UC38, A NOVEL, NON-NUCLEOSIDE AGENT READY FOR CLINICAL EVALUATION AGAINST THE HUMAN IMMUNODEFICIENCY VIRUS (HIV) (MEETING ABSTRACT) NLM AIDSLINE Important note: Information in this article was accurate in 1992. The state of the art may have changed since the publication date.

Click here to return to AIDSLINE main menu
DonateNow
Print this Article


UC38, A NOVEL, NON-NUCLEOSIDE AGENT READY FOR CLINICAL EVALUATION AGAINST THE HUMAN IMMUNODEFICIENCY VIRUS (HIV) (MEETING ABSTRACT)

Proc Annu Meet Am Assoc Cancer Res; 33:A2918 1992. Unique Identifier : AIDSLINE ICDB/92685451
Boyd MR; Stinson SF; McMahon JB; Shoemaker RH; Vistica DT; Buckheit RR; Weislow OS; Brouwer WG; Felauer EE; Schultz RJ; et al; Developmental Therapeutics Program (DTP), NCI, Bethesda, MD 20892

Abstract: In 1988, the NCI DTP implemented a high-capacity (greater than 20,000 cpds/yr) screen to support the empirical discovery of new leads active against HIV. One new chemotype discovered was oxathiin carboxanilide (OC; 'Uniroyal Sr;' Proc Natl Acad Sci 88:6740-4, 1991). Through extensive SAR studies, a surprisingly simple derivative (UC38; 'Uniroyal Jr') has been identified with improved activity and solubility characteristics, limitations which had precluded development of OC as a clinical candidate. UC38 and OC prevent HIV reproduction and cytopathicity in vitro by a common mechanism and have the same range of action. Both OC and UC38 are susceptible to extensive hydrolytic degradation in vitro and in vivo; yet, in vivo concentrations of UC38, which could be achieved and maintained after sc or po administration of a sesame oil solution to hamsters, were many-fold in excess of the in vitro effective concentration. Therefore, preclinical development of UC38 was undertaken. INDA filing is anticipated in early 1992. UC38 will thus represent the first discovery to reach clinical trials from the DTP effort in an exemplary government/industry collaboration.
Keywords: Animal Antiviral Agents/*PHARMACOLOGY Cytopathogenic Effect, Viral Drugs, Investigational/*PHARMACOLOGY Hamsters HIV/*DRUG EFFECTS/PHYSIOLOGY Virus Replication/DRUG EFFECTS ABSTRACTKWDanimalantiviralagents/KWDpharmacologycytopathogeniceffect,viraldrugs,investigational/KWDpharmacologyhamstershiv/KWDdrugeffects/physiologyvirusreplication/drugeffectsabstract
921030
M92A1033

Copyright © 1992 - National Library of Medicine. Reproduced under license with the National Library of Medicine, Bethesda, MD.

AEGiS is a 501(c)3, not-for-profit, tax-exempt, educational corporation. AEGiS is made possible through unrestricted funding from Boehringer Ingelheim, Bridgestone/Firestone Charitable Trust, Bristol-Myers Squibb Company, Elton John AIDS Foundation, Gill Foundation, the National Library of Medicine, Quest Diagnostics, Roche and Trimeris, and donations from users like you. Always watch for outdated information. This article first appeared in 1992. This material is designed to support, not replace, the relationship that exists between you and your doctor.

AEGiS presents published material, reprinted with permission and neither endorses nor opposes any material. All information contained on this website, including information relating to health conditions, products, and treatments, is for informational purposes only. It is often presented in summary or aggregate form. It is not meant to be a substitute for the advice provided by your own physician or other medical professionals. Always discuss treatment options with a doctor who specializes in treating HIV.

Copyright ©1980, 1992. AEGiS. All materials appearing on AEGiS are protected by copyright as a collective work or compilation under U.S. copyright and other laws and are the property of AEGiS, or the party credited as the provider of the content. .