@entity21926 is a small molecule antiangiogenic agent that inhibits @entity7 ( @entity7 ) stimulation of the @entity319 @entity669 kinase receptor. In this Phase I dose escalation trial, a weekly dose schedule of @entity21926 was tested whereby an initial 5-day loading dose was followed by weekly maintenance infusions. The start dose was 20 mg/m(2) for the loading dose followed by 65 mg/m(2) for the weekly infusions. Dose escalations occurred at 33% until a final dose of 65 mg/m(2) (loading dose) and 190 mg/m(2) (weekly infusion) was obtained. Twenty-two @entity1 were treated at five dose levels; @entity5 types included gastrointestinal (8), breast (3), lung (4), @entity242 (2), and other (5). The most common serious drug-related @entity137 was @entity10 , often associated with @entity390 and @entity391 . Grade 1 and 2 @entity137 included @entity10 , @entity390 , @entity391 , @entity1395 , @entity158 at the infusion site, @entity3527 , change in voice, and fevers. Of 19 evaluable @entity1 , 4 obtained clinical benefit as defined by @entity5 regression (1) or disease stabilization for at least 12 weeks (3). Pharmacokinetic data revealed that the weekly infusion schedule prevented the reported 50-60% induction in @entity21926 clearance observed with either daily or twice weekly dosing. Higher baseline levels of urine @entity7 were observed in the 4 @entity1 who gained clinical benefit, suggesting this may be a useful marker for predicting response to anti- @entity7 therapies. Our results suggest that a weekly schedule of @entity21926 shows signs of biological activity and is well tolerated at doses up to 145 mg/m(2).

Results of a Phase I dose-escalating study of the antiangiogenic agent, @entity21926 , in XXXX with advanced @entity5 .

@entity1 :: ('9606', 'Species') :: ['patients'] @entity137 :: ('MESH:D064420', 'Disease') :: ['toxicity', 'toxicities'] @entity390 :: ('MESH:D009325', 'Disease') :: ['nausea'] @entity242 :: ('MESH:D012509', 'Disease') :: ['sarcoma'] @entity7 :: ('7422', 'Gene') :: ['vascular endothelial growth factor', 'VEGF'] @entity5 :: ('MESH:D009369', 'Disease') :: ['tumor'] @entity3527 :: ('MESH:D010689', 'Disease') :: ['phlebitis'] @entity391 :: ('MESH:D014839', 'Disease') :: ['vomiting'] @entity1395 :: ('MESH:D001247', 'Disease') :: ['asthenia'] @entity319 :: ('3791', 'Gene') :: ['KDR'] @entity21926 :: ('MESH:C116890', 'Chemical') :: ['SU5416'] @entity158 :: ('MESH:D010146', 'Disease') :: ['pain'] @entity10 :: ('MESH:D006261', 'Disease') :: ['headache'] @entity669 :: ('CHEBI:18186', 'Chemical') :: ['tyrosine']
@entity1 :: (9606,Species) :: ['patients']
