Status:

COMPLETED

A Study to Evaluate the Pharmacokinetics, Pharmacodynamics and Safety of ASP8232 in Subjects With Renal Impairment and in Type 2 Diabetes Mellitus Subjects With Chronic Kidney Disease

Lead Sponsor:

Astellas Pharma Europe B.V.

Conditions:

Healthy Subjects

Pharmacokinetics of ASP8232

Eligibility:

All Genders

35-80 years

Phase:

PHASE1

PHASE2

Brief Summary

This study consists of two parts. Part 1 evaluates the effect of renal impairment on the PK and PD of a single dose of ASP8232. In addition, the safety and tolerability will be assessed. Part 2 eval...

Detailed Description

This is a two-part study. Part 1 compares the pharmacokinetics (PK), pharmacodynamics (PD) and safety and tolerability of ASP8232 in healthy subjects with subjects with different degrees of renal impa...

Eligibility Criteria

Inclusion

  • Main Inclusion: Part 1
  • Independent Ethics Committee (IEC)-approved written Informed Consent and privacy language as per national regulations must be obtained from the subject or legally authorized representative prior to any study-related procedures (including withdrawal of prohibited medication, if applicable).
  • Male subject and his female spouse/partner who is of childbearing potential must be using highly effective contraception consisting of 2 forms of birth control (1 of which must be a barrier method) starting at screening and continue throughout the study period and for 28 days (or 5 half-lives of the study drug whichever is longer) after final study drug administration.
  • Male subject must not donate sperm starting at screening and throughout the study period and for at least 90 days after final study drug administration.
  • Female subject must be either:
  • post-menopausal (defined as at least one year without any menses) prior to screening, or
  • premenarchal prior to screening, or
  • documented surgically sterile or status post hysterectomy (at least 1 month before screening), or
  • if of childbearing potential, must have a negative urine pregnancy test at screening and must be using highly effective contraception. All females of childbearing potential will be required to use highly effective contraception consisting of 2 forms of birth control (1 of which must be a barrier method) starting at screening and throughout the study period and for 28 days (or 5 half-lives of the study drug whichever is longer) after final study drug administration.
  • Female subject must not be lactating, and must not be breast feeding at screening or during the study period and for 28 days \[or 5 half-lives of the study drug whichever is longer\] after final study drug administration.
  • Female subject must not donate ova starting at screening and throughout the study period and for 28 days \[or 5 half-lives of the study drug whichever is longer\] after final study drug administration.
  • Subject agrees not to participate in another interventional study while on treatment.
  • Healthy Subjects:
  • Subject must have pre dose eGFR values (based on the MDRD method) at screening and day -1 higher or equal to 80 mL/min/1.73 m2.
  • Renal Impaired Subjects:
  • Subject must have pre dose eGFR values (based on the MDRD method) at screening and day -1 of 15 to \< 30 mL/min/1.73 m2, 30 to
  • \< 60 mL/min/1.73 m2 or 60 to \< 80 mL/min/1.73 m2 for severe, moderate or mild renal impaired subjects, respectively.
  • Part 2 Inclusion:
  • Independent Ethics Committee (IEC)-approved written Informed Consent and privacy language as per national regulations must be obtained from the subject or legally authorized representative prior to any study-related procedures (including withdrawal of prohibited medication, if applicable).
  • Subject has either known or confirmed T2DM with CKD for at least 1 year \[screening\].
  • Subject is ≥ 35 and ≤ 80 years of age.
  • Male subject and his female spouse/partner who is of childbearing potential must be using highly effective contraception consisting of 2 forms of birth control (1 of which must be a barrier method) starting at screening and continue throughout the study period and for 28 days (or 5 half-lives of the study drug whichever is longer) after final study drug administration.
  • Male subject must not donate sperm starting at screening and throughout the study period and for at least 90 days after final study drug administration.
  • Female subject must be either
  • post-menopausal (defined as at least one year without any menses) prior to Screening, or
  • premenarchal prior to screening, or
  • documented surgically sterile or status post hysterectomy (at least 1 month before screening), or
  • if of childbearing potential, must have a negative urine pregnancy test at screening and must be using highly effective contraception1. All females of childbearing potential will be required to use highly effective contraception consisting of 2 forms of birth control (1 of which must be a barrier method) starting at screening and throughout the study period and for 28 days (or 5 half-lives of the study drug whichever is longer) after final study drug administration.
  • Female subject must not be lactating, and must not be breast feeding at screening or during the study period and for 28 days (or 5 half-lives of the study drug whichever is longer) after final study drug administration.
  • Female subject must not donate ova starting at screening and throughout the study period and for 28 days (or 5 half-lives of the study drug whichever is longer\] after final study drug administration.
  • Subject is on a stable therapy with ACE inhibitors or ARB for at least 3 months \[screening\].
  • Subject is on a stable anti-hyperglycaemia therapy, e.g. with Metformin, SUD, TZD or DPP-4 inhibitor.
  • Subject's eGFR is between 15-60 mL/min/1.73 m2 (based on the MDRD method).
  • Subject's HbA1c level is lower than 7.5% at clinic admission on day -2.
  • Subject has a stable blood pressure for at least 3 to 6 months prior to enrolment.
  • Subject's UACR is higher than 30 mg/g at clinic admission on day -2.
  • Part 1 Exclusion:
  • All Subjects:
  • Female subject who has been pregnant within 6 months before screening or breast feeding within 3 months before screening.
  • Subject has a known or suspected hypersensitivity to ASP8232, or any components of the formulation used.
  • Subject has any clinically significant history of allergic conditions (including drug allergies, asthma, eczema, or anaphylactic reactions, but excluding untreated, asymptomatic, seasonal allergies at time of dosing).
  • Subject has Gilbert's syndrome.
  • Subject has/had febrile illness or symptomatic, viral, bacterial (including upper respiratory infection), or fungal (non-cutaneous) infection within 1 week prior to clinic check in.
  • Subject has a history of smoking more than 10 cigarettes (or equivalent amount of tobacco) per day within 3 months prior to admission to the Clinical Unit.
  • Subject has a history of drinking more than 21 units of alcohol per week (1 unit = 10 g pure alcohol = 250 mL of beer \[5%\] or 35 mL of spirits \[35%\] or 100 mL of wine \[12%\]) (\> 14 units of alcohol for female subjects) within 3 months prior to admission to the Clinical Unit.
  • Subject uses drugs of abuse within 3 months prior to admission to the Clinical Unit.
  • Subject regularly uses any inducer of metabolism (e.g. barbiturates, rifampin ) in the 3 months prior to admission to the Clinical Unit.
  • Subject had any significant blood loss, donated one unit (450 mL) of blood or more, or received a transfusion of any blood or blood products within 60 days or donated plasma within 7 days prior to clinic admission on day -1.
  • Subject has positive serology test for Hepatitis B Surface Antigen (HBsAg), anti-Hepatitis A virus (anti-HAV \[IgM\]), anti-Hepatitis C virus (anti-HCV) or anti- Human immunodeficiency virus 1 + 2 (anti-HIV 1+2).
  • Subject participated in any interventional clinical study or has been treated with any investigational drugs within 30 days or 5 half-lives whichever is longer, prior to the initiation of screening.
  • Subject is an employee of the Astellas Group or Clinical Research Organization (CRO) involved in the study.
  • Healthy Subjects:
  • Subject has any of the liver function tests (Alanine Aminotransferase \[ALT\], Aspartate Aminotransferase \[AST\], total bilirubin \[TBL\]) above the upper limit of normal. In such a case the assessment may be repeated once \[day -1\].
  • Subject has a mean QTc(F) interval of \> 430 ms (for males) and \> 450 ms (for females) at screening and day -1. If the mean QTc(F) exceeds the limits above, one additional triplicate electrocardiogram (ECG) can be taken. If this triplicate also gives abnormal result the subject should be excluded.
  • Subject uses any prescribed or non-prescribed drugs (including vitamins, hormone replacement therapy, natural and herbal remedies, e.g. St. John's Wort) in the 2 weeks prior to study drug administration, except for occasional use of paracetamol (up to 2 g/day).
  • Renal Impaired Subjects:
  • Subject is on or requires hemodialysis or has received a kidney transplantation.
  • Subject has a supine mean systolic blood pressure \< 90 or \> 160 mmHg and a mean diastolic blood pressure \< 50 or \> 100 mmHg, or pulse rate \< 40 or \> 90 beats p/m, on screening and day -1. In such a case the assessment may be repeated once (day -1).
  • Subject has a mean QTc(F) interval of \> 450 ms (for males) and \> 470 ms (for females) at screening and day -1. If the mean QTc(F) exceeds the limits above, one additional triplicate ECG can be taken. If this triplicate also gives abnormal result the subject should be excluded.
  • Subject has not been on a stable dose of allowed concomitant medications for at least 2 weeks prior to day 1 and/or for whom dose changes are likely to occur during the study.
  • Subject requires or is likely to require any new concomitant medications during the course of the study.
  • Subject has obstructive uropathy or other causes of renal impairment not related to parenchymal renal disorder and/or disease of the kidney.
  • Subject has renal disease secondary to malignancy.
  • Subject has a fluctuating or rapidly deteriorating renal function within 4 weeks prior to screening, as indicated by strongly varying or worsening of clinical and/or laboratory signs of renal impairment within the screening period.
  • Subject has any of the liver function tests (ALT, AST, TBL) out of range. In such a case the assessment may be repeated once \[day -1\].
  • ALT or AST \> 2 x upper limit of normal (ULN)
  • TBL \> 1.5 x ULN
  • Part 2 Exclusion
  • Female subject who has been pregnant within 6 months prior to screening assessment or breast feeding within 3 months prior to screening.
  • Subject has known or suspected hypersensitivity to ASP8232 or sinistrin, or any components of the formulation used.
  • Subject has participated in part 1 of the 8232-CL-0002 study.
  • Subject has a mean QTc(F) interval of \> 450 ms (for males) and \> 470 ms (for females) at screening and day -2. If the mean QTc(F) exceeds the limits above, one additional triplicate ECG can be taken. If this triplicate also gives abnormal result the subject should be excluded.
  • Subject has a pulse \< 40 or \> 90 bpm; mean systolic blood pressure \>140 mmHg; mean diastolic blood pressure \> 90 mmHg (measurements taken in triplicate after subject has been resting in supine position for 5 min; pulse will be measured automatically) at screening and day -2. In such a case the assessment may be repeated once \[day -2\].
  • Subject is on or requires hemodialysis or has received a kidney transplantation.
  • Subject has not been on a stable dose of allowed concomitant medications for at least 2 weeks prior to day 1 and/or for whom dose changes are likely to occur during the study.
  • Subject who requires or is likely to require any new concomitant medications during the course of the study.
  • Subject who has obstructive uropathy or other causes of renal impairment not related to parenchymal renal disorder and/or disease of the kidney.
  • Subject who has renal disease secondary to malignancy.
  • Subject who has a fluctuating or rapidly deteriorating renal function within 4 weeks prior to the study, as indicated by strongly varying or worsening of clinical and/or laboratory signs of renal impairment within the screening period.
  • Subject has type 1 diabetes mellitus.
  • Subject with any of the liver function tests (ALT, AST, TBL) out of range as indicated below. In such a case the assessment may be repeated once \[day -2\].
  • ALT or AST \> 2 x ULN
  • Total bilirubin \> 1.5 x ULN
  • Subject has had myocardial infarct or stroke within 6 months prior to screening.
  • The subject has Gilbert's Syndrome.
  • Subject has any clinically significant history of allergic conditions (including drug allergies, asthma, eczema, or anaphylactic reactions, but excluding untreated, asymptomatic, seasonal allergies at time of dosing).
  • The subject has/had febrile illness or symptomatic, viral, bacterial (including upper respiratory infection), or fungal (non-cutaneous) infection within one week prior to clinic admission on day -2.
  • Subject has a history of drinking more than 21 units of alcohol per week (1 unit = 10 g pure alcohol = 250 mL of beer \[5%\] or 35 mL of spirits \[35%\] or 100 mL of wine \[12%\]) (\> 14 units of alcohol for female subjects) within 3 months prior to admission to the Clinical Unit.
  • Subject uses of drugs of abuse within 3 months prior to admission to the Clinical Unit.
  • Subject regularly uses any inducer of metabolism (e.g. barbiturates, rifampin) in the 3 months prior to admission to the Clinical Unit.
  • Subject had any significant blood loss, donated one unit (450 mL) of blood or more, or received a transfusion of any blood or blood products within 60 days or donated plasma within 7 days prior to clinic admission on day -2.
  • Subject has positive serology test for HBsAg, anti HAV (IgM), anti-HCV or anti-HIV 1+2.
  • Subject participated in any interventional clinical study or has been treated with any investigational drugs within 30 days or 5 half-lives whichever is longer, prior to the initiation of screening.
  • Subject is employee of the Astellas Group or CRO involved in the study.

Exclusion

    Key Trial Info

    Start Date :

    September 16 2013

    Trial Type :

    INTERVENTIONAL

    Allocation :

    ACTUAL

    End Date :

    September 9 2014

    Estimated Enrollment :

    55 Patients enrolled

    Trial Details

    Trial ID

    NCT02218099

    Start Date

    September 16 2013

    End Date

    September 9 2014

    Last Update

    October 31 2024

    Active Locations (3)

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    Page 1 of 1 (3 locations)

    1

    Site: 35901

    Sofia, Bulgaria, 1612

    2

    Site: 37301

    Chisinau, Moldova

    3

    Site: 40001

    Bucharest, Romania, 10731

    A Study to Evaluate the Pharmacokinetics, Pharmacodynamics and Safety of ASP8232 in Subjects With Renal Impairment and in Type 2 Diabetes Mellitus Subjects With Chronic Kidney Disease | DecenTrialz