Penetration of orally administered prulifloxacin into human lung tissue.

Objective: To evaluate the distribution in lung tissue of ulifloxacin, the active metabolite of prulifloxacin, a new once-daily fluoroquinolone administered orally in a single 600mg dose.

Design: Open-label, randomised study.

Patients: Twenty-seven patients (25 males, 2 females; mean age 65.

Prulifloxacin: in vitro (HERG current) and in vivo (conscious dog) assessment of cardiac risk.

Prulifloxacin, a new thiazeto-quinoline derivative with antibiotic properties, was evaluated for cardiac risk both in vitro on the ether-à-go-go-related gene (HERG) K+ channel, and in vivo in the conscious dog monitored by telemetry. HERG current was measured from stably transfected human embryonic kidney (HEK) 293 cells by means of the patch-clamp technique. Application of AF 3013, the active metabolite of prulifloxacin, produced only minor reduction of HERG current amplitude (tail current=-40 mV), producing a maximum blockade of 12.

Double-blind randomized study of lonidamine and radiotherapy in head and neck cancer.

Purpose: Preclinical studies showed lonidamine to potentiate the effects of x-irradiation by inhibiting the repair of potentially lethal damage. This Phase III double blind, placebo-controlled study was performed to evaluate whether lonidamine can increase the tumor control of radiotherapy in the treatment of advanced head and neck cancer without any synergistic toxic effects on the exposed normal tissues.

Methods And Materials: Ninety-seven patients with Stages II-IV squamous cell carcinoma of the head and neck were enrolled.

Phase II study of lonidamine in non-small cell lung cancer: final report.

Lonidamine (LND) is a new anti-cancer drug which interferes with the energy-yielding processes of tumour cells without affecting DNA replication. A total of 69 previously untreated patients with non-small cell lung cancer (NSCLC) entered this study. LND was given orally as a single agent at doses ranging from 450 to 900 mg day-1 until tumour progression (2 to greater than or equal to 1,402 days).

The potential role of lonidamine (LND) in the treatment of malignant glioma. Phase II study.

Up-to-date unsatisfactory results obtained in multimodality treatments of malignant glioma have prompted the research of new therapeutic modalities with 'unconventional' modes of action. Lonidamine (LND) is a drug which reduces aerobic glycolytic activity in both human and experimental tumors. This effect mainly depends on the inhibition of mitochondrially-bound hexokinase (HK) which is present in large amounts in malignant cells.