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Pharmacokinetics of XNW4107 in Subjects With Various Degrees of Renal Function

E

Evopoint Biosciences

Status and phase

Completed
Phase 1

Conditions

Bacterial Infections

Treatments

Drug: XNW4107, Imipenem/Cilastatin

Study type

Interventional

Funder types

Industry

Identifiers

NCT04787562
XNW4107-003

Details and patient eligibility

About

This is a Phase 1, open-label study to assess the PK, safety and tolerability of XNW4107, imipenem and cilastatin administered by 60-minute (60-min) IV infusion to adults with various degrees of renal insufficiency as compared to subjects with normal renal function.

Enrollment

39 patients

Sex

All

Ages

18+ years old

Volunteers

Accepts Healthy Volunteers

Inclusion criteria

    1. Adult males or females, 18 years of age or older.

    2. BMI ≥ 18.5 and ≤ 39.9 (kg/m²) and weight between 50.0 and 130.0 kg (inclusive).

    3. Medically healthy (Cohort 1 only) or medically stable without clinically significant acute or chronic illness (Cohorts 2-5) that may impact the assessment of PK and safety.

    4. Normal renal function with eGFR ≥90 mL/min/1.73m² (Cohort 1), or renal insufficiency with eGFR 60 to <90 mL/min/1.73m² (Cohort 2), 30 to <60 mL/min/1.73m² (Cohort 3), or 15 to <30 mL/min/1.73m² (Cohort 4), ESRD receiving HDs at least 3 times per week for at least 3 months at Screening (Cohort 5)

    5. Participants of reproductive potential (male or female) must be willing to use contraception.

    6. Ability and willingness to abstain from alcohol, caffeine, xanthine-containing beverages or food or product containing any of these from 48 hours prior to study drug administration until discharge from the clinical unit.

Exclusion criteria

    1. Any clinically significant medical history or abnormal findings upon physical examination, or clinical laboratory tests.

    2. Electrocardiogram (ECG) with QTcF interval duration equal or greater than 500 msec obtained at Screening or Check-In.

    3. Results for alanine aminotransferase (ALT), aspartate aminotransferase (AST) and bilirubin greater than 1.5 × the upper limit of normal (ULN) for the reference laboratory.

    4. History of chronic liver disease, cirrhosis, or biliary disease.

    5. History or presence of CNS disorders, seizures, or other CNS adverse reactions such as confusional states and myoclonic activity.

    6. Positive testing for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) at Screening.

    7. Close contact with anyone who tested positive for SARS-CoV-2 infection, or presence of symptoms associated with SARS-CoV-2 infection at Screening or Check-in, or within 14 days prior to Screening.

    8. Recent history (within 6 months) of known or suspected Clostridium difficile infection.

    9. Positive testing for HIV Ab, HBsAg or HCV Ab.

    10. Recent history of substance or alcohol abuse within the previous year, or habitual use of tobacco or nicotine products or smoking within 3 months prior to Screening.

    11. Positive drug screen and alcohol testing at Screening or Check-in.

    12. For subjects with normal renal function (Cohort 1), the use of any over-the-counter (OTC) medications within 7 days prior to study drug administration or use of prescription medications including nonsteroidal anti-inflammatory drugs, health supplements, and herbal remedies taken within 13 days prior to study drug administration.

    13. For subjects with renal impairment (Cohorts 2-5), the use of prohibited concomitant medication with the exception of those essential for the management of renal impairment and other concomitant stable medical conditions as per the discretion of the Investigator.

    14. Use of probenecid or valproic acid within 30 days prior to study drug administration.

    15. Receipt of an investigational drug within 30 days or 5 half-lives prior to the first administration of study drug, whichever is longer.

    16. Known history of clinically significant hypersensitivity reaction or anaphylaxis to any medication, or history of clinically significant hypersensitivity to the study drug or any related drugs or to any of the excipients, or history of food intolerance.

    17. Donation of blood or plasma within 30 days prior to dosing, or loss of whole blood of more than 500 mL within 30 days prior to dosing, or receipt of a blood transfusion within 1 year of study enrollment.

Trial design

Primary purpose

Basic Science

Allocation

Non-Randomized

Interventional model

Parallel Assignment

Masking

None (Open label)

39 participants in 5 patient groups

Cohort 1: normal renal function
Experimental group
Description:
Participants with an eGFR ≥ 90 mL/min/1.73m2 receive a single dose of XNW4107 250mg IV co-administered with imipenem 500mg /cilastatin 500mg
Treatment:
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Cohort 2: Mild renal insufficiency
Experimental group
Description:
Participants with an eGFR 60 to \<90 mL/min/1.73m2 receive a single dose of XNW4107 250mg IV co-administered with imipenem 500mg /cilastatin 500mg
Treatment:
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Cohort 3: Moderate renal insufficiency
Experimental group
Description:
Participants with an eGFR 30 to \<60 mL/min/1.73m2 receive a single dose of XNW4107 250mg IV co-administered with imipenem 500mg /cilastatin 500mg
Treatment:
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Cohort 4: Severe renal insufficiency
Experimental group
Description:
Participants with an eGFR 15 to \<30 mL/min/1.73m2 receive a single dose of XNW4107 100mg IV co-administered with imipenem 200mg /cilastatin 200mg
Treatment:
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Cohort 5: End-stage renal disease (ESRD) receiving hemodialysis (HD) therapy
Experimental group
Description:
Participants with ESRD receiving HD therapy at least 3 times a week for at least 3 months prior to Screening visit receive a single dose of XNW4107 100mg IV co-administered with imipenem 200mg /cilastatin 200mg
Treatment:
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin
Drug: XNW4107, Imipenem/Cilastatin

Trial contacts and locations

2

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Data sourced from clinicaltrials.gov

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