@entity18152 ( @entity18152 ), a new @entity2353 antimetabolite, was evaluated in a phase I trial involving @entity1 with refractory @entity5 . The drug was administered i.v. as a 10-min infusion daily for 5 consecutive days repeated at 3-week intervals. The dose ranged from 550 to 3300 mg/sq m/day. Seventeen @entity1 received 23 courses and were evaluable for @entity137 . The maximally tolerated dose was 2200 mg/sq m/day. The major dose-limiting @entity137 were nonhematological. @entity2359 , including @entity10 , drowsiness, and @entity146 , was common and was the principal dose-limiting @entity137 at the higher doses. Severe @entity925 were also dose limiting in one @entity1 . Other side effects were mild, reversible elevations in serum transaminases; @entity390 , @entity391 , and @entity294 ; mild @entity101 ; @entity1282 ; and exfoliative @entity1909 of the hands and feet. Myelotoxicity was not significant. The pharmacokinetics of @entity18152 was studied in 16 @entity1 . Plasma disappearance was triphasic with half-lives of 9.7 min, 1.6 h, and 5.5 h. Clearance was dose related, ranging from 120 ml/min/sq m at 550 mg/sq m/day to 70 ml/min/sq m at 3300 mg/sq m/day. The primary route of elimination was renal with 85% of the drug recoverable in the urine as the parent compound in the 24 h following administration.

Pediatric phase I trial and pharmacokinetic study of @entity18152 ( XXXX ).

@entity1 :: ('9606', 'Species') :: ['children', 'patients', 'patient'] @entity2353 :: ('CHEBI:33838', 'Chemical') :: ['nucleoside'] @entity137 :: ('MESH:D064420', 'Disease') :: ['toxicity', 'toxicities'] @entity390 :: ('MESH:D009325', 'Disease') :: ['nausea'] @entity101 :: ('MESH:D006973', 'Disease') :: ['hypertension'] @entity146 :: ('MESH:D001523', 'Disease') :: ['irritability'] @entity18152 :: ('MESH:C033706', 'Chemical') :: ['2-beta-D-ribofuranosylthiazole-4-carboxamide', 'tiazofurin', 'Tiazofurin'] @entity5 :: ('MESH:D009369', 'Disease') :: ['cancers'] @entity294 :: ('MESH:D003967', 'Disease') :: ['diarrhea'] @entity391 :: ('MESH:D014839', 'Disease') :: ['vomiting'] @entity1282 :: ('MESH:D003680', 'Disease') :: ['dysphagia'] @entity10 :: ('MESH:D006261', 'Disease') :: ['headache'] @entity925 :: ('MESH:D063806', 'Disease') :: ['myalgias'] @entity1909 :: ('MESH:D003872', 'Disease') :: ['dermatitis'] @entity2359 :: ('MESH:D020258', 'Disease') :: ['Neurotoxicity']
@entity18152 :: (MESH:C033706,Chemical) :: ['NSC 286193']
