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Water soluble paclitaxel prodrugs
| Details |
Inventors: Li, Chun; Wallace, Sidney; Yu, Dong-Fang; Yang, David J.;
Assignee: PG-TXL Company, L. P. (Houston, TX)
Primary Examiner: Dees; Jose' G.
Assistant Examiner: Hartley; Michael G.
Attorney, Agent or Firm: Arnold White & Durkee
Disclosed are water soluble compositions of paclitaxel and docetaxel formed by conjugating the paclitaxel or docetaxel to a water soluble chelator, polyethylene glycol or polymer such as poly (1-glutamic acid) or poly (1-aspartic acid). Also disclosed are methods of using the compositions for treatment of tumors, auto-immune disorders such as rheumatoid arthritis and for prediction of paclitaxel uptake by tumors and radiolabeled DTPA-paclitaxel tumor imaging. Other embodiments include the coating of implantable stents for prevention of restenosis. |
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DETAILED DESCRIPTION The present invention seeks to overcome these and other drawbacks inherent in the prior art by providing compositions comprising a chemotherapeutic and antiangiogenic drug, such as paclitaxel or docetaxel conjugated to a water soluble polymer such as a polyglutamic acid or a polyaspartic acid, for example, or to a water soluble metal chelator.
These compositions are shown herein to be surprisingly effective as anti-tumor agents against exemplary tumor models, and are expected to be at least as effective as paclitaxel or docetaxel against any of the diseases or conditions for which taxanes or taxoids are known to be effective.
The compositions of the invention provide water soluble taxoids to overcome the drawbacks associated with the insolubility of the drugs themselves, and also provide the advantages of controlled release so that tumors are shown herein to be eradicated in animal models after a single intravenous administration.
The methods described herein could also be used to make water soluble polymer conjugates of other therapeutic agents, contrast agents and drugs, including etopside, teniposide, fludarabine, doxorubicin, daunomycin, emodin, 5-fluorouracil, FUDR, estradiol, camptothecin, retinoic acids, verapamil, epothilones and cyclosporin.
In particular, those agents with a free hydroxyl group would be conjugated to the polymers by similar chemical reactions as described herein for paclitaxel.
Such conjugation would be well within the skill of a routine practitioner of the chemical art, and as such would fall within the scope of the claimed invention.
Those agents would include, but would not be limited to etopside, teniposide, camptothecin and the epothilones.
As used herein, conjugated to a water soluble polymer means the covalent bonding of the drug to the polymer or chelator.
It is also understood that the water soluble conjugates of the present invention may be administered in conjunction with other drugs, including other anti-tumor or anti-cancer drugs
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