ArQule's ARQ 501 data shows clinical tolerability, signs of antitumor activity

By Elaine Rigoli

Tampa, Fla., June 15 - ArQule, Inc. announced data from two phase 1b combination therapy trials, one with ARQ 501 and docetaxel and one with ARQ 501 and gemcitabine, that support previously announced findings demonstrating clinical tolerability, favorable pharmacokinetics and promising signs of antitumor activity in cancer patients with a range of advanced solid tumors who had failed prior treatments with chemotherapy.

The objectives of ARQ 501 and docetaxel study were to determine the maximum tolerated dose, safety and tolerability, pharmacokinetics and preliminary antitumor activity of the combination of ARQ 501 and docetaxel. All patients enrolled in the study had failed prior courses of chemotherapy.

The data demonstrated the clinical tolerability and favorable pharmacokinetics of ARQ 501 in combination with docetaxel, including no alteration of docetaxel pharmacokinetic parameters.

The most common adverse events were anemia (81%) and neutropenia (68%), similar to those associated with docetaxel monotherapy, according to a news release.

Of note, eight patients with ovarian cancer were treated in the study, four with each dosing regimen.

Two of the four who received the first regimen achieved near normalization of CA-125 levels and reduction in tumor burden.

Four of the four patients who received the second regimen achieved a best response of stable disease or better (13+ - 27 weeks).

Based on these findings, combined with preclinical data, a regimen of weekly administration of 450 mg per meter squared of ARQ 501 is expected to be used in the company's phase 2 trial with ARQ 501 and a taxane in patients with ovarian cancer.

The objectives of the ARQ 501 and gemcitabine phase 1b study were to determine the maximum tolerated dose, safety and tolerability, pharmacokinetics and preliminary antitumor activity of this combination therapy in patients with advanced solid tumors. All patients enrolled in the study had failed prior courses of chemotherapy.

ARQ 501 was administered once weekly for all cycles of treatment, 30 minutes after the end of the gemcitabine infusion. Gemcitabine was administered once weekly for the first four weeks of cycle 1 and then three out of four weeks for each successive cycle.

A total of 36 patients have been enrolled in this study, with 34 receiving the combination regimen.

Of these, 26 patients were evaluable for efficacy, defined as having completed eight weeks of study and one post-baseline tumor assessment.

Of these, 14 patients (54%) achieved a response of stable disease or better, ranging from eight to 33 weeks, including one minor response in a patient with colorectal cancer who achieved a 28% reduction in tumor burden over 33 weeks on study.

A recommended phase 2 regimen of 400 mg/m2 of ARQ 501 in combination with gemcitabine has been determined in this study, the release said.

ArQule is a biotechnology company located in Woburn, Mass.

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