent need to develop microbicides with and without contraceptive qualities to also address socio-cultural settings where the woman's status is linked to fertility. A safe and efficacious anti-HIV-1 vaginal formulation is not yet available though a large number of candidates are in preclinical or clinical studies. Presently marketed topical microbicides are by and large toxic and damage the vaginal mucosa with frequent use. The microbicidal system of alkylureas evaluated here lends itself to contraceptive and non-contraceptive anti- HIV-1 formulations. Alkylureas are agents that irreversibly disrupt free and intracellular HIV-1, have a wide margin of safety and are spermicidal above their virucidal concentration without any mucosal toxicity. Butylurea, the lead compound is also effective against other sexually transmitted diseases (STDs) while sparing the normal vaginal flora. Alkylureas with longer alkyl chains still have to be explored and may have a greater selective microbicidality.

Original languageEnglish (US)
Pages (from-to)3769-3778
Number of pages10
JournalCurrent Pharmaceutical Design
Volume11
Issue number29
DOIs
StatePublished - 2005

Fingerprint

Contraceptive Agents
HIV-1
Local Anti-Infective Agents
Women's Rights
Poisons
Heterosexuality
Sexually Transmitted Diseases
Anti-Infective Agents
Fertility
Mucous Membrane
Safety

Keywords

  • Alkylureas
  • Butylurea
  • HIV-1
  • Vaginal microbicide

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Preclinical studies of alkylureas as anti-HIV-1 contraceptive. / Rubinstein, Arye.

In: Current Pharmaceutical Design, Vol. 11, No. 29, 2005, p. 3769-3778.

Research output: Contribution to journalArticle

@article{54965def8f7342fb8a9f7f667100c3ab,
title = "Preclinical studies of alkylureas as anti-HIV-1 contraceptive",
abstract = "The HIV-I epidemic continues to spread at a rate ofover 15,000 new cases daily. HIV-I transmission through heterosexual contact became the dominant risk for women globally. About half of the over 40 million HIV- I infected individuals worldwide are now women. The lack of empowerment of women is the fundamental cause for the rampant spread of HIV-1 inwomen. Topical microbicides applied intravaginally offer an option for female-initiated HIV-1 prevention. There is an urgent need to develop microbicides with and without contraceptive qualities to also address socio-cultural settings where the woman's status is linked to fertility. A safe and efficacious anti-HIV-1 vaginal formulation is not yet available though a large number of candidates are in preclinical or clinical studies. Presently marketed topical microbicides are by and large toxic and damage the vaginal mucosa with frequent use. The microbicidal system of alkylureas evaluated here lends itself to contraceptive and non-contraceptive anti- HIV-1 formulations. Alkylureas are agents that irreversibly disrupt free and intracellular HIV-1, have a wide margin of safety and are spermicidal above their virucidal concentration without any mucosal toxicity. Butylurea, the lead compound is also effective against other sexually transmitted diseases (STDs) while sparing the normal vaginal flora. Alkylureas with longer alkyl chains still have to be explored and may have a greater selective microbicidality.",
keywords = "Alkylureas, Butylurea, HIV-1, Vaginal microbicide",
author = "Arye Rubinstein",
year = "2005",
doi = "10.2174/138161205774580697",
language = "English (US)",
volume = "11",
pages = "3769--3778",
journal = "Current Pharmaceutical Design",
issn = "1381-6128",
publisher = "Bentham Science Publishers B.V.",
number = "29",

}

TY - JOUR

T1 - Preclinical studies of alkylureas as anti-HIV-1 contraceptive

AU - Rubinstein, Arye

PY - 2005

Y1 - 2005

N2 - The HIV-I epidemic continues to spread at a rate ofover 15,000 new cases daily. HIV-I transmission through heterosexual contact became the dominant risk for women globally. About half of the over 40 million HIV- I infected individuals worldwide are now women. The lack of empowerment of women is the fundamental cause for the rampant spread of HIV-1 inwomen. Topical microbicides applied intravaginally offer an option for female-initiated HIV-1 prevention. There is an urgent need to develop microbicides with and without contraceptive qualities to also address socio-cultural settings where the woman's status is linked to fertility. A safe and efficacious anti-HIV-1 vaginal formulation is not yet available though a large number of candidates are in preclinical or clinical studies. Presently marketed topical microbicides are by and large toxic and damage the vaginal mucosa with frequent use. The microbicidal system of alkylureas evaluated here lends itself to contraceptive and non-contraceptive anti- HIV-1 formulations. Alkylureas are agents that irreversibly disrupt free and intracellular HIV-1, have a wide margin of safety and are spermicidal above their virucidal concentration without any mucosal toxicity. Butylurea, the lead compound is also effective against other sexually transmitted diseases (STDs) while sparing the normal vaginal flora. Alkylureas with longer alkyl chains still have to be explored and may have a greater selective microbicidality.

AB - The HIV-I epidemic continues to spread at a rate ofover 15,000 new cases daily. HIV-I transmission through heterosexual contact became the dominant risk for women globally. About half of the over 40 million HIV- I infected individuals worldwide are now women. The lack of empowerment of women is the fundamental cause for the rampant spread of HIV-1 inwomen. Topical microbicides applied intravaginally offer an option for female-initiated HIV-1 prevention. There is an urgent need to develop microbicides with and without contraceptive qualities to also address socio-cultural settings where the woman's status is linked to fertility. A safe and efficacious anti-HIV-1 vaginal formulation is not yet available though a large number of candidates are in preclinical or clinical studies. Presently marketed topical microbicides are by and large toxic and damage the vaginal mucosa with frequent use. The microbicidal system of alkylureas evaluated here lends itself to contraceptive and non-contraceptive anti- HIV-1 formulations. Alkylureas are agents that irreversibly disrupt free and intracellular HIV-1, have a wide margin of safety and are spermicidal above their virucidal concentration without any mucosal toxicity. Butylurea, the lead compound is also effective against other sexually transmitted diseases (STDs) while sparing the normal vaginal flora. Alkylureas with longer alkyl chains still have to be explored and may have a greater selective microbicidality.

KW - Alkylureas

KW - Butylurea

KW - HIV-1

KW - Vaginal microbicide

UR - http://www.scopus.com/inward/record.url?scp=27744581334&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=27744581334&partnerID=8YFLogxK

U2 - 10.2174/138161205774580697

DO - 10.2174/138161205774580697

M3 - Article

C2 - 16305511

AN - SCOPUS:27744581334

VL - 11

SP - 3769

EP - 3778

JO - Current Pharmaceutical Design

JF - Current Pharmaceutical Design

SN - 1381-6128

IS - 29

ER -