Paclitaxel-hyaluronic acid conjugate in the treatment of non-muscle invasive bladder cancer
AssigneeFidia Farmaceutici S.P.A.
InventorsGiorgio MOSCONI, Daniela JABES, Carlo PIZZOCARO
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Abstract
A pharmaceutical composition is described, essentially consisting of the paclitaxel prodrug associated with pharmacologically acceptable diluents/excipients, for use in the treatment of non-muscle invasive bladder cancer (NMIBC) by means of intravesical instillations according to a single weekly dose of 600 mg of said prodrug, or two weekly doses equal to a total of 1,200 mg, for 12 or 6 consecutive weeks of treatment. The paclitaxel prodrug used was prepared according to an indirect synthesis process between molecules of hyaluronic acid (HA) and paclitaxel by introducing a spacer (4-bromobutyric acid) between the hyaluronic acid and chemotherapeutic agent.
Claims11
A method of treating non-muscle invasive bladder cancer (NMIBC) by intravesical instillation, which comprises administering to a patient in need thereof a pharmaceutical composition comprising a paclitaxel prodrug associated with pharmaceutically acceptable diluents/excipients,
- wherein the pharmaceutical composition is administered as,
- a) a single weekly dose of 600 mg for 12 consecutive weeks of treatment;
- or
- b) a double weekly dose for a total of 1,200 mg of said composition per week for 6 consecutive weeks of treatment, and
- wherein the paclitaxel prodrug consists of a conjugate between paclitaxel and hyaluronic acid by means of 4-bromobutyric acid, said HA being bound indirectly to the paclitaxel through the ester bond between the carboxyl of HA and the 4-bromobutyric acid spacer in turn bound with an ester bond through its carboxyl to the hydroxyl group of the carbon in C2′ of paclitaxel, with a derivatization degree within the range of 18-21% weight/weight.
Dependencies are inferred from the claim text.