title: Single- and multiple dose pharmacokinetics of lonidamine in patients suffering from non-small-cell lung cancer.
abstract: Pharmacokinetic studies of lonidamine (1-[2,4-dichlorobenzyl]- 1H- indazole- 3-carboxylic acid, Doridamina: CAS 50264-69-2) in humans showed a wide variation of the plasma concentration-time profiles following a single peroral dose of 300 mg (Cmax between 6.5 and 40.9 micrograms/ml, tmax between 0.75 and 5.5 h). In order to investigate single and multiple dose pharmacokinetics after peroral administration of this chemotherapeutic compound, a study was performed involving 12 patients with non-small-cell malignancies of the lungs. Plasma and urinary concentration profiles were analyzed for determination of the pharmacokinetic parameters for lonidamine after single dose administration and in the steady state. In addition, age dependency and the presence of liver induction or inhibition was evaluated. Results indicate that steady state was reached after 2 dosing intervals of 12 h and no changes in liver metabolism or age dependent pharmacokinetics could be revealed after 4 days of multiple dose treatment.
authors.affiliation: Department of Pneumology, Centre for Pneumology and Thoracic Surgery, Krankenhaus Grosshansdorf, Fed. Rep. of Germany.
authors.forename: U
authors.initials: U
authors.lastname: Gatzemeier
authors.forename: H
authors.initials: H
authors.lastname: Toomes
authors.forename: R
authors.initials: R
authors.lastname: Picollo
authors.forename: V
authors.initials: V
authors.lastname: Christoffel
authors.forename: P W
authors.initials: PW
authors.lastname: Lücker
authors.forename: J
authors.initials: J
authors.lastname: Ulmer
mesh_terms: D000328:Adult; D000368:Aged; D000375:Aging / Q000378:metabolism; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000493:pharmacokinetics* / Q000627:therapeutic use; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy / Q000378:metabolism*; D002849:Chromatography, Gas; D002851:Chromatography, High Pressure Liquid; D005260:Female; D006801:Humans; D007191:Indazoles / Q000009:adverse effects / Q000493:pharmacokinetics* / Q000627:therapeutic use; D008099:Liver / Q000378:metabolism; D008175:Lung Neoplasms / Q000188:drug therapy / Q000378:metabolism*; D008297:Male; D008875:Middle Aged
chemical_list: D000970:Antineoplastic Agents; D007191:Indazoles; C016371:lonidamine