title: Dendrimers as drugs: discovery and preclinical and clinical development of dendrimer-based microbicides for HIV and STI prevention.
abstract: Starpharma focuses on the use of dendrimers as drugs in their own right, in contrast to dendrimers as drug delivery vehicles or diagnostics. This contextual review describes how dendrimers offer a unique platform for exploring chemical diversity on the nanoscale and how the production of dendrimer libraries covering a diverse array of macromolecular structures can be used in drug discovery and development. Using Starpharma's work on the prevention of HIV and sexually transmitted infections (STIs) through the development of microbicide candidates as an example, the process from which SPL7013 emerged as a development candidate is described. Following a range of preclinical studies, Starpharma submitted an investigational new drug application (IND) for SPL7013 gel (VivaGel) to the United States Food and Drug Administration (FDA) in June 2003, the first such submission for a dendrimer-based drug. The first clinical trial under this IND was completed in 2004.
authors.affiliation: Starpharma Pty Limited, 75 Commercial Road, Melbourne, VIC 3004, Australia. tom.mccarthy@starpharma.com
authors.forename: Tom D
authors.initials: TD
authors.lastname: McCarthy
authors.forename: Peter
authors.initials: P
authors.lastname: Karellas
authors.forename: Scott A
authors.initials: SA
authors.lastname: Henderson
authors.forename: Michael
authors.initials: M
authors.lastname: Giannis
authors.forename: David F
authors.initials: DF
authors.lastname: O'Keefe
authors.forename: Graham
authors.initials: G
authors.lastname: Heery
authors.forename: Jeremy R A
authors.initials: JR
authors.lastname: Paull
authors.forename: Barry R
authors.initials: BR
authors.lastname: Matthews
authors.forename: George
authors.initials: G
authors.lastname: Holan
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D015195:Drug Design; D015658:HIV Infections / Q000517:prevention & control*; D006801:Humans; D046911:Macromolecular Substances / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D008958:Models, Molecular; D012749:Sexually Transmitted Diseases / Q000517:prevention & control*
chemical_list: D000900:Anti-Bacterial Agents; D019380:Anti-HIV Agents; D000998:Antiviral Agents; D046911:Macromolecular Substances