Imaging of drug accumulation as a guide to antitumor therapy

A method of determining the efficacy of an anti-tumor drug for treating solid tumors comprising:

• administering an anti-tumor drug labeled with a positron-emitter to a patient having a solid tumor;
• and
• imaging at least part of the patient by PET to measure accumulation of the labeled anti-tumor drug,
• wherein said anti-tumor drug is an insoluble taxane.

A method of measuring the effectiveness of modulators of cellular accumulation mechanisms in tumors comprising:

• administering an anti-tumor drug labeled with a positron-emitter to a patient;
• administering a modulator to the patient, and
• imaging at least part of the patient by PET to measure accumulation of the labeled anti-tumor drug,
• wherein said anti-tumor drug is an insoluble taxane;
• the accumulation of labeled anti-tumor drug is measured before and after administering the modulator to the patient;
• and
• the levels of anti-tumor drug accumulation before and after administering the modulator are compared.

A compound having the formula:

• wherein:
• R1 is selected from the group consisting of H, acetate and 11C-acetate;
• R2 is selected from the group of acetate and 11C-acetate;
• R3 is selected from the group consisting of benzoyl, 11C-benzoyl, —CO2C(CH3)3 and —11CO2C(CH3)3;
• and
• R4 selected from the group consisting of benzoyl, 11C-benzoyl;
• and
• wherein the compound contains at least one atom of 11C.

A method of measuring the accumulation of anti-tumor drugs by solid tumors comprising,

• administering an anti-tumor drug labeled with a positron-emitter to a patient having a solid tumor, and
• imaging at least part of the patient using PET;
• wherein the anti-tumor drug comprises a compound having the formula:
• wherein:
• R1 is selected from the group consisting of H and acetate;
• R2 is acetate;
• R3 is selected from the group consisting of benzoyl and —CO2C(CH3)3;
• and
• R4 is benzoyl,
• wherein the compound contains at least one atom of 11C.

A method of measuring the effectiveness of modulators of cellular accumulation mechanisms in tumors comprising:

• administering an anti-tumor drug labeled with a positron-emitter to a patient;
• administering a modulator to the patient, and
• imaging at least part of the patient by PET to measure accumulation of the labeled anti-tumor drug,
• wherein said anti-tumor drug is an insoluble taxane and the modulator affects tumor concentration of the anti-tumor drug or normal host cell concentration of the anti-tumor drug;
• the accumulation of labeled anti-tumor drug is measured before and after administering the modulator to the patient;
• and
• the levels of anti-tumor drug accumulation before and after administering the modulator are compared.