Phase I and clinical pharmacologic evaluation of Lonidamine in patients with advanced cancer.
Lonidamine was studied in 31 patients with different types of advanced cancer. With one exception, patients were pretreated. Lonidamine was given at 6 dosage levels from 180 to 520 mg/m2 for at least 28 days. No toxicity on hematopoietic function was observed. Side effects consisted mostly in musculoskeletal discomfort, testicular pain in males and a reversible ototoxicity. In 2 patients conjunctivitis and photophobia occurred. Plasma Lonidamine levels were measured in 14 patients. Peak concentrations were observed from 1 to 2 h after administration and ranged from 3 to 35 micrograms/ml. Objective antitumoral effects were observed in only 2 patients with mycosis fungoides; a 3rd patient with mycosis fungoides was considered to have stable disease.
D000293:Adolescent; D000328:Adult; D000368:Aged; D000970:Antineoplastic Agents / Q000009:adverse effects; D004341:Drug Evaluation; D005260:Female; D006410:Hematopoiesis / Q000187:drug effects; D006801:Humans; D007191:Indazoles / Q000009:adverse effects / Q000627:therapeutic use*; D008297:Male; D008875:Middle Aged; D009132:Muscles / Q000187:drug effects; D009369:Neoplasms / Q000188:drug therapy*; D011720:Pyrazoles / Q000627:therapeutic use*; D013737:Testis / Q000187:drug effects
D000970:Antineoplastic Agents; D007191:Indazoles; D011720:Pyrazoles; C016371:lonidamine