Prodrugs for oral administration containing taxol or substituted taxol covalently bound to a phospholipid
US5484809A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Dec 14, 1994 |
| Grant date | Jan 16, 1996 |
| Priority date | — |
| Expiry date | Dec 14, 2014 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07H19/16
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The oral delivery of many classes of drugs is facilitated by converting drugs having suitable functional groups to 1-O-alkyl-, 1-O-acyl-, 1-S-acyl, and 1-S-alkyl-sn-glycero-3-phosphate derivatives. The method confers the ability to be absorbed through the digestive tract to drugs that are not orally bioavailable in the non-derivatized state, and enhances the effectiveness of drugs that are poorly absorbed or rapidly eliminated. The method provides orally bioavailable lipid prodrugs of zaxol and taxol-related compounds. Potency of the lipid prodrugs is comparable to that of the corresponding nonderivatized drugs. In a preferred embodiment, taxol or substituted taxol is covalently bound to a phospholipid.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.