A Study to Look at How a Single Oral Dose of 14C-OSI-906 is Absorbed, Broken Down and Eliminated in the Body

NCT01529684 | Completed Phase 1

• 1 other identifier: OSI-906-104
• Study Type: interventional
• Target: 5
• Locations: 1 country
• Sites: 2

Brief Summary

The purpose of this study is to evaluate the pharmacokinetics, in particular the routes of excretion and extent of metabolism of OSI-906 after a single oral dose of 14C-labeled OSI-906. Subjects with Advanced Solid Tumors may participate and then continue into the Optional Treatment Phase.

Conditions

Advanced Solid Tumors; Pharmacokinetics of 14C-OSI-906

Keywords

oncology patients; Metabolic profile of 906; OSI-906; mass balance; Pharmacokinetics of 14C-OSI-906; Cancer, solid tumors; Absorption, Metabolism, and Excretion of OSI-906

Outcome Measures

Primary Outcomes (5)

• Radioactivity in whole blood and plasma

  Outcome measure for Part A: Area under the time concentration curve extrapolated to infinity (AUCinf), AUC from time of dosing to last quantifiable time point (AUClast), Maximum Plasma Concentration (Cmax), Time to maximum concentration (Tmax), Terminal half-life (t 1/2), Apparent Body Clearance after dosing (CL/F), and Apparent volume of distribution (Vz/F)

  Up to 10 days from time of receipt of 14C-labeled OSI-906

• Radioactivity ratio in blood/plasma

  Outcome Measure for Part A of OSI-906 distribution between cellular components and plasma

  Up to 10 days from time of receipt of 14C-labeled OSI-906

• Excretion ratio and cumulative excretion of radioactivity in urine and feces

  Outcome measure for Part A

  Up to 10 days from time of receipt of 14C-labeled OSI-906

• Composite of Pharmacokinetics of OSI-906 in plasma: AUC inf, AUC last, C max, t max, t 1/2, CL/F, and Vz/F

  Outcome measure for Part A

  Up to 10 days from time of receipt of 14C-labeled OSI-906

• Composite of Pharmacokinetics of OSI-906 in urine: Cumulative amount of drug excreted into urine, feces or bile up to collection time of last measurable concentration (Ae last), Renal Clearance (CL R), and percentage of dose excreted (Ae last%)

  Outcome measure for Part A

  Up to 10 days from time of receipt of 14C-labeled OSI-906

Secondary Outcomes (2)

• Metabolic Profile: Profiling of possible metabolites in OSI-906 plasma, urine, and feces

  Up to 10 days from time of receipt of 14C-labeled OSI-906

• Safety as assessed by recording adverse events, laboratory assessments and vital signs, and electrocardiograms (ECGs)

  For Part A: Days 1-10 and/or 30 days post treatment visit. For Part B: Treatment Period 1 (TP1) through 30 day post treatment visit (up to two years)

Study Arms (1)

OSI-906

EXPERIMENTAL

Two Parts: Part A: 14C-labeled OSI-906 Part B: (Optional) OSI-906 (non-labeled)

Drug: radio-labeled OSI-906; Drug: OSI-906

Interventions

radio-labeled OSI-906 DRUG

Part A: oral solution of 14C-OSI-906

OSI-906

OSI-906 DRUG

Part B: oral tablets OSI-906

OSI-906

Eligibility Criteria

• Age: 18 Years+
• Sex: all
• Healthy Volunteers: No
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• The subject has histologically or cytologically confirmed diagnosis of advanced solid tumor (measurable or non-measurable disease) for which no conventional therapy is available
• The subject has an Eastern Cooperative Oncology Group (ECOG) Performance Status (PS) ≤ 2
• The subject has a predicted life expectancy ≥12 weeks
• The subject has a fasting glucose ≤125 mg/dL (7 mmol/L) at Screening, Day -1 and pre-dose Day 1
• The subject has adequate organ function defined by the following laboratory parameters:
• absolute neutrophil count (ANC) ≥1.5 x 10 9/L
• platelet count ≥100 x 10 9/L
• total bilirubin ≤1.5 x upper limit of normal (ULN)
• aspartate aminotransferase (AST) and alanine aminotransferase (ALT) ≤ 2.5 x ULN, or ≤ 5 x ULN if subject has documented liver metastases
• serum creatinine ≤1.5 x ULN
• potassium, calcium, and magnesium within normal limits or determined by the investigator to be not clinically significant (NCS)
• The subject has a negative cotinine test
• If male, is surgically sterile, or is using a medically acceptable method to prevent pregnancy and agrees to continue using this method while participating in the study and for 90 days after the last dose of study medication
• If female, the subject is surgically sterile or status post hysterectomy, post-menopausal, or is using 2 forms of medically acceptable methods of birth control, one of which must be a barrier method to prevent pregnancy and agrees to continue using this method from screening until 90 days after the last dose of study medication
• If female, the subject must not be breastfeeding at Screening, during the study period and for 90 days after last dose of study drug administration

You may not qualify if:

• The subject has Type 1 or Type 2 diabetes mellitus currently requiring insulinotropic or insulin therapy
• The subject has a history of poorly controlled gastrointestinal disorder (s) that could affect the absorption or metabolism of study drug
• The subject has used IGF-1R inhibitor therapy in last 6 months
• The subject has hepatocellular carcinoma
• The subject has used a CYP1A2 inhibitor or inducer within 14 days prior to Day 1
• The subject has used drugs with a risk of causing QTc interval prolongation and Torsade de Pointes (TdP) within 14 days prior to Day 1
• The subject has a history (within last 6 months) of significant cardio-vascular disease
• The subject has a history (within the last 6 months) of significant arrhythmia disease, unless the disease is well-controlled with medication per the Principal Investigator's clinical judgment
• The subject has had major surgery ≤ 3 weeks prior to Day 1
• The subject has had radiation ≤ 3 weeks prior to Day 1
• The subject has had chemotherapy ≤ 3 weeks prior to Day 1
• The subject has participated in a radiolabeled study in the last 12 months
• The subject has a history of cerebrovascular accident (CVA) within 6 months prior to Day 1 or that resulted in ongoing neurologic instability
• The subject has an active infection or serious underlying medical condition (including any type of active seizure disorder within 12 months prior to Day 1) that would impair the ability of the subject to receive study drug
• The subject has participated in any interventional clinical study within 21 days or has been treated with any investigational drugs within 30 days or 5 half lives whichever is longer, prior to the initiation of Screening

Sponsors & Collaborators

• Astellas Pharma Global Development, Inc.: lead

Study Sites (2)

Northwest Medical Specialties, PLLC

Tacoma, Washington, 98405, United States

Location

Comprehensive Clinical Development NW, Inc.

Tacoma, Washington, 98418, United States

Location

Related Links

• Link to results on the Astellas Clinical Study Results website

MeSH Terms

Conditions

Neoplasms

Interventions

3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo(1,5-a)pyrazin-3-yl)-1-methylcyclobutanol

Study Officials

• Medical Director

  Astellas Pharma Global Development

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: OTHER
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: February 7, 2012
• First Posted: February 9, 2012
• Study Start: March 19, 2012
• Primary Completion: December 8, 2012
• Study Completion: February 20, 2013
• Last Updated: November 7, 2024

Record last verified: 2024-10

Data Sharing

• IPD Sharing: Will not share

Locations

US (2)