This is an open-label study being conducted to determine the metabolism and physiological disposition of radiolabeled LY2603618 after a single dose in patients with advanced and/or metastatic solid tumors. After a minimum 7-day washout period following the carbon-14-labeled LY2603618 (\[\^14C\]LY2603618) dose, patients will be allowed to continue to receive continued access to LY2603618 in combination with pemetrexed or gemcitabine as outpatients.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
3
Administered intravenously
Administered intravenously
Administered intravenously
For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician.
Bruderholz, Switzerland
Urinary and Fecal Excretion of LY2603618 Radioactivity Over Time Expressed as a Percentage of the Total Radioactive Dose Administered
Urinary and fecal excretion samples from each participant were measured by liquid scintillation counting. The radioactive counts detected in urine and fecal samples were each divided by the theoretical radioactive count in the total radioactive dose administered and multiplied by 100% to arrive at a percentage of total radioactive dose excreted in urine and feces.
Time frame: 0 to 6 hours, 6 to 12, 12 to 24, 24 to 48, 48 to 72 and 72 to 96 hours post-dose
Plasma Pharmacokinetics of LY2603618: Maximum Observed Drug Concentration (Cmax)
Plasma LY2603618 Cmax following a single dose on Day 1.
Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose
Plasma Pharmacokinetics of Radioactivity: Maximum Observed Drug Concentration (Cmax)
Plasma radioactivity Cmax \[nanogram equivalents per milliliter (ng Eq/mL)\] following a single dose on Day 1.
Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose
Plasma Pharmacokinetics of LY2603618: Area Under the Concentration Time Curve From Time Zero to Infinity [AUC(0-infinity)]
Plasma LY2603618 AUC(0-infinity) following a single dose on Day 1.
Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose
Plasma Pharmacokinetics of Radioactivity: Area Under the Concentration Time Curve From Time Zero to Infinity [AUC(0-infinity)]
Plasma radioactivity AUC(0-infinity) \[nanogram equivalents\*hours per milliliter (ng Eq\*h/mL)\] following a single dose on Day 1.
Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.
Plasma Pharmacokinetics of LY2603618: Area Under the Concentration Time Curve From Time Zero to Time t [AUC(0-tlast)]
Plasma LY2603618 AUC(0-tlast) where tlast is the last time point with a measurable concentration following a single dose on Day 1.
Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose
Plasma Pharmacokinetics of Radioactivity: Area Under the Concentration Time Curve From Time Zero to Time t [AUC(0-tlast)]
Plasma radioactivity AUC(0-tlast) \[nanogram equivalents\*hours per milliliter (ng Eq\*h/mL)\] where tlast is the last time point with a measurable concentration following a single dose on Day 1.
Time frame: 0, 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose
Relative Abundance of LY2603618 and the Metabolites of LY2603618 in Urine
Relative abundance was expressed as the percentage of the dose of study drug administered and calculated as %=\[amount of LY2603618 or its metabolites excreted/amount of radioactive dose administered\]\*100.
Time frame: Day 1 through 7 days postdose
Relative Abundance of LY2603618 and the Metabolites of LY2603618 in Feces
Relative abundance was expressed as the percentage of the dose of study drug administered and calculated as %=\[amount of LY2603618 or its metabolites excreted/amount of radioactive dose administered\]\*100.
Time frame: Day 1 through 7 days postdose
The Number of Participants With a Tumor Response
Tumor responses were followed and measured according to Response Evaluation Criteria In Solid Tumors (RECIST) criteria. Complete response was defined as the disappearance of all target and non-target lesions and any pathological lymph nodes (whether target or non-target) must have reduction in short axis to \<10 millimeter (mm) and normalization of tumor marker level of non-target lesions. Partial response was defined as at least a 30% decrease in sum of longest diameter of target lesions. Progressive disease was defined as at least 20% increase in sum of longest diameter of target lesions and minimum 5 mm increase over nadir; Stable disease was defined as small changes that did not meet above criteria.
Time frame: Baseline through study completion [Cycle 5 (28 days/cycle) and 21-day safety follow-up]