Absolute 1010 Absolute 14 /14 Abs BA ~ 43%; PIC:IV bioavailability 250:50 mg. (sd) 1008 BE (fasted) 24/24 BE shown 250 mg – – (250 mg) PIC vs IRT doses. 1011 BE (fasted) - CIC 36/35 BE shown 250 mg – (250 mg) vs IRT 36/35 doses BE shown 250 – BE (fasted) - CIC mg doses vs PIC Food Effect 1011 Food Effect - CIC Food decreases BA by (250 mg) fast/fed ~ 14%. Mass balance 1009 14C 6/6 PKs and ADME (250 mg) radiolabelled investigated. crizotinib PK 1015 Ketoconazole / 15 Systemic exposure Crizotinib increased. Interaction Patients with advanced cancer single and multiple dose studies – Single and 1001 Phase I, Comprehensive PK multiple single-arm data in patients with dose; efficacy and advanced cancer; safety in dose-escalation Various qd patients with (n=37), and RP2D and bd advanced cohorts (n=171; 250 Asian vs cancer. mg bd) including non-Asian; ALK+ NSCLC (n=119). PK interaction; Food effect Trough 1005 Phase II, Limited data only. Only1 arm, efficacy and safety in patients with ALK+ advanced NSCLC.
Absolute (sd) 1010 Absolute bioavailability 14 /14 Abs BA ~ 43%; PIC:IV 250:50 mg. (250 mg) 1008 BE (fasted) – PIC vs IRT 24/24 BE shown – 250 mg doses. (250 mg) 1011 BE (fasted) - CIC vs IRT BE (fasted) - CIC vs PIC 36/35 36/35 BE shown – 250 mg doses BE shown – 250 mg doses Food Effect (250 mg) 1011 Food Effect - CIC fast/fed Food decreases BA by ~ 14%. Mass balance (250 mg) 1009 14C radiolabelled crizotinib 6/6 PKs and ADME investigated. PK Interaction 1015 Ketoconazole / Crizotinib 15 Systemic exposure increased. Patients with advanced cancer – single and multiple dose studies Single and multiple dose; Various qd and bd Asian vs non-Asian; PK interaction; Food effect 1001 Phase I, single-arm efficacy and safety in patients with advanced cancer. Comprehensive PK data in patients with advanced cancer; dose-escalation (n=37), and RP2D cohorts (n=171; 250 mg bd) including ALK+ NSCLC (n=119). Trough Only1 1005 Phase II, efficacy and safety in patients with ALK+ advanced NSCLC. Limited data only. arm,
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