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Comparative Study
. 2001 Apr;12(4):305-13.
doi: 10.1097/00001813-200104000-00002.

A new prodrug of paclitaxel: synthesis of Protaxel

A L Seligson  1 , R C Terry, J C Bressi, J G Douglass 3rd, M Sovak
Affiliations
Comparative Study

A new prodrug of paclitaxel: synthesis of Protaxel

A L Seligson et al. Anticancer Drugs. 2001 Apr.

Abstract

2' and 7 Polyol carbonates of paclitaxel were synthesized and screened as potential paclitaxel prodrugs. Paclitaxel is released from 7-(2",3"-dihydroxypropylcarbonato) paclitaxel (Protaxel) at rates inversely proportional to pH, by an intramolecular cyclization. Compared to paclitaxel, maximum tolerated i.v. or i.p. doses (MTD) of Protaxel are about 2.5- to 3-fold higher; its efficacy is substantially higher in human cancer line xenografts in athymic mice, especially in prostate PC-3, breast MDA-MB 468 and ovary OVCAR-1.

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